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Tofacitinib (CP-690550) Citrate

別名: Tasocitinib Citrate,CP-690550 中文名稱：枸櫞酸托法替尼

Tofacitinib citrate (CP-690550, Tasocitinib)是一種新型JAK抑制劑，對JAK3，JAK2，JAK1的IC50分別為1 nM, 20 nM 和112 nM。Tofacitinib citrate 還具有抗感染的活性。

Tofacitinib (CP-690550) Citrate Chemical Structure

Tofacitinib (CP-690550) Citrate Chemical Structure

CAS: 540737-29-9

規(guī)格 價格 庫存 購買數(shù)量
10mM (1mL in DMSO) 1561.36 現(xiàn)貨
10mg 1194.19 現(xiàn)貨
50mg 3843.17 現(xiàn)貨
200mg 5487.3 現(xiàn)貨
1g 7944.3 現(xiàn)貨
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常與Tofacitinib (CP-690550) Citrate一起在實驗中被使用的化合物

Methotrexate

Tofacitinib和Methotrexate聯(lián)合療法在治療類風(fēng)濕性關(guān)節(jié)炎方面不劣于Adalimumab和Methotrexate聯(lián)合療法。

Fleischmann R, et al. Lancet. 2017 Jul 29;390(10093):457-468.

Cyclosporine

CP-690550與Cyclosporine聯(lián)合使用，在小鼠新生血管同種異體心臟移植模型中的療效得到顯著提高。

Kudlacz E, et al. Am J Transplant. 2004 Jan;4(1):51-7.

Mycophenolate mofetil

CP-690550和Mycophenolate mofetil聯(lián)合使用可顯著提高同種異體移植物的存活率。

Borie DC, et al. Transplantation. 2005 Dec 27;80(12):1756-64.

Ruxolitinib

Tofacitinib和Ruxolitinib在治療多種自身免疫性疾病方面表現(xiàn)出潛在功效。

Sadeghi S, et al. Dermatol Pract Concept. 2022 Oct 1;12(4):e2022178.

Baricitinib

在CD4+T細(xì)胞、NK細(xì)胞和單核細(xì)胞中，Tofacitinib對IL-2、IL-4、IL-15和IL-21信號傳導(dǎo)的STAT抑制率高于Baricitinib。

Mclnnes IB, et al. Arthritis Res Ther. 2019 Aug 2;21(1):183.

Tofacitinib (CP-690550) Citrate相關(guān)產(chǎn)品

相關(guān)信號通路圖

JAK Signaling Pathways

JAK信號通路圖

細(xì)胞實驗數(shù)據(jù)示例

細(xì)胞系 實驗類型 給藥濃度 孵育時間 活性描述 文獻(xiàn)信息
NK Immunosuppressive assay 1 to 5 mg/kg 4 weeks Immunosuppressive activity in naive cynomolgus monkey assessed as effect on CD3-CD16+ NK cells at 1 to 5 mg/kg, po for 4 weeks 14593182
T-cells Function assay 5 to 500 nM 1 hr Inhibition of IL2-induced Stat5 phosphorylation in human CD4+ T cells at 5 to 500 nM after 1 hr by Western blot 19053756
SUM149PT Function assay 3 uM 16 hrs Induction of PTPN6 in human SUM149PT cells assessed as inhibition of STAT3 phosphorylation at 3 uM after 16 hrs by Western blotting analysis in presence of pervanadate 24978112
Hs578T Function assay 3 uM 16 hrs Induction of PTPN6 in human Hs578T cells assessed as inhibition of STAT3 phosphorylation at 3 uM after 16 hrs by Western blotting analysis in presence of pervanadate 24978112
T-cells Function assay 50 to 300 nM 1 hr Inhibition of JAK1/JAK3 in human CD4 positive T cells assessed as inhibition of IL4-stimulated STAT6 phosphorylation at 50 to 300 nM preincubated for 1 hr followed by IL-4 stimulation measured after 30 mins by immunoblot analysis 29852068
T-cells Function assay 50 to 300 nM 1 hr Inhibition of JAK1/JAK3 in human CD4 positive T cells assessed as inhibition of IL2-stimulated STAT5 phosphorylation at Tyr-695 residue at 50 to 300 nM preincubated for 1 hr followed by IL-2 stimulation measured after 30 mins by immunoblot analysis 29852068
T-cells Function assay >300 nM 1 hr Inhibition of JAK1/JAK2/TYK2 in human CD4 positive T cells assessed as inhibition of IL6-stimulated STAT3 phosphorylation at >300 nM preincubated for 1 hr followed by IL-6 stimulation measured after 30 mins by immunoblot analysis 29852068
TALL-1 Function assay 1 uM 3 hrs Inhibition of JAK3 in human TALL-1 cells assessed as inhibition of IL-2 induced STAT5 phosphorylation at 1 uM preincubated for 3 hrs followed by IL-2 induction measured after 30 mins by immunoblotting 26258521
BA/F3 Function assay 300 nM 3 hrs Inhibition of JAK3 (unknown origin) expressed in mouse BA/F3 cells assessed as reduction of STAT5 phosphorylation at 300 nM after 3 hrs by immunoblotting analysis 26258521
OCL-AML5 Function assay 1 uM 3 hrs Inhibition of JAK2 in human OCL-AML5 cells assessed as inhibition of GM-CSF induced STAT5 phosphorylation at 1 uM preincubated for 3 hrs followed by GM-CSF induction measured after 30 mins by immunoblotting 26258521
BA/F3 Function assay 1 uM 3 hrs Inhibition of JAK3 (unknown origin) expressed in mouse BA/F3 cells at 1 uM preincubated for 3 hrs followed by pulldown with streptavidin beads by immunoblotting analysis 26258521
Huh7 Function assay 10 uM 30 mins Inhibition of Tyk2 in human Huh7 cells assessed as reduction of IFNalpha5-induced STAT3 phosphorylation at 10 uM pre-incubated for 30 mins before IFNalpha5 stimulation for 30 mins mins by immunoblotting 26231159
Huh7 Function assay 10 uM 30 mins Inhibition of Tyk2 in human Huh7 cells assessed as reduction of basal level STAT3 phosphorylation at 10 uM after 30 mins by immunoblotting 26231159
Huh7 Function assay 1 uM 30 mins Inhibition of Tyk2 in human Huh7 cells assessed as reduction of IFNalpha5-induced STAT3 phosphorylation at 1 uM pre-incubated for 30 mins before IFNalpha5 stimulation for 30 mins mins by immunoblotting 26231159
YT Function assay 30 ng/ml Inhibition of IL2-induced JAK3 phosphorylation in human YT cells at 30 ng/ml by immunoblotting analysis 14593182
YT Function assay 30 ng/ml Inhibition of IL2-induced STAT5A phosphorylation in human YT cells at 30 ng/ml by immunoblotting analysis 14593182
YT Function assay 30 ng/ml Inhibition of IL2-induced STAT5B phosphorylation in human YT cells at 30 ng/ml by immunoblotting analysis 14593182
TF1 Function assay 20 mins Inhibition of JAK1 in human TF1 cells assessed as inhibition of IL6-induced STAT3 phosphorylation incubated for 20 mins followed by IL6 challenge for 30 mins in presence of whole blood, EC50 = 0.043 μM. 23659214
Ba/F3 Function assay 60 mins Inhibition of TEL-fused JAK1 expressed in Ba/F3 cells assessed as inhibition of STAT5 phosphorylation after 60 mins by AlphaScreen assay, IC50 = 0.026 μM. 22087750
T-cells Function assay 72 hrs Inhibition of IL2-induced proliferation of human T cells assessed as [3H]thymidine incorporation after 72 hrs by scintillation counting, IC50 = 0.011 μM. 14593182
SF21 Function assay 10 mins Inhibition of JAK2 (unknown origin) expressed in SF21 cells using Biotin-KAIETDKEYYTVKD as substrate and [33Pgamma]ATP incubated for 10 mins prior to substrate addition measured after 30 mins by Topcount analysis, IC50 = 0.004 μM. 23541670
Sf9 Function assay 90 mins Inhibition of human recombinant N-terminal GST-tagged JAK2 expressed in Sf9 cells using Biotin-LC-EQEDEPEGDYFEWLE as substrate after 90 mins by TR-FRET assay, IC50 = 0.004 μM. 22087750
Sf9 Function assay 90 mins Inhibition of human recombinant N-terminal GST-tagged JAK1 expressed in Sf9 cells using Biotin-LC-EQEDEPEGDYFEWLE as substrate after 90 mins by TR-FRET assay, IC50 = 0.003 μM. 22087750
Sf9 Function assay 30 mins Inhibition of human GST-fused JAK2 catalytic domain expressed in baculovirus-infected Sf9 cells using polyglutamic acid-tyrosine as substrate after 30 mins by ELISA, Ki = 0.0007 μM. 23668484
Sf9 Function assay 30 mins Inhibition of human GST-fused JAK1 catalytic domain expressed in baculovirus-infected Sf9 cells using polyglutamic acid-tyrosine as substrate after 30 mins by ELISA, Ki = 0.0007 μM. 23668484
Sf9 Function assay 90 mins Inhibition of human recombinant N-terminal GST-tagged JAK3 expressed in Sf9 cells using Biotin-LC-EQEDEPEGDYFEWLE as substrate after 90 mins by TR-FRET assay, IC50 = 0.0006 μM. 22087750
Sf9 Function assay 30 mins Inhibition of human GST-fused JAK3 catalytic domain expressed in baculovirus-infected Sf9 cells using polyglutamic acid-tyrosine as substrate after 30 mins by ELISA, Ki = 0.0004 μM. 23668484
Sf9 Function assay 90 mins Inhibition of human recombinant N-terminal GST-tagged TYK2 expressed in Sf9 cells using Biotin-LC-EQEDEPEGDYFEWLE as substrate after 90 mins by TR-FRET assay, IC50 = 0.052 μM. 22087750
TF1 Function assay 20 mins Inhibition of JAK1 in human TF1 cells assessed as inhibition of IL6-induced STAT3 phosphorylation incubated for 20 mins prior to IL6-induction measured after 30 to 45 mins, EC50 = 0.053 μM. 22698084
TF1 Function assay 20 mins Inhibition of JAK1 in human TF1 cells assessed as inhibition of IL6-induced STAT3 phosphorylation incubated for 20 mins followed by IL6 challenge for 30 mins, EC50 = 0.053 μM. 23659214
Ba/F3 Function assay 60 mins Inhibition of TEL-fused JAK3 expressed in Ba/F3 cells assessed as inhibition of STAT5 phosphorylation after 60 mins by AlphaScreen assay, IC50 = 0.054 μM. 22087750
TF1 Function assay 20 mins Inhibition of JAK2 in human TF1 cells assessed as inhibition of EPO-induced STAT5 phosphorylation incubated for 20 mins prior to EPO-induction measured after 30 to 45 mins, EC50 = 0.093 μM. 22698084
TF1 Function assay 20 mins Inhibition of JAK2 in human TF1 cells assessed as inhibition of EPO-induced STAT5 phosphorylation incubated for 20 mins followed by IL6 challenge for 30 mins, EC50 = 0.093 μM. 23659214
TF1 Function assay 2 hrs Inhibition of JAK2 in GMCSF-stimulated human TF1 cells assessed as suppression of STAT5 phosphorylation preincubated for 2 hrs followed by GMCSF stimulation for 50 mins by FACS reader analysis, IC50 = 0.095 μM. 27130359
CTLL-2 Antiproliferative assay 72 hrs Antiproliferative activity against IL-2-stimulated mouse CTLL-2 cells expressing JAK1/JAK3 after 72 hrs by alamar blue assay, IC50 = 0.132 μM. 19762238
DND/L12 Function assay 30 mins Inhibition of JAK3 in human DND/L12 cells after 30 mins by luciferase assay in presence of human serum albumin, IC90 = 0.16 μM. 14593182
Ba/F3 Function assay 60 mins Inhibition of TEL-fused JAK2 expressed in Ba/F3 cells assessed as inhibition of STAT5 phosphorylation after 60 mins by AlphaScreen assay, IC50 = 0.265 μM. 22087750
CD34+ Function assay 45 mins Inhibition of JAK2 homodimer in human CD34+ cells spiked into human whole blood assessed as inhibition of EPO-induced STAT-5 phosphorylation preincubated for 45 mins followed by EPO addition measured after 15 mins by FACS analysis, IC50 = 0.302 μM. 24417533
BA/F3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BA/F3 cells expressing TEL-JAK3 after 72 hrs by cell titer glo assay 26258521
TF1 Function assay Inhibition of JAK1 in human TF1 cells assessed as suppression of IL6-stimulated STAT3 phosphorylation by AlphaScreen assay, INH = 0.045 μM. 26372653
PBMC Function assay Inhibition IL-7-indcued STAT5 phosphorylation in human PBMC cells by flow cytometry, IC50 = 0.039 μM. 26927423
T-cells Function assay Inhibition of JAK3/1 in human T cells expressing CD3 assessed as inhibition of IL2-stimulated STAT5a phosphorylation, IC50 = 0.028 μM. 23540648
MO7 Function assay Inhibition of Jak3-mediated IL15-induced Stat5 phosphorylation in human MO7 cells by cell-based assay, IC50 = 0.024 μM. 21155605
insect Function assay Inhibition of GST-tagged Jak2 expressed in insect cells using 20 uM ATP, IC50 = 0.012 μM. 21155605
insect cells Function assay Inhibition of GST-tagged Jak3 expressed in insect cells using 18 uM ATP, IC50 = 0.008 μM. 21155605
insect cells Function assay Inhibition of GST-tagged Jak1 expressed in insect cells using 70 uM ATP, IC50 = 0.0061 μM. 21155605
Sf9 Function assay Inhibition of GST-tagged human JAK3 catalytic domain expressed in Sf9 cells by ELISA, IC50 = 0.0033 μM. 21105711
Sf9 Function assay Inhibition of GST-tagged human JAK3 catalytic domain expressed in Sf9 cells by ELISA, IC50 = 0.001 μM. 21105711
Sf9 Function assay Inhibition of human recombinant GST-tagged JH1 domain (785 to1125) of JAK3 expressed in insect Sf9 cells by ELISA, IC50 = 0.001 μM. 14593182
CTLL Function assay Inhibition of Jak3-mediated IL2-induced Stat5 phosphorylation in mouse CTLL cells by cell-based assay, IC50 = 0.048 μM. 21155605
TF1 Function assay Inhibition of JAK1 in human TF1 cells assessed as inhibition of IL2-induced STAT3 phosphorylation, EC50 = 0.053 μM. 22591402
T-cells Function assay Inhibition of allogenic cells-stimulated proliferation in monkey T cells by mixed lymphocyte reaction method, IC50 = 0.057 μM. 14593182
CD34+ Function assay Inhibition of JAK2 in human CD34+ cells assessed as inhibition of EPO-mediated cell proliferation, IC50 = 0.071 μM. 26927423
TF1 Function assay Inhibition of IL4-induced proliferation of TF1 cells, IC50 = 0.08 μM. 16934457
T-cells Function assay Inhibition of allogenic cells-stimulated proliferation in human T cells by mixed lymphocyte reaction method, IC50 = 0.087 μM. 14593182
PBMC Function assay Inhibition of JAK1 in human PBMC cells assessed as inhibition of IL-6-induced MCP1 secretion, IC50 = 0.095 μM. 26927423
TF1 Function assay Inhibition of JAK2 in EPO-stimulated human TF1 cells expressing stably integrated beta-lactamase reporter gene under control of STAT5 response elements in interferon regulatory factor 1 gene promoter by fluorescence assay, IC50 = 0.107 μM. 29156136
Sf9 Function assay Inhibition of GST-tagged human JAK1 catalytic domain expressed in Sf9 cells by ELISA, IC50 = 0.11 μM. 21105711
T-cells Function assay Inhibition of allogenic cells-stimulated proliferation in mouse T cells by mixed lymphocyte reaction method, IC50 = 0.115 μM. 14593182
ME180 Function assay Inhibition of JAK1 in IL6-stimulated human ME180 cells expressing stably integrated beta-lactamase reporter gene under control of sis-inducible element by fluorescence assay, IC50 = 0.124 μM. 29156136
HT2 Function assay Inhibition of JAK3 in mouse HT2 cells assessed as suppression of cell growth, IC50 = 0.156 μM. 27771180
T-cells Function assay Inhibition of JAK2/1 in human T cells expressing CD3 assessed as inhibition of IFNgamma-stimulated STAT1 phosphorylation, IC50 = 0.17 μM. 23540648
insect cells Function assay Inhibition of GST-tagged Tyk2 expressed in insect cells using 35 uM ATP, IC50 = 0.176 μM. 21155605
TF1 Function assay Inhibition of JAK2 in human TF1 cells assessed as suppression of cell growth, IC50 = 0.2751 μM. 27771180
A2780 Function assay Inhibition of cdk-mediated NPM phosphorylation at thr199 in human A2780 cells 14593182
A2780 Function assay Inhibition of cdk-mediated NPM phosphorylation at thr199 in human A2780 cells 21105711
A2780 Function assay Inhibition of cdk-mediated NPM phosphorylation at thr199 in human A2780 cells 19762238
A2780 Function assay Inhibition of cdk-mediated NPM phosphorylation at thr199 in human A2780 cells 30460842
A2780 Function assay Inhibition of cdk-mediated NPM phosphorylation at thr199 in human A2780 cells 23659214
A2780 Function assay Inhibition of cdk-mediated NPM phosphorylation at thr199 in human A2780 cells 16934457
A2780 Function assay Inhibition of cdk-mediated NPM phosphorylation at thr199 in human A2780 cells 26372653
A2780 Function assay Inhibition of cdk-mediated NPM phosphorylation at thr199 in human A2780 cells 22087750
A2780 Function assay Inhibition of cdk-mediated NPM phosphorylation at thr199 in human A2780 cells 30139575
A2780 Function assay Inhibition of cdk-mediated NPM phosphorylation at thr199 in human A2780 cells 27771180
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生物活性

產(chǎn)品描述 Tofacitinib citrate (CP-690550, Tasocitinib)是一種新型JAK抑制劑，對JAK3，JAK2，JAK1的IC50分別為1 nM, 20 nM 和112 nM。Tofacitinib citrate 還具有抗感染的活性。
靶點
JAK3 [1]
(Cell-free assay)		 JAK2 [4]
(Cell-free assay)
1 nM 20 nM
體外研究(In Vitro)
體外研究活性 CP-690550抑制IL-2調(diào)節(jié)的人T細(xì)胞爆發(fā)式增殖，和IL-15誘導(dǎo)的CD69表達(dá)，IC50分別為11和48 nM。CP-690550抑制混合淋巴細(xì)胞反應(yīng)，IC50為87 nM。CPCP-690550 處理含人野生型或V617F JAK2的鼠因子依賴的細(xì)胞Patersen–促紅細(xì)胞生成素受體(FDCP-EpoR) 細(xì)胞，抑制細(xì)胞增殖，IC50分別為2.1 μM 和0.25 μM。CP-690550 抑制白細(xì)胞介素-6誘導(dǎo)的STAT1 和STAT3磷酸化，IC50分別為23和77 nM。而且, CP-690550作用于攜帶JAK2V617F的小鼠 FDCP-EpoR細(xì)胞，具有顯著的促凋亡作用,然而效果比作用于攜帶野生型JAK2的細(xì)胞低。伴隨著抑制關(guān)鍵JAK2V617F依賴的下游信號效應(yīng)器信號轉(zhuǎn)導(dǎo)的磷酸化，及(STAT)3, STAT5, 和v-akt小鼠胸腺瘤病毒癌基因同源(AKT)的轉(zhuǎn)錄激活。[2] 此外, CP-690550 在體外作用于人獼猴 NK 和CD8+ T 細(xì)胞，抑制IL-15誘導(dǎo)的CD69表達(dá)。[3]
激酶實驗 酶實驗
進(jìn)行JAK1, JAK2, 和JAK3 激酶實驗，使用在桿狀病毒感染的 SF9細(xì)胞中表達(dá)的蛋白(GST 和人類JAK酶催化結(jié)構(gòu)域的融合蛋白)，通過親和層析在谷胱甘肽-瓊脂糖凝膠中純化。反應(yīng)底物是聚谷氨酸-酪氨酸 [PGT (4:1)], 按100 μg/mL包被到Nunc Maxi Sorp板上，在 37oC下過夜。然后沖洗板三次, 在每孔中加入JAK 酶，孔中含100 μL激酶buffer(50 mM HEPES, pH 7.3, 125 mM NaCl, 24 mM MgCl2) + ATP + 1 mM 釩酸鈉)。按不同劑量加入CP-690550，進(jìn)行激酶實驗。然后在室溫下溫育30分鐘，再沖洗實驗板三次。通過標(biāo)準(zhǔn)ELISA實驗，使用 磷酸化抗體測定一個給定孔中的磷酸化的酪氨酸水平。
細(xì)胞實驗 細(xì)胞系 HEL細(xì)胞, 擴(kuò)增的紅系祖細(xì)胞
濃度 0.1 μM,1 μM
孵育時間 40分鐘
方法

HEL細(xì)胞, 從正常供著，兩個PV病人體內(nèi)獲得的擴(kuò)大紅系祖細(xì)胞，和 FDCP-EpoR受體細(xì)胞(每組樣本2 × 107 個細(xì)胞),使用濃度不斷增高的 CP-690550處理, 然后在不同時間點收集。細(xì)胞制成顆粒，使用冷磷酸鹽緩沖液沖洗三次，然后懸浮在300 µL裂解液中 ，再在冰上處理1小時。細(xì)胞裂解液按20 000g轉(zhuǎn)速在 4oC下離心20分鐘,取出上清液。在上清液中加入15 µL anti-JAK2 (處理細(xì)胞) 或 anti-JAK3 兔抗體(未處理細(xì)胞)，然后在冰上再處理1小時。最后, 在上清液中加入50 µL 蛋白A/G瓊脂糖漿，然后在 4oC下不斷旋轉(zhuǎn)溫育過夜。沖洗抗體-蛋白復(fù)合體三次, 再使用放射免疫沉淀法(RIPA) buffer沖洗一次,使用沖洗沖洗一次,最后使用50 mM Tris-HCl buffer pH 為7.5沖洗一次。通過 Western blotting 分析免疫沉淀復(fù)合物，使用磷酸酪氨酸抗體，除去，再使用anti-JAK2和anti-JAK3抗體做探針，來分析免疫沉淀復(fù)合物。
實驗圖片 檢測方法 檢測指標(biāo) 實驗圖片 PMID
Western blot JAK3 / p-JAK3 / STAT3 LMP1 / EBNA1 / BZLF1 JAK3 / STAT5 / p-STAT5 26082451
Growth inhibition assay Cell number 27732937
體內(nèi)研究(In Vivo)
體內(nèi)研究活性 CP-690550 作用于小鼠模型，降低遲發(fā)型超敏感反應(yīng)和延長心臟移植存活。而且, CP-690550 處理來自JAK2V617F陽性 PV患者體內(nèi)外膨脹的紅系祖細(xì)胞，產(chǎn)生特定的抗增殖(IC50 = 0.2 μM) 和促凋亡活性。 相反, 在增殖(IC50 > 1.0 μM)和凋亡檢測時，從健康對照組中的膨脹祖細(xì)胞對CP-690550敏感性低很多。 [2] CP-690550按 10和30 mg/kg劑量每天處理NK細(xì)胞，持續(xù)處理2周，與對照組相比，細(xì)胞數(shù)顯著降低,這種作用存在時間依賴性。 CP-690550處理實驗組的動物效應(yīng)小樣記憶CD8+ 細(xì)胞數(shù)比對照組低55% 。[3]
動物實驗 Animal Models 毛里求斯成年獼猴
Dosages 10, 30 mg/kg/d
Administration 口服飼喂
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT06202560 Enrolling by invitation
Frontal Fibrosing Alopecia|Lichen Planopilaris
Institute of Dermatology Thailand
 November 29 2023 Not Applicable
NCT05487703 Completed
Arthritis Rheumatoid
Pfizer
 November 14 2022 --
NCT05082428 Completed
Ulcerative Colitis
Pfizer
 May 30 2022 --
NCT05728008 Completed
Ulcerative Colitis
IRCCS San Raffaele
 April 5 2022 --
NCT04768504 Recruiting
Immune-Mediated Colitis
Khashayar Esfahani|Sir Mortimer B. Davis - Jewish General Hospital
 March 22 2022 Phase 2

化學(xué)信息&溶解度

分子量 504.49 分子式

C16H20N6O.C6H8O7
CAS號 540737-29-9 SDF Download Tofacitinib (CP-690550) Citrate SDF
Smiles CC1CCN(CC1N(C)C2=NC=NC3=C2C=CN3)C(=O)CC#N.C(C(=O)O)C(CC(=O)O)(C(=O)O)O
儲存條件(自收到貨起)

體外溶解度
批次：

DMSO : 100 mg/mL ( (198.21 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : 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(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:
What is the difference between the two products (S5001, S2789)?

回答：
Tofacitinib (S2789) is the base form of Tofacitinib citrate (S5001). The biological activity of these two compound are same. S5001 is better than S2789 for Oral gavage.

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