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LY294002

別名: SF 1101, NSC 697286

LY294002 (SF 1101, NSC 697286) 是首個(gè)合成的已知抑制PI3Kα/δ/β的小分子,在無細(xì)胞測(cè)定中IC50分別為 0.5 μM/0.57 μM/0.97 μM;在溶液中比在Wortmannin中穩(wěn)定,也能夠阻斷自噬體的形成。它不僅能夠結(jié)合class I PI3Ks和其他PI3K相關(guān)的激酶,還能夠結(jié)合一些與PI3K家族無關(guān)的新型靶點(diǎn)。LY294002 可以抑制CK2,對(duì)應(yīng)的IC50值為98 nM。LY294002 是一種非特異的 DNA-PKcs 抑制劑,并可激活自噬和凋亡。

LY294002 Chemical Structure

LY294002 Chemical Structure

CAS: 154447-36-6

規(guī)格 價(jià)格 庫存 購買數(shù)量
10mM (1mL in DMSO) 1570.11 現(xiàn)貨
10mg 1188.16 現(xiàn)貨
25mg 2196.01 現(xiàn)貨
200mg 6298.74 現(xiàn)貨
1g 12039.3 現(xiàn)貨
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LY294002相關(guān)產(chǎn)品

相關(guān)信號(hào)通路圖

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系 實(shí)驗(yàn)類型 給藥濃度 孵育時(shí)間 活性描述 文獻(xiàn)信息
human HCT116 cells Function assay 10 μM 10 min Inhibition of PI3Kalpha in human HCT116 cells using [32P]ATP at 10 uM after 10 mins 22212721
human HCT116 cells Function assay 10 μM 10 min Inhibition of PI3Kalpha H1047R mutant in human HCT116 cells using [32P]ATP at 10 uM after 10 mins 22212721
HUVEC Function assay 10-25 μM 16 h Inhibition of TNFalpha-stimulated ICAM-1 mRNA expression in HUVEC at 10 to 25 uM pretreated for 16 hrs before TNFalpha challenge measured after 6 hrs by RT-PCR analysis 22026410
HUVEC Function assay 10-25 μM 30 min Inhibition of TNFalpha-stimulated human ICAM-1 promoter activity expressed in HUVEC assessed as beta-galactosidase activity at 10 to 25 uM pretreated for 30 mins before TNFalpha challenge measured after 5 hrs by luciferase reporter gene assay 22026410
human A2780 cells Apoptosis assay 2 μM 12 h Induction of apoptosis in cisplatin-resistant human A2780 cells assessed as decrease in phosphorylated Akt level at 2 uM after 12 hrs by immunoblot analysis. 17684018
human SW480 cells Function assay 20 μM 24 h Decrease in survivin expression in human SW480 cells at 20 uM after 24 hrs by immunoblot analysis 17472962
human BJ cells Function assay 25 μM 2 h Inhibition of PI3K signaling in PDGF-stimulated serum starved human BJ cells transfected with plasmid EGFP/PH domain of Akt assessed as suppression of PH-EGFP redistribution to plasma membrane at 25 uM treated 2 hrs before PDGF challenge by confocal microscopy 16767085
human BJ cells Function assay 25 μM 2 h Activation of Akt phosphorylation at Thr308 in PDGF-stimulated serum starved human BJ cells at 25 uM treated 2 hrs before PDGF challenge by immunoblotting 16767085
human PC3 cells Proliferation assay 25 μM 120 h Antiproliferative activity against human PC3 cells at 25 uM after 120 hrs by MTT assay relative to DMSO 16680159
human H1299 cells Function assay 0.1-30 μM 24 h Induction of JNK-mediated CHOP expression in human H1299 cells at 0.1 to 30 uM after 24 hrs by Western blot analysis 22622069
human H1299 cells Function assay 0.1-30 μM 24 h Induction of DR5 expression in human H1299 cells at 0.1 to 30 uM after 24 hrs by Western blot analysis 22622069
human H1299 cells Function assay 0.1-30 μM 24 h Down regulation of cIAP2 expression in human H1299 cells at 0.1 to 30 uM after 24 hrs by Western blot analysis in presence of 100 ug/ml TRAIL and PI3K inhibitor LY294002 22622069
human H1299 cells Function assay 0.1-30 μM 24 h Down regulation of cIAP2 expression in human H1299 cells at 0.1 to 30 uM after 24 hrs by Western blot analysis 22622069
human LNCAP cells Function assay 0.1-30 μM 24 h Downregulation of survivin expression in human LNCAP cells at 0.1 to 30 uM after 24 hrs by Western blot analysis 22832316
human LNCAP cells Function assay 0.1-30 μM 30 min Inhibition of Akt phosphorylation in human LNCAP cells at 0.1 to 30 uM after 30 mins by Western blot analysis 22832316
human PC3 cells Function assay 50 μM 8 h Induction of p21 protein expression in human PC3 cells at 50 uM incubated for 8 hrs by Western blotting relative to untreated control 22998472
human MGC803 cells Function assay 25 μM 48 h Cell cycle arrest in human MGC803 cells assessed as accumulation at G2/M phase at 25 uM after 48 hrs using propidium iodide staining after 48 hrs by flow cytometer relative to control 24119869
mouse RAW264.7 cells Function assay 25 μM 20 h Inhibition of PI3K/AKT in mouse RAW264.7 cells assessed as inhibition of LPS-induced iNOS protein expression at 25 μM after 20 hrs by Western blot analysis 24299616
MCF7 cells Function assay 10 uM 1 hr Inhibition of IGF1R phosphorylation at Tyr1161 residue in human MCF7 cells at 10 uM after 1 hr by Hoechst 33258 staining based immunohistochemical analysis 28557430
SKOV3 cells Function assay 20 uM 24 hrs Inhibition of BDNF-induced invasion in human SKOV3 cells at 20 uM after 24 hrs in by matrigel invasion assay 29122484
SKOV3 cells Antimigratory assay 20 uM 24 hrs Antimigratory activity against human SKOV3 cells assessed as inhibition of BDNF-induced cell migration at 20 uM after 24 hrs by scratch wound healing assay 29122484
J774 cells Function assay 10 uM 4 hrs Inhibition of PI3K/Akt in mouse J774 cells assessed as reduction in LPS-induced Akt phosphorylation at Ser473 at 10 uM after 4 hrs by Western blot analysis 29726680
human HCT116 cells Function assay 10 μM Inhibition of PI3Kalpha in human HCT116 cells assessed as inhibition of Akt Ser473 phosphorylation at 10 uM by immunoblot analysis 22212721
human HCT116 cells Function assay 10 μM Inhibition of PI3Kalpha H1047R mutant in human HCT116 cells assessed as inhibition of Akt Ser473 phosphorylation at 10 uM by immunoblot analysis 22212721
human HCT116 cells Function assay 10 μM Inhibition of Akt expression in human HCT116 cells at 10 uM by immunoblot analysis 22212721
human H460 cells Function assay 30 μM Inhibition of PI3K in human H460 cells assessed as Akt phosphorylation at Ser 473 up to 30 uM 18501601
mouse mast cells Function assay 20 μM Inhibition of SCF-induced PKB/Akt phosphorylation in mouse mast cells at 20 μM 16789742
human HCT116 cells Growth inhibition assay 48 h Growth inhibition of human HCT116 cells overexpressing PI3Kalpha after 48 hrs by MTT assay, IC50=6.7 μM. 22212721
human KB cells Cytotoxic?assay 72 h Cytotoxicity against human KB cells after 72 hrs by MTT assay, IC50=44.76 μM. 21945250
human HCT116 cells Cytotoxic?assay 72 h Cytotoxicity against human HCT116 cells after 72 hrs by MTT assay, IC50=56.01 μM. 21945250
human IGROV1 cells Function assay 24/48 h Inhibition of PI3K/Akt in human IGROV1 cells assessed as decrease in phosphorylated AKT level at 1 to 5 times IC50 after 24 to 48 hrs by Western blot analysis 21216151
human IGROV1 cells Function assay 24/48 h Inhibition of PI3K/Akt in human IGROV1 cells assessed as decrease in cyclin D1 level at 1 to 5 times IC50 after 24 to 48 hrs by Western blot analysis 21216151
human IGROV1 cells Function assay 24 h Cell cycle arrest in human IGROV1 cells assessed as accumulation at G1 phase at 5 fold IC50 after 24 hrs by flow cytometry 21216151
human IGROV1 cells Function assay 24 h Cell cycle arrest in human IGROV1 cells assessed as accumulation at G1 phase at 1 fold IC50 after 24 hrs by flow cytometry 21216151
human H4 cells Function assay 2 h Decrease in FYVE-RFP+ vesicle intensity per cell in human H4 cells after 2 hrs relative to control 18024584
human A375 cells Proliferation assay 46 h Antiproliferative activity against human A375 cells after 46 hrs, IC50=8.4 μM. 17049248
human HCT116 cells Growth inhibition assay 48 h Growth inhibition of human HCT116 cells after 48 hrs by MTT assay, IC50=5.8 μM. 22212721
human HCT116 cells Growth inhibition assay 48 h Growth inhibition of human HCT116 cells overexpressing PI3Kalpha H1047R mutant after 48 hrs by MTT assay, IC50=5.3 μM 22212721
human A549 cells Cytotoxic?assay 72 h Cytotoxicity against human A549 cells after 72 hrs by MTT assay 22480851
human PC3 cells Cytotoxic?assay 72 h Cytotoxicity against human PC3 cells after 72 hrs by MTT assay, IC50=61.35 μM. 22480851
human HL60 cells Cytotoxic?assay 72 h Cytotoxicity against human HL60 cells after 72 hrs by MTT assay, IC50=9.94 μM. 22480851
HEK293 cells Function assay 1.5 h Displacement of [3H]LSD from human 5HT6 receptor expressed in HEK293 cells after 1.5 hrs by liquid scintillation counting 22537153
MDA-MB-231 cells Cell invasion assay 24 h Inhibition of epithelial growth factor-induced cell migration of human MDA-MB-231 cells pre-incubated for 24 hrs by cell invasion assay, IC50=0.38 μM. 22804108
human BT474 cell Proliferation assay 72 h Inhibition of human BT474 cell proliferation after 72 hrs by spectrophotometric analysis, IC50=20.7 μM. 23410005
human PC3 cell Proliferation assay 72 h Inhibition of human PC3 cell proliferation after 72 hrs by spectrophotometric analysis, IC50=12.1 μM. 23410005
human PC3 cells Function assay 30 min Inhibition of PI3K in human PC3 cells assessed as decrease in AKT phosphorylation at serine 473 after 30 mins by ELISA, IC50=1.3μM. 23410005
human A549 cells Proliferation assay 72 h Antiproliferative activity against human A549 cells assessed as inhibition of absorbance after 72 hrs by MTT assay, IC50=82.32 μM. 25693787
human HuH7 cells Proliferation assay 72 h Antiproliferative activity against human HuH7 cells assessed as inhibition of absorbance after 72 hrs by MTT assay, IC50=67.18 μM. 25693787
human HCT116 cells Proliferation assay 72 h Antiproliferative activity against human HCT116 cells assessed as inhibition of absorbance after 72 hrs by MTT assay, IC50=51.82 μM. 25693787
human HL60 cells Proliferation assay 72 h Antiproliferative activity against human HL60 cells assessed as inhibition of absorbance after 72 hrs by MTT assay, IC50=18.43 μM. 25693787
HL60 cells Antiproliferative assay 3 days Antiproliferative activity against human HL60 cells measured after 3 days by MTS assay, IC50 = 14 μM. 26945110
U937 cells Antiproliferative assay 3 days Antiproliferative activity against human U937 cells measured after 3 days by MTS assay, IC50 = 14 μM. 26945110
Jurkat cells Antiproliferative assay 3 days Antiproliferative activity against human Jurkat cells measured after 3 days by MTS assay, IC50 = 22 μM. 26945110
K562 cells Antiproliferative assay 3 days Antiproliferative activity against human K562 cells measured after 3 days by MTS assay, IC50 = 38 μM. 26945110
U266 cells Antiproliferative assay 3 days Antiproliferative activity against human U266 cells measured after 3 days by MTS assay, IC50 = 46 μM. 26945110
MDA-MB-231 cells Antimigratory assay 24 hrs Antimigratory activity against EGF induced chemotaxis in human MDA-MB-231 cells preincubated for 24 hrs followed by EGF addition for 3.5 hrs by light microscopy, IC50 = 0.38 μM. 27598237
MDA-MB-231 cells Antiinvasive assay 3.5 hrs Antiinvasive activity in human MDA-MB-231 cells assessed as inhibition of EGF-induced cell invasion after 3.5 hrs, IC50 = 0.38 μM. 28009521
HEK293T cells Function assay 1 hr Inhibition of immobilized N-LY294002 bead binding to PI3Kbeta (unknown origin) expressed in HEK293T cells incubated for 1 hr by LC-MS/MS analysis, IC50 = 0.42 μM. 28280261
HEK293T cells Function assay 1 hr Inhibition of immobilized N-LY294002 bead binding to PI3Kdelta (unknown origin) expressed in HEK293T cells incubated for 1 hr by LC-MS/MS analysis, IC50 = 1.53 μM. 28280261
HEK293T cells Function assay 1 hr Inhibition of immobilized N-LY294002 bead binding to PI3Kalpha (unknown origin) expressed in HEK293T cells incubated for 1 hr by LC-MS/MS analysis, IC50 = 2.37 μM. 28280261
J774 cells Antiinflammatory assay 24 hrs Antiinflammatory activity in mouse J774 cells assessed as reduction in LPS-induced MCP1 expression after 24 hrs by ELISA, IC50 = 3.7 μM. 29726680
J774 cells Antiinflammatory assay 24 hrs Antiinflammatory activity in mouse J774 cells assessed as reduction in LPS-induced IL6 expression after 24 hrs by ELISA, IC50 = 5.1 μM. 29726680
J774 cells Antiinflammatory assay 24 hrs Antiinflammatory activity in mouse J774 cells assessed as reduction in LPS-induced nitric oxide production after 24 hrs by Griess assay, IC50 = 8.9 μM. 29726680
Sf9 cells Fluorescent polarization assay Inhibition of human PI3Kalpha expressed in Sf9 cells by fluorescent polarization assay, IC50=0.55 μM. 21121631
Sf9 cells fluorescent polarization assay Inhibition of human PI3Kgamma expressed in Sf9 cells by fluorescent polarization assay 21121631
Sf21 cells Function assay Inhibition of mouse recombinant PI3Kalpha expressed in baculovirus-infected Sf21 cells, IC50=0.5 μM. 19748269
human MCF7 cells Cytotoxic?assay Cytotoxicity against human MCF7 cells in presence of 20 μM chloroquine by SRB assay, GI50=2.63 μM. 18691894
human MCF7 cells Cytotoxic?assay Cytotoxicity against human MCF7 cells in presence of 10 uM chloroquine by SRB assay, GI50=3.08 μM. 18691894
human MCF7 cells Cytotoxic?assay Cytotoxicity against human MCF7 cells by SRB assay, GI=3.16 μM. 18691894
human MDA-MB-231 cells Cytotoxic?assay Cytotoxicity against human MDA-MB-231 cells in presence of 20 μM chloroquine by SRB assay, GI=3.32 μM. 18691894
human MDA-MB-231 cells Cytotoxic?assay Cytotoxicity against human MDA-MB-231 cells in presence of 10 uM chloroquine by SRB assay, GI50=4.35 μM. 18691894
human MDA-MB-468 cells Cytotoxic?assay Cytotoxicity against human MDA-MB-468 cells in presence of 20 uM chloroquine by SRB assay, IC50=4.76 μM. 18691894
MDA-MB-231 cells Cytotoxic?assay Cytotoxicity against human MDA-MB-231 cells by SRB assay, GI50=6.71 μM. 18691894
human MDA-MB-468 cells Cytotoxic?assay Cytotoxicity against human MDA-MB-468 cells in presence of 10 uM chloroquine by SRB assay, GI50=8.2 μM. 18691894
human MDA-MB-468 cells Cytotoxic?assay Cytotoxicity against human MDA-MB-468 cells by SRB assay, IC50=10.4 μM. 18691894
human 184B5 cells Cytotoxic?assay Cytotoxicity against human 184B5 cells by SRB assay, GI50=39.37 μM. 18691894
human U251HRE cells Function assay Inhibition of hypoxia-induced HIF1 activation in human U251HRE cells by cell based reporter gene assay 18501601
human U87MG cells Function assay Inhibition of GSK3-beta in human U87MG cells by ELISA, IC50=8.1 μM. 18345609
rat RBL2H3 cells Function assay Inhibition of A23187-induced degranulation in rat RBL2H3 cells 18328716
Sf9 cells Function assay Inhibition of CK2 expressed in Sf9 cells, IC50=6.9 μM. 18321716
human A375 cells Proliferation assay Inhibition of serum-induced proliferation of human A375 cells, IC50=8.4 μM. 17601739
HeLa cells Function assay Inhibition of AX-7503 binding to recombinant Plk3 expressed in HeLa cells by Western blot, IC5=3 μM. 17135248
THP1 cells Function assay Inhibition of SCF1-induced PKB/Akt phosphorylation in THP1 cells, IC50=1.01 μM. 16789742
THP1 cells Function assay Inhibition of MCP1-induced PKB/Akt phosphorylation in THP1 cells, IC50=1.65 μM. 16789742
mouse Raw264 macrophage Function assay Inhibition of C5a-mediated PKB/Akt phosphorylation in mouse Raw264 macrophage, IC50=10 μM. 16789742
THP1 cells Function assay Inhibition of MCP1-induced chemotaxis of THP1 cells, IC50=37 μM. 16789742
HeLa (human carcinoma) cells. Function assay In vitro inhibition of DNA-dependent protein kinase(DNA-PK) from HeLa (human carcinoma) cells, IC50=1.4 μM. 15658870
HeLa cells Binding affinity assay Binding affinity for PI3-kinase isolated from HeLa cells, Ki=6 μM 15658870
HeLa cells Function assay Inhibition of mTOR protein isolated from HeLa cells, IC50=2.5 μM. 15658870
Sf9 cells Function assay Inhibition of His-tagged bovine PI3K expressed in Sf9 cells, IC50=10 μM. 10998351
Sf21 cells Function assay Inhibition of mouse wild type PI3Kalpha expressed in Sf21 cells co-expressing N-terminal His-tagged human p85a using L-alpha-phosphatidylinositol substrate by TLC based phosphor imaging, IC50=0.5 μM 22520630
Sf9 cells Function assay Inhibition of His-tagged human CK2 expressed in Sf9 cells, IC50 = 6.9 μM. 10998351
HeLa cells Function assay In vitro inhibition of DNA-dependent protein kinase(DNA-PK) from HeLa (human carcinoma) cells., IC50 = 1.4 μM. 12941339
HeLa cells Function assay Inhibition of DNA dependent protein kinase isolated from HeLa cells, IC50 = 1.5 μM. 15658870
Sf21 cells Function assay Inhibition of human recombinant PI3Kbeta expressed in baculovirus-infected Sf21 cells, IC50 = 0.9 μM. 19748269
Sf21 cells Function assay Inhibition of bovine recombinant PI3Kgamma expressed in baculovirus-infected Sf21 cells, IC50 = 7 μM. 19748269
HeLa cells Function assay Activity at PI3K in human HeLa cells by ELISA, EC50 = 1.5 μM. 20092323
Sf21 cells Function assay Inhibition of PI3Kdelta expressed in cells co-expressing N-terminal His-tagged human p85a using L-alpha-phosphatidylinositol substrate by TLC based phosphor imaging, IC50 = 0.57 μM. 22520630
Sf21 cells Function assay Inhibition of human wild type PI3Kbeta expressed in Sf21 cells co-expressing N-terminal His-tagged human p85a using L-alpha-phosphatidylinositol substrate by TLC based phosphor imaging, IC50 = 0.97 μM. 22520630
MDA-MB-231 cells Function assay Inhibition of EGF-induced invasion of human MDA-MB-231 cells by MTT assay, IC50 = 0.38 μM. 28302401
NB1643 cells qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB1643 cells 29435139
OHS-50 cells qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells 29435139
SJ-GBM2 cells qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells 29435139
SK-N-MC cells qHTS assay qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells 29435139
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生物活性

產(chǎn)品描述 LY294002 (SF 1101, NSC 697286) 是首個(gè)合成的已知抑制PI3Kα/δ/β的小分子,在無細(xì)胞測(cè)定中IC50分別為 0.5 μM/0.57 μM/0.97 μM;在溶液中比在Wortmannin中穩(wěn)定,也能夠阻斷自噬體的形成。它不僅能夠結(jié)合class I PI3Ks和其他PI3K相關(guān)的激酶,還能夠結(jié)合一些與PI3K家族無關(guān)的新型靶點(diǎn)。LY294002 可以抑制CK2,對(duì)應(yīng)的IC50值為98 nM。LY294002 是一種非特異的 DNA-PKcs 抑制劑,并可激活自噬和凋亡。
特性 LY294002是選擇性的, 可滲透細(xì)胞的特定PI3K抑制劑,可作用于酶的ATP結(jié)合位點(diǎn),且抑制自體吞噬的螯合作用。
靶點(diǎn)
CK2 [5]
(Cell-free assay)
p110α [1]
(Cell-free assay)
p110δ [1]
(Cell-free assay)
p110β [1]
(Cell-free assay)
DNA-PK [6]
(Cell-free)
98 nM 0.5 μM 0.57 μM 0.97 μM 1.4 μM
體外研究(In Vitro)
體外研究活性

LY294002是一種非特異性抑制劑,除了class I PI3Ks,它同樣還能抑制其他類型PI3Ks、mTOR、DNA-PK以及其他蛋白激酶,如CK2和Pim-1[5]。LY294002使Akt/PKB失活,因此抑制細(xì)胞增殖和誘導(dǎo)細(xì)胞凋亡。 LY294002作用于結(jié)腸癌細(xì)胞系,使磷酸化Akt (Ser473)的表達(dá)下降, 明顯抑制生長(zhǎng)和誘導(dǎo)凋亡。[2] LY294002作用于腫瘤細(xì)胞,誘導(dǎo)明顯的核固縮和減少細(xì)胞質(zhì)體積。因此,在體外,LY294002明顯抑制卵巢癌細(xì)胞增殖。LY294002誘導(dǎo)細(xì)胞停在G1期,導(dǎo)致幾乎全部的黑色素瘤細(xì)胞增殖被抑制,部分MG-63 (骨肉瘤細(xì)胞系)增殖被抑制。LY294002作用于細(xì)胞周期的效果可用于研究PI3K激活通路和癌細(xì)胞周期之間關(guān)系。[3]

激酶實(shí)驗(yàn) 激酶實(shí)驗(yàn)
使用重組酶和1 μM ATP,通過輻射實(shí)驗(yàn)測(cè)定LY294002對(duì)PI3K的抑制效果。室溫下(24oC)進(jìn)行激酶反應(yīng)1小時(shí),然后加入PBS終止反應(yīng)。通過劑量反應(yīng)曲線測(cè)定IC50值。通過激酶選擇性篩選來抑制CK2和GSK3β。加入10 μM ATP,測(cè)定LY294002作用于一組激酶的效果。
細(xì)胞實(shí)驗(yàn) 細(xì)胞系 結(jié)腸癌細(xì)胞系: DLD-1, LoVo, HCT15, 和Colo205
濃度 0-50 μM
孵育時(shí)間 0-48小時(shí)
方法

1×105個(gè)細(xì)胞(每孔100 μL)接種在96孔板上。設(shè)三個(gè)復(fù)孔,加入LY294002,在37oC下培養(yǎng)0-48小時(shí)。處理后, 10 μL Premix WST-1 加到每孔中,然后在37oC下溫育60分鐘,然后用微型計(jì)數(shù)板在450nm處測(cè)定吸光值。

實(shí)驗(yàn)圖片 檢測(cè)方法 檢測(cè)指標(biāo) 實(shí)驗(yàn)圖片 PMID
Western blot E-cadherin / p-Akt / Akt beta-catenin / p-GSK3β / Cyclin D1 Bcl-xl / Bax / caspase3 / cleaved caspase-3 p-p70S6K (T389) / p-GSK3β(S9) / pERK / Vinculin pPKB-S473 29731993
Growth inhibition assay Cell viability 25344912
Immunofluorescence α-SMA / CD31 E-cadherin / beta-catenin COX-2 / p-NFκB FOXO3a 27671604
ELISA IL-10 / IL-1β / TNFα / IL-6 22208359
體內(nèi)研究(In Vivo)
體內(nèi)研究活性

體內(nèi),LY294002也抑制腫瘤生長(zhǎng)和誘導(dǎo)凋亡,尤其作用于LoVo腫瘤, 因此作用于鼠癌性腹膜炎模型具有明顯藥效。[2] LY294002明顯抑制卵巢癌生長(zhǎng)和腹水形成。[3]

動(dòng)物實(shí)驗(yàn) Animal Models 腹腔注射OVCAR-3細(xì)胞的無胸腺裸鼠(5-7周大)
Dosages 0-100 mg/kg
Administration 每天腹腔注射,持續(xù)3周
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02337309 Terminated
Neuroblastoma
New Approaches to Neuroblastoma Therapy Consortium|SignalRX Pharmaceuticals Inc.|University of Southern California
July 9 2015 Phase 1

化學(xué)信息&溶解度

分子量 307.34 分子式

C19H17NO3

CAS號(hào) 154447-36-6 SDF Download LY294002 SDF
Smiles C1COCCN1C2=CC(=O)C3=C(O2)C(=CC=C3)C4=CC=CC=C4
儲(chǔ)存條件(自收到貨起)

體外溶解度
批次:

DMSO : 61 mg/mL ( (198.47 mM) ;DMSO吸濕會(huì)降低化合物溶解度,請(qǐng)使用新開封DMSO)

Ethanol : 15 mg/mL (48.8 mM)

Water : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次:

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

動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量 濃度 體積 分子量

動(dòng)物體內(nèi)配方計(jì)算器(澄清溶液)

第一步:請(qǐng)輸入基本實(shí)驗(yàn)信息(考慮到實(shí)驗(yàn)過程中的損耗,建議多配一只動(dòng)物的藥量)

mg/kg g μL

第二步:請(qǐng)輸入動(dòng)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(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方)

% DMSO % % Tween 80 % ddH2O
%DMSO %

計(jì)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,:如該濃度超過該批次藥物DMSO溶解度,請(qǐng)先聯(lián)系Selleck);

體內(nèi)配方配制方法: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: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(jìn)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 want to buy a inhibitor that can inactivates Akt/PI3K. I notice the protocol of LY294002 (catalog no. s1105) says it will inactivates Akt/PKB. Is LY294002 available for Akt/PI3K inhibition?

回答:
LY294002 is the first synthetic molecule known to inhibit PI3Kα/δ/β with IC50 of 0.5 μM/0.57 μM/0.97 μM, respectively. It can inhibit PI3K/AKT. PKB is the alternative name of AKT.

問題 2:
What is the suggested formulation of this compound for mouse injection(i.p.)?

回答:
It can be dissolved in 4% DMSO/30% PEG 300/5% Tween 80/ddH2O at 5 mg/ml clearly, and the concentration of DMSO is safe for in vivo experiments.

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