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Tofacitinib

別名: CP-690550, Tasocitinib 中文名稱：托法替尼,托法替布

Tofacitinib是一種新型JAK3抑制劑，在無細(xì)胞試驗(yàn)中IC50為1 nM，作用于JAK2和JAK1選擇性低20到100倍。Tofacitinib 可在人類漿細(xì)胞樣樹突狀細(xì)胞PDC中抑制抗凋亡的BCL-A1和BCL-XL并誘導(dǎo)PDC凋亡。

Tofacitinib Chemical Structure

Tofacitinib Chemical Structure

CAS: 477600-75-2

規(guī)格 價格 庫存 購買數(shù)量
10mM (1mL in DMSO) 744.01 現(xiàn)貨
5mg 582.19 現(xiàn)貨
10mg 729.41 現(xiàn)貨
100mg 3012.77 現(xiàn)貨
1g 7944.3 現(xiàn)貨
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常與Tofacitinib一起在實(shí)驗(yàn)中被使用的化合物

Ruxolitinib

Tofacitinib和Ruxolitinib用于治療多種自身免疫性疾病。

Baricitinib

與抗風(fēng)濕生物藥相比，Tofacitinib和Baricitinib具有同等的療效。

Barbulescu A, et al. Rheumatology (Oxford). 2022 Oct 6;61(10):3952-3962.

Fedratinib (TG101348)

Tofacitinib被批準(zhǔn)用于治療類風(fēng)濕性關(guān)節(jié)炎，而Fedratinib則被FDA批準(zhǔn)用于治療類風(fēng)濕性關(guān)節(jié)炎的臨床。

Shwaky AM, et al. Pharmaceutics. 2022 May 6;14(5):1001.

Infliximab (anti-TNF-alpha)

Tofacitinib和Infliximab通過降低免疫原性來治療難治性潰瘍性結(jié)腸炎，顯示出協(xié)同作用。

Gilmore R, et al. Clin Gastroenterol Hepatol. 2021 Jun;19(6):1302-1303.

Dexamethasone

Tofacitinib和Dexamethasone可降低hMSC移植產(chǎn)生的免疫反應(yīng)。

Lee NK, et al. Biomedicines. 2022 Aug 4;10(8):1882.

Tofacitinib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(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系 實(shí)驗(yàn)類型 給藥濃度 孵育時間 活性描述 文獻(xiàn)信息
CD4+?T? Growth Inhibition Assay 100/500 nM 48 h inhibits anti-CD3-induced CD4+?T cell proliferation 21884580
CD4+?T? Function Assay 100 nM 24/48 h abrogates CD3-induced phosphorylation of STATs 21884580
T cells Function Assay 0.1/0.3/1 μM 24 h disrupts γc-chain cytokine signaling 21383241
CD4+?T? Function Assay 20/100/500 nM 48 h inhibits the levels of IL-4, IFN-γ, IL-17A and IL-22 21884580
NK-cells 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
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 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 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 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 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 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
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
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
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
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
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
HUO3 Function assay 4 days Inhibition of human GM-CSF-induced proliferation in human HUO3 cells assessed as [3H]thymidine incorporation after 4 days by scintillation counting, IC50 = 0.324 μM. 14593182
HU03 Function assay 72 hrs Inhibition of GM-CSF-induced human HU03 cells proliferation after 72 hrs by [3H]thymidine incorporation assay, IC50 = 0.324 μM. 21105711
BAF3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BAF3 cells expressing TEL-JAK3 kinase after 72 hrs by alamar blue assay, IC50 = 0.57 μM. 19762238
T-cells Function assay 3 days Inhibition of cell proliferation of IL2-activated and CD3 and CD28 antibody-stimulated mouse CD4-positive T cells after 3 days by XTT assay, IC50 = 0.63 μM. 30460842
NK92 Function assay 20 mins Inhibition of TYK2 in human NK92 cells assessed as inhibition of IL12-induced STAT4 phosphorylation incubated for 20 mins followed by IL12 challenge for 45 mins, EC50 = 0.71 μM. 23659214
Ba/F3 Function assay 60 mins Inhibition of TEL-fused TYK2 expressed in Ba/F3 cells assessed as inhibition of STAT5 phosphorylation after 60 mins by AlphaScreen assay, IC50 = 1.2 μM. 22087750
T-cells Function assay 72 hrs Inhibition of JAK3 in rat splenocytic T cells assessed as reduction in IL-2-induced cell proliferation after 72 hrs by MTS assay, IC50 = 1.2 μM. 30139575
BAF3 Antiproliferative assay 72 hrs Antiproliferative activity against mouse BAF3 cells expressing TEL-JAK2 kinase after 72 hrs by alamar blue assay, IC50 = 1.574 μM. 19762238
HEL Function assay 1 hr Inhibition of JAK2 V617F mutant in human HEL cells after 1 hr, IC50 = 4.724 μM. 27771180
Jurkat Function assay 24 hrs Inhibition of anti-CD3/anti-CD28-induced IL2 production in human Jurkat cells after 24 hrs by scintillation counting, IC50 = 7.84 μM. 14593182
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
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
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 GST-tagged human JAK3 catalytic domain expressed in Sf9 cells by ELISA, IC50 = 0.0033 μM. 21105711
insect cells Function assay Inhibition of GST-tagged Jak1 expressed in insect cells using 70 uM ATP, IC50 = 0.0061 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 Jak2 expressed in insect cells using 20 uM ATP, IC50 = 0.012 μM. 21155605
MO7 Function assay Inhibition of Jak3-mediated IL15-induced Stat5 phosphorylation in human MO7 cells by cell-based assay, IC50 = 0.024 μM. 21155605
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
PBMC Function assay Inhibition IL-7-indcued STAT5 phosphorylation in human PBMC cells by flow cytometry, IC50 = 0.039 μM. 26927423
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
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 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
CD34+ Function assay 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
TF1 Function assay Inhibition of IL3-induced proliferation of TF1 cells, IC50 = 0.8 μM. 16934457
UT7 Function assay Inhibition of JAK2 in human UT7 cells assessed as suppression of EPO-stimulated STAT5 phosphorylation by AlphaScreen assay, INH = 1.12 μM. 26372653
SZ4 Function assay Inhibition of JAK3 in human SZ4 cells assessed as reduction in IL2-stimulated STAT5 phosphorylation preincubated for 1 hr followed by IL2 stimulation and measured after 15 mins by MSD assay, IC50 = 1.21 μM. 30460842
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生物活性

產(chǎn)品描述 Tofacitinib是一種新型JAK3抑制劑，在無細(xì)胞試驗(yàn)中IC50為1 nM，作用于JAK2和JAK1選擇性低20到100倍。Tofacitinib 可在人類漿細(xì)胞樣樹突狀細(xì)胞PDC中抑制抗凋亡的BCL-A1和BCL-XL并誘導(dǎo)PDC凋亡。
靶點(diǎn)
JAK3 [1]
(Cell-free assay)		 JAK2 [1]
(Cell-free assay)		 JAK1 [1]
(Cell-free assay)
1 nM 20 nM 112 nM
體外研究(In Vitro)
體外研究活性 CP-690550 是特定的口服JAK3抑制劑, 作用于JAK2 和 JAK1,效果分別低20和100倍。CP-690550 對30種其他激酶沒有作用效果，平均IC50 > 3000 nM。CP-690,550抑制IL-2誘導(dǎo)的增殖，比作用于GM-CSF誘導(dǎo)的增殖效果強(qiáng)30倍。[1] CP-690550 高效抑制小鼠混合淋巴反應(yīng)(MLR)(IC50 = 91 nM)。[2] CP-690550 作用于小鼠 B細(xì)胞，有效抑制 IL-4 誘導(dǎo)的 CD23 (IC50=57 nM) 和II 類主要組織相容性復(fù)合體(MHCII) 表達(dá)上調(diào)，IC50=71 nM。[3]最新研究顯示，通過加強(qiáng) Th17分化，低劑量CP-690550加速實(shí)驗(yàn)性自身免疫腦脊髓炎的發(fā)生。[4]
激酶實(shí)驗(yàn) JAK3 激酶實(shí)驗(yàn)
全長cDNA中編碼人JAK3 催化結(jié)構(gòu)域(785aa到 1125aa, JH1 催化結(jié)構(gòu)域)的片段通過PCR放大，且克隆到桿狀病毒轉(zhuǎn)移載體 pVL1393的EcoRI位點(diǎn)。使用重組桿狀病毒感染 Sf9 細(xì)胞，在谷胱甘肽瓊脂糖凝膠上分離重組 GSTJAK3融合蛋白。使用還原型谷胱甘肽洗脫融合蛋白，然后儲存在含50 mM Tris, pH 7.5, 10 mM DTT 和 10% 甘油的緩沖液中。通過ELISA按如下測量JAK3激酶活性: 使用隨機(jī)L-谷氨酸和酪氨酸共聚物 (4:1) (100 ug/mL)包被實(shí)驗(yàn)板過夜。沖洗實(shí)驗(yàn)板，在有或無抑制劑時，重組JAK3 JH1:GST(每孔100 ng)在室溫下溫育30分鐘，然后加入HRP結(jié)合的PY20抗磷酸酪氨酸抗體(ICN)，然后通過TMB(3,3’,5,5’-四甲基聯(lián)苯胺)電泳。使用 ELISA法測定酪氨酸激酶催化活性，而通過放射性酶實(shí)驗(yàn)測定絲/蘇氨酸激酶。
細(xì)胞實(shí)驗(yàn) 細(xì)胞系 人類T 細(xì)胞
濃度 0-4000 nM
孵育時間 4天
方法 為了測量 IL-2依賴的增殖，分離的淋巴細(xì)胞按1-2 × 106/mL密度再懸浮在完全RPMI培養(yǎng)基(RPMI 1640含 10% (w/v)胎牛血清(FCS), 1%(w/v) 青霉素和鏈霉素 )中。加入植物血細(xì)胞凝集素(PHA)，終濃度為10mg/mL, 培養(yǎng)物在37oC 下含 5% (v/v) CO2 濕潤孵育器中溫育3天，用于上調(diào)IL-2R 和 JAK3 表達(dá)。在有或無CP-690,550 時，加入 IL-2 (200U/mL), 細(xì)胞在 37oC下含 5% (v/v) CO2濕潤孵育器中溫育，72小時后加入50 mL 3H-胸甘(5mCi/mL)。實(shí)驗(yàn)板再溫育18小時，使用 96孔收集器收集，然后在閃爍計(jì)數(shù)器中計(jì)數(shù)。HUO3細(xì)胞培養(yǎng)在含粒細(xì)胞-巨噬細(xì)胞集落刺激因子的培養(yǎng)基中，人包皮成纖維細(xì)胞培養(yǎng)在含10% 胎牛血清的培養(yǎng)基中。在新鮮培養(yǎng)的細(xì)胞中加入CP-690550，培養(yǎng)4天。在培養(yǎng)期的最后18小時，加入3 H胸甘。
實(shí)驗(yàn)圖片 檢測方法 檢測指標(biāo) 實(shí)驗(yàn)圖片 PMID
Western blot JAK3 / STAT5 / p-STAT5 LMP1 / EBNA1 / BZLF1 JAK3 / p-JAK3 / STAT3 27732937
Growth inhibition assay Cell number 27732937
體內(nèi)研究(In Vivo)
體內(nèi)研究活性 CP-690550作用于異位心臟移植(DBA2供體心臟移到C57/BL6宿主 )的小鼠模型，提高移植后心臟的壽命，這種作用存在劑量依賴性。EC50(50%小鼠將保持移植 >28天時血液中藥物濃度) 為~60 ng/mL。CP-690550 作用于非人靈長類動物 (NHPs, 食蟹猴) (50 到100 ng/ml劑量實(shí)驗(yàn)組和200 到400 ng/ml劑量實(shí)驗(yàn)組的MST分別為62和83天)，防止同種異體腎移植的排斥反應(yīng)。[1] CP-690550 每天按1.5-15 mg/kg劑量長期作用于小鼠，通過流式細(xì)胞儀檢測，發(fā)現(xiàn)淋巴細(xì)胞亞群發(fā)生改變，這種作用存在劑量和時間依賴性。處理21天，觀察到最顯著的變化是脾NK1.1+TCRb 細(xì)胞數(shù)降低96%。CP-690550 按1.87-30 mg/kg劑量皮下注射給藥敏感小鼠，延遲型過敏反應(yīng)降低，這種作用存在劑量依賴性。
動物實(shí)驗(yàn) Animal Models DBA/2 和 C57/BL6 小鼠
Dosages 0-136 ng/mL
Administration 滲透微泵輸入
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 312.37 分子式

C16H20N6O
CAS號 477600-75-2 SDF Download Tofacitinib SDF
Smiles CC1CCN(CC1N(C)C2=NC=NC3=C2C=CN3)C(=O)CC#N
儲存條件(自收到貨起)

體外溶解度
批次：

DMSO : 62 mg/mL ( (198.48 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(jì)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(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

動物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請輸入基本實(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(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，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:
I was just wondering what the main differences between S2789 and S5001?

回答：
S2789(Tofacitinib (CP-690550)) is the base form of S5001 (Tofacitinib (CP-690550) Citrate). The biological activity of these two compounds are same. The S5001 (Tofacitinib (CP-690550) Citrate) is more suitable for oral administration.

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