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Celecoxib

別名: SC 58635 中文名稱：塞來昔布

Celecoxib是一種選擇性COX-2抑制劑，在Sf9細胞中IC50為40 nM。

Celecoxib Chemical Structure

Celecoxib Chemical Structure

CAS: 169590-42-5

規(guī)格 價格 庫存 購買數(shù)量
10mM (1mL in DMSO) 997 現(xiàn)貨
100mg 780.67 現(xiàn)貨
1g 2213.24 現(xiàn)貨
更大包裝 有超大折扣

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Celecoxib相關(guān)產(chǎn)品

相關(guān)信號通路圖

COX Signaling Pathways

COX信號通路圖

細胞實驗數(shù)據(jù)示例

細胞系 實驗類型 給藥濃度 孵育時間 活性描述 文獻信息
LNCaP Growth Inhibition Assay 2/5/10 μM 96 h inhibits cell growth significantly combined with atorvastatin 24296978
CF33 Function Assay 10-100 μM 4-24 h decreases cells in the S phase and increases cells in G0/G1 arrest 24503782
CF33 Growth Inhibition Assay 10-100 μM 0-4 d inhibits cell proliferation in a dose-dependent manner 24503782
CF33 Function Assay 100 μM 24 h induces downregulation of COX-2 protein expression 24503782
OVCAR-3 Function Assay 10 μM 1 h inhibits paclitaxel-induced Akt phosphorylation 24520227
OVCAR-3 Function Assay 10 μM 1 h down-regulates NF-κB activation induced by paclitaxel 24520227
OVCAR-3 Function Assay 10 μM 1 h enhances paclitaxel-induced activation of caspase-9? 24520227
OVCAR-3 Apoptosis Assay 10 μM 1 h promotes paclitaxel-induced apoptosis? 24520227
LMeC Function Assay 20/50 μM 48 h induces caspase-3 activation 24656746
OVCAR-3 Cell Viability Assay 10 μM 1 h enhances paclitaxel-induced ovarian cancer cell death? 24520227
CMeC-1 Function Assay 20/50 μM 48 h induces caspase-3 activation 24656746
LMeC Function Assay 20/50 μM 48 h decreases the levels of cyclin D1 in a dose-dependent manner 24656746
CMeC-1 Function Assay 20/50 μM 48 h decreases the levels of cyclin D1 in a dose-dependent manner 24656746
LMeC Function Assay 20/50 μM 48 h induces G1-S arrest 24656746
CMeC-1 Function Assay 20/50 μM 48 h induces G1-S arrest 24656746
LMeC Cell Viability Assay 20/50 μM 48 h inhibits cell viability in a dose dependent manner 24656746
CMeC-1 Cell Viability Assay 20/50 μM 48 h inhibits cell viability in a dose dependent manner 24656746
LMeC? Function Assay 20/50 μM 48 h decreases the expression of COX-2 protein 24656746
SGC-7901 Function Assay 75/100/125 μM 24/48/72 h increases caspase-8 and -9 mRNA expression in both time and dose manner 24676394
SGC-7901 Apoptosis Assay 100 μM 72 h induces apoptosis 24676394
SGC-7901 Growth Inhibition Assay 50-125 μM 24/48/72 h inhibits cell growth in both time and dose dependent manner 24676394
SNU-1041 Function Assay 0-40 μM 4 h up-regulates CHOP?after treatment with high concentrations 24692703
SNU-1041 Function Assay 20/30 μM 4 h induces expression of?CHOP, GRP78?and?XBP1?at the RNA level? 24692703
SNU-1041 Growth Inhibition Assay 0-40 μM 48 h inhibits cell viability in a dose dependent manner 24692703
CNE-1 Cytotoxicity Assay 60 μM 7 d enhances radiation cytotoxicity through COX-2-dependent manner 24854838
C666-1 Cytotoxicity Assay 60 μM 7 d enhances radiation cytotoxicity through COX-2-dependent manner 24854838
CNE-2 Cytotoxicity Assay 20-80 μM 24 h decreases colony formation in a dose-dependent manner? 24854838
CNE-1 Cytotoxicity Assay 20-80 μM 24 h decreases colony formation in a dose-dependent manner? 24854838
C666-1 Cytotoxicity Assay 20-80 μM 24 h decreases colony formation in a dose-dependent manner? 24854838
MKN-45 Function Assay 10/50/100 μM 48 h downregulates the mRNA expression levels of COX-2 and PCNA in a dose dependent manner 24992958
SGC-7901 Function Assay 10/50/100 μM 48 h downregulates the mRNA expression levels of COX-2 and PCNA in a dose dependent manner 24992958
MKN-45 Growth Inhibition Assay 10/50/100 μM 24/48/72 h inhibits cell growth in both time and dose dependent manner 24992958
SGC-7901 Growth Inhibition Assay 10/50/100 μM 24/48/72 h inhibits cell growth in both time and dose dependent manner 24992958
Hep-2 Function Assay 50 μM 0-48 h reduces the telomerase activity gradually 24998564
Hep-2 Function Assay 50 μM 0-48 h decreases the mRNA expression of hTERT 24998564
Hep-2 Apoptosis Assay 50 μM 0-48 h induces apoptosis in a time dependent manner 24998564
Hep-2 Growth Inhibition Assay 30/50/100 μM 12/24/36/48 h inhibits cell growth in both time and dose dependent manner 24998564
HSC3? Function Assay 25 μM 72 h decreases MMP-2 and MMP-9 proteins? 25198789
HSC3? Function Assay 25 μM 48 h inhibits HSC3 cell invasion combined with CET 25198789
HSC3? Function Assay 25 μM 48 h exhibits significantly reduced migration combined with CET 25198789
HSC3? Apoptosis Assay 25 μM 48 h induces apoptosis 25198789
HSC3? Cell Viability Assay 0–40 μM 48 h IC50=25.5±1.780 μM 25198789
HT-29? Function Assay 10-50 μM 6-36 h induces the expression of COX-2 in both dose and time dependent manner 25218028
HCT-15 Function Assay 10-50 μM 6-36 h induces the expression of COX-2 in both dose and time dependent manner 25218028
SKOV3? Function Assay 5/10/15 μM 1 h increases the expression of p-AKT and p-ERK in a dose-dependent manner 25424898
A2780 Function Assay 5/10/15 μM 1 h increases the expression of p-AKT and p-ERK in a dose-dependent manner 25424898
SKOV3? Function Assay 5/10/15 μM 48 h decreases the expression of N-cadherin and Vimentin 25424898
A2780 Function Assay 5/10/15 μM 48 h decreases the expression of N-cadherin and Vimentin 25424898
SKOV3? Function Assay 5/10/15 μM 48 h elevates the expression of E-cadherin and keratin 25424898
A2780 Function Assay 5/10/15 μM 48 h elevates the expression of E-cadherin and keratin 25424898
SKOV3? Function Assay 5/10/15 μM 48 h decreases Cox-2 expression in a dose-dependent manner 25424898
A2780 Function Assay 5/10/15 μM 48 h decreases Cox-2 expression in a dose-dependent manner 25424898
MCF7-MX? Function Assay 0-40 μM 4-24 h enhances the effects of TPA on ABCG2 expression? 25587329
MDA-MB-231 Function Assay 0-40 μM 4-24 h stimulates the expression of ABCG2 up to 4.27 times to control level by 12 h? 25587329
MCF-7 Function Assay 0-40 μM 4-24 h enhances the effects of TPA on ABCG2 expression? 25587329
MDA-MB-231 Function Assay 0-40 μM 4-24 h increases COX-2 protein expression in both time and dose dependent manner 25587329
LNCaP Apoptosis Assay 2/5/10 μM 96 h induces apoptosis combined with atorvastatin 24296978
MDA-MB-231? Growth Inhibition Assay 1/10 μM 72 h enhances calcitriol-induced cell growth inhibition 25667510
MCF-7? Growth Inhibition Assay 1/10 μM 72 h enhances calcitriol-induced cell growth inhibition 25667510
SGC7901 Function Assay 40?μM 8/16/24 h upregulats Cbl-b expression 25701378
MGC803 Function Assay 40?μM 8/16/24 h upregulats Cbl-b expression 25701378
SGC7901 Growth Inhibition Assay 0-60 μM 72 h IC50=43.53?±?5.12 μM 25701378
MGC803 Growth Inhibition Assay 0-60 μM 72 h IC50=47.25?±?6.43 μM 25701378
HLCZ01 Function Assay 40?μM 24 h increases TRAIL expression combined with Interferon-α 25724899
HLCZ01 Apoptosis Assay 40?μM 24 h enhances apoptosis combined with IFN-α 25724899
HLCZ01 Function Assay 40?μM 24 h increases accumulation of G0/G1-phase cells combined with IFN-α 25724899
HLCZ01 Growth Inhibition Assay 0–60?μM 48 h inhibits cell growth in a dose dependent manner 25724899
SACC-83 Function Assay 20/40/80 μM 24?h upregulats PTEN partially by inhibiting Sp1, and activates PTEN and inactivates AKT 25770423
HeLa? Function Assay 20/40/80 μM 24?h upregulats PTEN partially by inhibiting Sp1, and activates PTEN and inactivates AKT 25770423
SACC-83 Apoptosis Assay 20?μM? 24?h enhances radiation-induced inhibition of cell apoptosis 25770423
HeLa? Apoptosis Assay 20?μM? 24?h enhances radiation-induced inhibition of cell apoptosis 25770423
SACC-83 Growth Inhibition Assay 20?μM? 24?h enhances radiation-induced inhibition of cell proliferation 25770423
HeLa? Growth Inhibition Assay 20?μM? 24?h enhances radiation-induced inhibition of cell proliferation 25770423
PANC-1 Function Assay 20/60/100 μM 24 h attenuats cell invasion and migration in a concentration-dependent manner? 25973062
PANC-1 Growth Inhibition Assay 20/60/100 μM 24/48/72 h inhibits cell growth in both time and dose dependent manner 25973062
TAF Function Assay 10?μM 48 h increases EGFR mRNA and protein expression 25987127
TAF Function Assay 10?μM 30-120 min poorly affects dAkt phosphorylation consequent to EGF signaling 25987127
TAF Function Assay 10?μM 7 d affects TAFs adhesive properties 25987127
H357 Growth Inhibition Assay 7.5/10 μM 48 h inhibits cell growth?combined with Sabutoclax 26009874
SGC-7901/DDP Function Assay 10?μM 24 h causes a marked decrease in the level of Bcl-2 protein 26407653
SGC-7901/DDP Function Assay 10?μM 24 h inhibits the expression of P-glycoprotein through blocking EP2, and inactivating PKA and CREB? 26407653
SGC-7901/DDP Apoptosis Assay 10?μM 24 h induces apoptosis combined with with cisplatin 26407653
SGC-7901/DDP Function Assay 10?μM 24 h inhibits cyclooxygenase-2 and P-glycoprotein expression 26407653
HCC827 Apoptosis Assay 80 μM 48?h? induces apoptosis 26464643
A549 Apoptosis Assay 80 μM 48?h? induces apoptosis 26464643
HCC827 Growth Inhibition Assay 5-160 μM 48?h? IC50=69.2 μM 26464643
A549 Growth Inhibition Assay 5-160 μM 48?h? IC50=163.4 μM 26464643
CaES-17 Apoptosis Assay 20?μM 48?h? reduces oxaliplatin-induced apoptosis 26474693
HKESC-2 Apoptosis Assay 20?μM 48?h? reduces oxaliplatin-induced apoptosis 26474693
CaES-17 Growth Inhibition Assay 20?μM 48?h? significantly increases the IC50?values of oxaliplatin? 26474693
HKESC-2 Growth Inhibition Assay 20?μM 48?h? significantly increases the IC50?values of oxaliplatin? 26474693
H460 Function Assay 0.1-30 μM 48 h induces ICAM-1 expression on both protein and mRNA level 26513172
A549 Function Assay 0.1-30 μM 48 h induces ICAM-1 expression on both protein and mRNA level 26513172
PC-3? Growth Inhibition Assay 0-50 μM 48?h inhibits cell growth in a dose dependent manner 24127882
PC-3? Cell Viability Assay 0-100 μM 72 h decreases cell viability in a dose dependent manner 24127882
A549 Function assay 5 uM 10 mins Inhibition of mPGES1 in IL1-beta induced human A549 cells assessed as PGE2 production at 5 uM preincubated for 10 mins 19884011
PANC1 Function assay 25 to 50 M 30 mins Inhibition of IL-6-induced STAT3 phosphorylation in human PANC1 cells at 25 to 50 M pretreated 2 hrs prior to IL-6 challenge measured after 30 mins 21678971
HCA-7 Function assay 5 uM 24 hrs Inhibition of hyaluronan-induced CD44v6 in human HCA-7 cells transfected with Has2cDNA assessed as downregulation of 5-LOX protein expression at 5 uM after 24 hrs by Western blotting analysis 24295787
HCA-7 Function assay 5 uM 24 hrs Inhibition of hyaluronan-induced CD44v6 in human HCA-7 cells transfected with Has2cDNA assessed as downregulation of COX-2 protein expression at 5 uM after 24 hrs by Western blotting analysis 24295787
HCA-7 Function assay 5 uM 24 hrs Inhibition of hyaluronan-induced CD44v6 in human HCA-7 cells transfected with Has2cDNA assessed as downregulation of COX-1 protein expression at 5 uM after 24 hrs by Western blotting analysis 24295787
HeLa Function assay 100 uM 24 hrs Inhibition of mPGES-1 in human HeLa cells using PGH2 as substrate assessed as inhibition of IL-1beta/TNFalpha-stimulated PGE2 production at 100 uM after 24 hrs by LC-MS/MS analysis 24183739
HeLa Function assay 0.1 uM 24 hrs Inhibition of PGE2 secretion in human HeLa cells at 0.1 uM after 24 hrs by EIA monoclonal assay 27349331
RAW264.7 Antiinflammatory assay 20 uM 2 hrs Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS induced cox-2 expression at 20 uM preincubated for 2 hrs followed by LPS challenge measured after 24 hrs by Western blot method 29100799
RAW264.7 Antiinflammatory assay 20 uM 2 hrs Antiinflammatory activity against mouse RAW264.7 cells assessed as inhibition of LPS induced iNOS expression at 20 uM preincubated for 2 hrs followed by LPS challenge measured after 24 hrs by Western blot method 29100799
A549 Function assay 5 uM Inhibition of mPGES1 in human A549 cells assessed as inhibition of IL-1-beta-induced PGE2 formation at 5 uM by cell-intact assay 19053751
HT29 Function assay 10 uM Inhibition of hyaluronan-induced CD44 antigen variant exon 6 activity in human HT29 cells assessed as decrease in 5-LOX expression at 10 uM 23517721
HT29 Function assay 10 uM Inhibition of hyaluronan-induced CD44 antigen variant exon 6 activity in human HT29 cells assessed as decrease in COX-2 expression at 10 uM 23517721
201T? Growth Inhibition Assay 72 h IC50=48.6 μM 25057941
273T Growth Inhibition Assay 72 h IC50=80.5 μM 25057941
SGC-7901/DDP Growth Inhibition Assay 24?h? IC50=35.45 μM 26407653
SGC-7901? Growth Inhibition Assay 24?h? IC50=115.08 μM 26407653
HCA-7 Function assay 72 hrs Inhibition of IL-1beta-induced PGE2 production in human HCA-7 cells after 72 hrs by EIA, EC50 = 0.00115 μM. 22516282
insect cells Function assay 1 min Inhibition of human recombinant COX2 expressed in insect cells using arachidonic acid as substrate incubated for 1 min prior to substrate addition measured for 25 secs by TMPD-based chromogenic assay, IC50 = 0.042 μM. 23010270
HNSCC 1483 Function assay 30 mins Inhibition of COX-2 in human HNSCC 1483 cells using [14C] arachidonic acid as substrate preincubated for 30 mins before substrate addition measured after 30 mins, IC50 = 0.054 μM. 22263894
J774 Function assay 15 mins Inhibition of COX2 in LPS-stimulated mouse J774 cells assessed as inhibition of PGE2 production after 15 mins by radioimmunoassay, IC50 = 0.06 μM. 18752957
J774 Function assay 24 hrs Inhibition of COX-2-mediated PGE2 production in LPS-stimulated mouse J774 cells after 24 hrs by radioimmunoassay, IC50 = 0.061 μM. 21992176
Sf21 Function assay 5 mins Inhibition of recombinant N-terminal His6-tagged human COX-2 expressed in Baculovirus infected Sf21 cells using arachidonic acid as substrate preincubated for 5 mins followed by substrate addition measured after 1 hr, IC50 = 0.26 μM. 30293795
SF9 Function assay 15 mins Inhibition of full length recombinant human N-terminal GST-tagged HDAC6 expressed in baculovirus infected sf9 cells using Boc-Lys-(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence assay, IC50 = 0.643 μM. 29500130
HT-29 Cytotoxicity assay 48 hrs Cytotoxicity against COX-2 positive human HT-29 cells transfected with CD44v6shRNA assessed as growth inhibition after 48 hrs by MTT assay, IC50 = 0.7 μM. 24295787
SF9 Function assay 15 mins Inhibition of recombinant Leishmania donovani chagasi beta-carbonic anhydrase expressed in baculovirus infected insect Sf9 cells incubated for 15 mins prior to testing by stopped flow CO2 hydrase assay, Ki = 0.705 μM. 23977960
HCA-7 Cytotoxicity assay 48 hrs Cytotoxicity against COX-2 positive human HCA-7 cells transfected with CD44v6shRNA assessed as growth inhibition after 48 hrs by MTT assay, IC50 = 0.75 μM. 24295787
HepG2 Antiproliferative assay 48 hrs Antiproliferative activity against human HepG2 cells incubated for 48 hrs by MTT assay, IC50 = 0.76 μM. 26346367
SF9 Function assay 15 mins Inhibition of full length recombinant human C-terminal FLAG/His-tagged HDAC1 expressed in baculovirus infected sf9 cells using Boc-Lys-(Ac)-AMC as substrate preincubated for 15 mins followed by substrate addition measured after 60 mins by fluorescence ass, IC50 = 1.185 μM. 29500130
RAW264.7 Antiinflammatory assay 18 hrs Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced TNF-alpha secretion after 18 hrs by sandwich ELISA, IC50 = 1.28 μM. 24679441
APC10.1 Cytotoxicity assay 48 hrs Cytotoxicity against COX-2 positive mouse APC10.1 cells transfected with CD44v6shRNA overexpressing HAS-2 assessed as growth inhibition after 48 hrs by MTT assay, IC50 = 1.3 μM. 24295787
RAW264.7 Antiinflammatory assay 30 mins Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production preincubated for 30 mins followed by LPS stimulation measured after 24 hrs by Griess assay, IC50 = 1.6 μM. 26444098
RAW264.7 Antiinflammatory assay 18 hrs Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced nitric oxide production after 18 hrs by griess reaction analysis, IC50 = 1.84 μM. 24679441
HCA-7 Cytotoxicity assay 18 hrs Cytotoxicity against human HCA-7 cells assessed as decrease in cell survival after 18 hrs by MTS assay, IC50 = 2 μM. 23517721
A549 Antiproliferative assay 48 hrs Antiproliferative activity against human A549 cells incubated for 48 hrs by MTT assay, IC50 = 2.15 μM. 26346367
Escherichia coli Arctic cells Function assay 15 mins Inhibition of recombinant Streptococcus mutans UA159 beta-carbonic anhydrase expressed in Escherichia coli Arctic cells preincubated for 15 mins by stopped flow CO2 hydrase assay, Ki = 2.425 μM. 25913199
HT-29 Cytotoxicity assay 18 hrs Cytotoxicity against human HT-29 cells assessed as decrease in cell survival after 18 hrs by MTS assay, IC50 = 3 μM. 23517721
J774 Function assay 15 mins Inhibition of COX1 in arachidonic acid-stimulated mouse J774 cells assessed as inhibition of PGE2 production after 15 mins by radioimmunoassay, IC50 = 3.7 μM. 18752957
J774 Function assay 15 mins Inhibition of COX-1-mediated PGE2 production in arachidonic acid-stimulated mouse J774 cells incubated for 15 mins prior to arachidonic acid-challenge by radioimmunoassay, IC50 = 3.84 μM. 21992176
J774 Function assay 15 mins Inhibition of COX1 in mouse J774 cells using arachidonic acid as substrate assessed as inhibition of PGE2 production incubated for 15 mins prior to substrate addition measured after 30 mins by radioimmunoassay, IC50 = 3.84 μM. 23680444
APC10.1 Cytotoxicity assay 18 hrs Cytotoxicity against mouse APC10.1 cells assessed as decrease in cell survival after 18 hrs by MTS assay, IC50 = 4.2 μM. 23517721
B16F10 Antiproliferative assay 24 hrs Antiproliferative activity against mouse B16F10 cells after 24 hrs by MTT assay, IC50 = 4.56 μM. 25866240
SH-SY5Y Antineurotoxicity assay 72 hrs Antineurotoxicity in human SH-SY5Y cells assessed as inhibition human THP1 cell supernatant-induced cytotoxicity compound pretreated 24 to 48 hrs to THP1 cells measured after 72 hrs of supernatant addition, IC50 = 5 μM. 20138770
THP1 Neuroprotective assay 72 hrs Neuroprotective activity against LPS and IFN-gamma-stimulated neurotoxin production in human THP1 cell assessed as inhibition of THP1 cell secretion-induced toxicity to human SH-SY5Y cells after 72 hrs by MTT assay, IC50 = 5 μM. 20609589
MCF7 Antiproliferative assay 24 hrs Antiproliferative activity against human MCF7 cells after 24 hrs by MTT assay, IC50 = 5.94 μM. 25866240
APC10.1 Function assay 18 hrs Inhibition of hyaluronan-induced CD44 antigen variant exon 6 activity in mouse APC10.1 cells expressing Has2 assessed as decrease in cell survival after 18 hrs by MTS assay, IC50 = 6 μM. 23517721
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells incubated for 48 hrs by MTT assay, IC50 = 6.88 μM. 26346367
HeLa Antiproliferative assay 24 hrs Antiproliferative activity against human HeLa cells after 24 hrs by MTT assay, IC50 = 7.35 μM. 25866240
HeLa Antiproliferative assay 48 hrs Antiproliferative activity against human HeLa cells incubated for 48 hrs by MTT assay, IC50 = 7.55 μM. 26346367
HeLa Antiproliferative assay 24 hrs Antiproliferative activity against human HeLa cells after 24 hrs by MTT assay, IC50 = 7.79 μM. 27349331
HepG2 Antiproliferative assay 24 hrs Antiproliferative activity against human HepG2 cells after 24 hrs by MTT assay, IC50 = 10.03 μM. 27349331
B16F10 Antiproliferative assay 24 hrs Antiproliferative activity against mouse B16F10 cells after 24 hrs by MTT assay, IC50 = 14.36 μM. 27349331
A549 Antitumor assay 48 hrs Antitumor activity against human A549 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay, IC50 = 15.6 μM. 23353741
A549 Antiproliferative assay 24 hrs Antiproliferative activity against human A549 cells after 24 hrs by MTT assay, IC50 = 15.64 μM. 27349331
HeLa Antiproliferative assay 48 hrs Antiproliferative activity against human HeLa cells after 48 hrs by MTT assay, IC50 = 15.69 μM. 30031652
A549 Antiproliferative assay 48 hrs Antiproliferative activity against human A549 cells after 48 hrs by MTT assay, IC50 = 16.08 μM. 30031652
NCI60 Growth inhibition assay 48 hrs Growth inhibition of human NCI60 cells after 48 hrs by sulforhodamine B assay, GI50 = 17.5 μM. 20387815
HCA-7 Function assay 18 hrs Inhibition of hyaluronan-induced CD44 antigen variant exon 6 activity in human HCA-7 cells expressing Has2 assessed as decrease in cell survival after 18 hrs by MTS assay, IC50 = 17.5 μM. 23517721
HT-29 Function assay 18 hrs Inhibition of hyaluronan-induced CD44 antigen variant exon 6 activity in human HT-29 cells expressing Has2 assessed as decrease in cell survival after 18 hrs by MTS assay, IC50 = 18.3 μM. 23517721
B16F10 Antiproliferative assay 48 hrs Antiproliferative activity against mouse B16F10 cells after 48 hrs by MTT assay, IC50 = 19.15 μM. 30031652
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay, IC50 = 26.78 μM. 30031652
LNCAP Cytotoxicity assay 72 hrs Cytotoxicity against human LNCAP cells assessed as cell growth inhibition after 72 hrs by MTT assay, IC50 = 32.6 μM. 28057407
BL21(DE3) Function assay 15 mins Inhibition of GST-tagged Malassezia globosa ATCC 96807/CBS 7966 MG-CA expressed in Escherichia coli BL21(DE3) cells preincubated for 15 mins measured for 10 to 100 sec by stopped-flow method, Ki = 34.8 μM. 22424239
MDA-MB-231 Cytotoxicity assay 48 hrs Cytotoxicity against human MDA-MB-231 cells after 48 hrs by MTS assay, IC50 = 40 μM. 22780961
MCF7 Antiproliferative assay 48 hrs Antiproliferative activity against human MCF7 cells after 48 hrs by MTT colorimetric assay, IC50 = 40.8 μM. 22000948
MCF7 Antitumor assay 48 hrs Antitumor activity against human MCF7 cells assessed as inhibition of cell proliferation after 48 hrs by MTT assay, IC50 = 40.8 μM. 23353741
HCT116 Anticancer assay 72 hrs Anticancer activity against human HCT116 cells after 72 hrs by MTT assay, IC50 = 43.3 μM. 21678971
L1210 Cytotoxicity assay 72 hrs Cytotoxicity against mouse L1210 cells after 72 hrs by MTT assay, IC50 = 44 μM. 20451397
PC3 Antiproliferative assay 72 hrs Antiproliferative activity against androgen-independent human PC3 cells after 72 hrs by MTT test, IC50 = 47 μM. 15566290
PC3 Antiproliferative assay 72 hrs Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay, IC50 = 48 μM. 17937972
PC3 Function assay 2 hrs Inhibition of PDK1-mediated Akt activation in human PC3 cells after 2 hrs by Western blotting analysis, IC50 = 48 μM. 23735281
PC3 Cytotoxicity assay 72 hrs Cytotoxicity against human PC3 cells after 72 hrs by MTT assay, IC50 = 48.5 μM. 20451397
MCF7 Antiproliferative assay 72 hrs Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay, IC50 = 49.66 μM. 29191502
CHO Function assay In vitro inhibitory potency against human COX-2 in stably transfected chinese hamster ovary (CHO) cells, IC50 = 0.002 μM. 10576684
CHO Function assay Inhibition of PGE-2 production in CHO cells expressing human COX-2, IC50 = 0.002 μM. 10576685
CHO Function assay In vitro potency against human Prostaglandin G/H synthase 2 in transfected CHO cells, IC50 = 0.002 μM. 10197970
CHO Function assay Inhibitory of human Prostaglandin G/H synthase 2 expressed in CHO cells, IC50 = 0.002 μM. 12643942
synovial cells Function assay Inhibitory effect on production of cyclooxygenase-2 (COX-2) prostaglandin E2 (PGE2) in human IL1-beta stimulated synovial cells, IC50 = 0.0079 μM. 10821716
RAW264.7 Function assay Inhibition of COX-2 in mouse RAW264.7 cells assessed as decrease in LPS-induced PGE2 production treated prior to LPS challenge by enzyme immunoassay, IC50 = 0.0087 μM. 24656662
HEK293 Function assay Inhibition of cloned Stylophora pistillata alpha-CA expressed in human HEK293 cells by stopped-flow CO2 assay, Ki = 0.0342 μM. 19520577
SF9 Function assay Inhibitory activity against human Prostaglandin G/H synthase 2 expressed in sf-9 cells infected with baculovirus, IC50 = 0.036 μM. 14698190
SF9 Function assay In vitro inhibitory activity against human recombinant prostaglandin G/H synthase 2 expressed in sf-9 cells infected with baculovirus, IC50 = 0.036 μM. 15026050
CHO Function assay Inhibition of COX2 expressed in CHO cells assessed as inhibition of arachidonic acid-stimulated PGE2 production by enzyme immunoassay, IC50 = 0.036 μM. 15566290
J774 Function assay Inhibition of COX2 in LPS-stimulated J774 cells assessed as inhibition of PGE2 levels by radioimmunoassay, IC50 = 0.06 μM. 17915854
J774 Function assay Inhibition of COX2 in mouse J774 cells assessed as inhibition of LPS-induced PGE2 production by radioimmunoassay, IC50 = 0.061 μM. 23680444
SF9 Function assay Inhibition of human COX2 expressed in baculovirus-infected SF9 cells assessed as inhibition of arachidonic acid-stimulated PGE2 production treated 1 hr before arachidonic acid challenge by enzyme immunoassay, IC50 = 0.063 μM. 19520573
COS Function assay Inhibition of human cyclooxygenase-2 expressed in COS cells, IC50 = 0.068 μM. 15454242
COS Function assay Inhibition of human COX2 expressed in african green monkey COS cells assessed as inhibition of arachidonic acid-stimulated PGE2 production treated 1 hr before arachidonic acid challenge by enzyme immunoassay, IC50 = 0.068 μM. 19520573
143982 Function assay In vitro inhibitory activity against human Prostaglandin G/H synthase 2 (COX-2) in 143982 cells, IC50 = 0.079 μM. 12877584
J774 Function assay In vitro inhibitory activity against Prostaglandin G/H synthase 2 in murine J774 cells, IC50 = 0.079 μM. 15857149
J774 Function assay Inhibition of COX2-dependent PGE2 production in LPS-stimulated mouse J774 cells by RIA, IC50 = 0.079 μM. 19957931
osteosarcoma cells Function assay Inhibition of Prostaglandin G/H synthase 2 in 143.98.2 from human osteosarcoma cells, IC50 = 0.08 μM. 11462976
SF9 Function assay Inhibition of human COX2 expressed in sf9 cells, IC50 = 0.08 μM. 16252917
RAW264.7 Antiinflammatory assay Antiinflammatory activity in mouse RAW264.7 cells assessed as inhibition of LPS-induced PGE2 production, IC50 = 0.1 μM. 22000948
RAW264.7 Function assay Inhibition of COX-2 in mouse RAW264.7 cells assessed as decrease in LPS-induced PGE2 production, IC50 = 0.12 μM. 23353741
Sf21 Function assay Inhibition of recombinant human N-terminal His-tagged COX2 expressed in baculovirus infected Sf21 cells assessed as reduction in prostaglandin production by enzyme immunoassay, IC50 = 0.15 μM. 29373271
MC9 Function assay Inhibition of PGF2apha production in arachidonic acid-stimulated mouse MC9 cells, IC50 = 0.3 μM. 18498150
MC9 Function assay Inhibition of PGF2alpha production in mouse MC9 cells, IC50 = 0.4 μM. 18498150
293E Function assay Inhibition of human microsomal PGES1 expressed in 293E cells by LC/MS/MS analysis, IC50 = 0.425 μM. 26653180
COS Function assay Inhibition of human cyclooxygenase-1 expressed in COS cells, IC50 = 1.689 μM. 15454242
COS Function assay Inhibition of human COX1 expressed in african green monkey COS cells assessed as inhibition of arachidonic acid-stimulated PGE2 treated 1 hr before arachidonic acid challenge by enzyme immunoassay, IC50 = 1.689 μM. 19520573
J774 Function assay Inhibition of COX1 in mouse J774 cells assessed as arachidonic acid-induced PGE2 levels by radio immunoassay, IC50 = 3.7 μM. 17915854
HCA-7 Cytotoxicity assay Cytotoxicity against COX-2 positive human HCA-7 cells assessed as growth inhibition by CellTiter-96 AQueous assay, IC50 = 4.9 μM. 24295787
U-937 Function assay Inhibition of Prostaglandin G/H synthase 1 in U-937 cells from human histiocytic lymphoma, IC50 = 5.1 μM. 11462976
U-937 Function assay In vitro inhibitory activity against human Prostaglandin G/H synthase 1 (COX-1) in U-937 cells, IC50 = 5.1 μM. 12877584
J774 Function assay In vitro inhibitory activity against Prostaglandin G/H synthase 1 in murine J774 cells, IC50 = 5.1 μM. 15857149
J774 Function assay Inhibition of COX1-dependent PGE2 production in LPS-stimulated mouse J774 cells by RIA, IC50 = 5.1 μM. 19957931
HT-29 Cytotoxicity assay Cytotoxicity against COX-2 positive human HT-29 cells assessed as growth inhibition by CellTiter-96 AQueous assay, IC50 = 5.7 μM. 24295787
SW480 Cytotoxicity assay Cytotoxicity against COX-2 negative human SW480 cells assessed as growth inhibition by CellTiter-96 AQueous assay, IC50 = 6.9 μM. 24295787
APC10.1 Cytotoxicity assay Cytotoxicity against COX-2 positive mouse APC10.1 cells overexpressing HAS-2 assessed as growth inhibition by CellTiter-96 AQueous assay, IC50 = 13.4 μM. 24295787
CHO Function assay Inhibition of COX1 expressed in CHO cells assessed as inhibition of arachidonic acid-stimulated PGE2 production by enzyme immunoassay, IC50 = 13.5 μM. 15566290
platelet Function assay Inhibitory effect on production of cyclooxygenase-1 (COX-1) thromboxane B2 (TXB2) in human platelet cells, IC50 = 19 μM. 10821716
MDA231 Antiproliferative assay Antiproliferative activity against human MDA231 cells by MTT assay, IC50 = 22.79 μM. 30216848
HCT116 Antiproliferative assay Antiproliferative activity against human HCT116 cells by MTT assay, IC50 = 29.54 μM. 30216848
MCF7 Antiproliferative assay Antiproliferative activity against human MCF7 cells by MTT assay, IC50 = 31.28 μM. 30216848
HeLa Antiproliferative assay Antiproliferative activity against human HeLa cells by MTT assay, IC50 = 36.08 μM. 30216848
Caco2 Antiproliferative assay Antiproliferative activity against human Caco2 cells by MTT assay, IC50 = 42.74 μM. 30216848
HT-29 Cytotoxicity assay Cytotoxicity against human HT-29 cells by MTT assay, IC50 = 45.5 μM. 20804197
PC3 Anticancer assay Anticancer activity against human PC3 cells, GI50 = 47 μM. 18262309
A549 Function assay Inhibition of COX2-dependent PGE2 production in IL1B stimulated human A549 cells in presence of arachidonic acid 18498150
A549 Function assay Inhibition of COX2-dependent PGE2 production in IL1B stimulated human A549 cells 18498150
Saos-2 qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for Saos-2 cells 29435139
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生物活性

產(chǎn)品描述 Celecoxib是一種選擇性COX-2抑制劑，在Sf9細胞中IC50為40 nM。
靶點
COX-2 [1]
(Sf9 cells)
40 nM
體外研究(In Vitro)
體外研究活性

在體外, Celecoxib有效選擇性抑制COX-2，IC50為40 nM, 而作用于COX-1時，IC50為15 μM。[1]Celecoxib 作用于鼻咽癌 (NPC)細胞系，包括 HNE1和CNE1-LMP1，具有抗增殖效果，IC50分別為32.86 μM 和 61.31 μM。[4]
激酶實驗 體外COX酶實驗
細胞勻漿與COX-1或COX-2桿狀病毒溫育3天，通過測評PG合成能力，而測定昆蟲細胞中COX蛋白表達。攪勻表達COX-1或COX-2的細胞，然后與花生四烯酸 (10 μM)混合。通過監(jiān)測PG產(chǎn)量，而測定COX活性。在模擬感染的Sf9細胞中檢測不出COX活性。Celecoxib與天然1% CHAPS 勻漿(2-10 μg 蛋白)預(yù)溫育10分鐘，然后加入花生四烯酸。溫育10分鐘后，通過ELISA檢測形成的PGE2。
細胞實驗 細胞系 HNE1和CNE1-LMP1
濃度 0 到75 μM
孵育時間 48 小時
方法

使用MTT實驗測定 Celecoxib 作用于 NPC細胞的抗增殖效果。細胞接種在96孔板上，粘附24小時。使用濃度不斷增高的Celecoxib (0 到 75 μM) （溶于 DMSO， 終濃度 ≤0.1%)處理細胞，然后再溫育48小時。 溫育后，每孔加入 20 μL MTT 染料 (5 mg/mL) ，然后在37oC下溫育4小時。移除上清液，晶體溶解在 DMSO 中，然后在490 nm處測定吸光值。使用 Probit回歸模型及SPSS 15.0 軟件計算IC50值和95%置信區(qū)間。每組實驗至少重復(fù)進行三次。
實驗圖片 檢測方法 檢測指標 實驗圖片 PMID
Western blot pAKT / AKT / PPARγ / PTEN COX-2 Fibronectin / Vimentin / N-cadherin / E-cadherin 24721996
Immunofluorescence PPARγ / PTEN 24721996
Growth inhibition assay Cell viability 28521485
體內(nèi)研究(In Vivo)
體內(nèi)研究活性

在體內(nèi), Celecoxib 具有有效的口服抗炎活性。Celecoxib 降低卡拉膠水腫檢測中的急性炎癥，也降低佐劑性關(guān)節(jié)炎模型中的慢性炎癥，ED50分別為7.1 mg/kg和 0.37 mg/kg/day。此外, Celecoxib作用于Hargreaves 痛模型，也具有鎮(zhèn)痛活性，ED50為34.5 mg/kg。此外, Celecoxib 按200 mg/kg劑量處理大鼠，不會產(chǎn)生急性GI毒性，每天按600 mg/kg劑量處理大鼠，持續(xù)10天以上，不會產(chǎn)生GI毒性。[1]13.5 Gy 局部胸部照射(LTI)142天(范圍為 94-155 天)后，Celecoxib 作用于C3Hf/KamLaw 雌性小鼠模型，提高105天的平均壽命 (范圍為79-145 天)。[5]
動物實驗 Animal Models 溶于0.9%生理鹽水的0.1 mL 1%卡拉膠溶液或溶于50 μL 礦物油的1 mg 乳酸分枝桿菌注射到雄性Sprague?Dawley大鼠右后腿足墊
Dosages ≤200 mg/kg
Administration 口服處理
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT01344200 Recruiting
Pharmacokinetics of Celecoxib in Children
Children''s Hospital of Eastern Ontario
 January 29 2024 Phase 2
NCT05648916 Enrolling by invitation
Heterotopic Ossification
McGill University Health Centre/Research Institute of the McGill University Health Centre
 August 2 2022 --
NCT05256823 Active not recruiting
To Evaluate the Safety and Efficacy of Celecoxib Plus Nucleos(t)Ide Analogues in Nucleos(t)Ide-treated Patients With Chronic Hepatitis B
Lai Wei|Beijing Tsinghua Chang Gung Hospital
 February 24 2022 Phase 2
NCT05324163 Completed
KNEE OSTEOARTHRITIS
Jiangsu XinChen-Techfields Pharma Co. LTD.
 September 29 2021 Phase 3
NCT04526197 Completed
Wilson Disease
Alexion Pharmaceuticals Inc.
 July 7 2020 Phase 1

化學(xué)信息&溶解度

分子量 381.37 分子式

C17H14F3N3O2S
CAS號 169590-42-5 SDF Download Celecoxib SDF
Smiles CC1=CC=C(C=C1)C2=CC(=NN2C3=CC=C(C=C3)S(=O)(=O)N)C(F)(F)F
儲存條件(自收到貨起)

體外溶解度
批次：

DMSO : 76 mg/mL ( (199.28 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Ethanol : 76 mg/mL (199.28 mM)

Water : Insoluble

摩爾濃度計算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請按從左到右的順序依次添加，澄清后再加入下一溶劑

 動物體內(nèi)配方計算器

實驗計算

摩爾濃度計算器

質(zhì)量 濃度 體積 分子量

動物體內(nèi)配方計算器（澄清溶液）

第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）

mg/kg g μL 只

第二步：請輸入動物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過該批次藥物DMSO溶解度，請先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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常見問題及建議解決方法

問題 1:
I am doing an animal experiment with mice and planning to administrate S1261 via oral gavage. what are your recommendations for diluting the compound?

回答：
For oral administration, Celecoxib can be dissolved in vehicle one: "0.5% methyl cellulose and 0.025% Tween-20", or the vehicle 2 "2% DMSO/30% PEG 300/5% Tween 80/ ddH2O".

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