Tofacitinib (CP-690550) Citrate
别名: Tasocitinib Citrate,CP-690550 中文名称：枸橼酸托法替尼
Tofacitinib citrate (CP-690550, Tasocitinib)是一种新型JAK抑制剂，对JAK3，JAK2，JAK1的IC50分别为1 nM, 20 nM 和112 nM。Tofacitinib citrate 还具有抗感染的活性。
Tofacitinib (CP-690550) Citrate Chemical Structure
CAS: 540737-29-9
产品质控
批次：
纯度：
99.99%
99.99
常与Tofacitinib (CP-690550) Citrate一起在实验中被使用的化合物
Tofacitinib和Methotrexate联合疗法在治疗类风湿性关节炎方面不劣于Adalimumab和Methotrexate联合疗法。
Fleischmann R, et al. Lancet. 2017 Jul 29;390(10093):457-468.
CP-690550与Cyclosporine联合使用，在小鼠新生血管同种异体心脏移植模型中的疗效得到显着提高。
CP-690550和Mycophenolate mofetil联合使用可显着提高同种异体移植物的存活率。
Borie DC, et al. Transplantation. 2005 Dec 27;80(12):1756-64.
Tofacitinib和Ruxolitinib在治疗多种自身免疫性疾病方面表现出潜在功效。
Sadeghi S, et al. Dermatol Pract Concept. 2022 Oct 1;12(4):e2022178.
在CD4+T细胞、NK细胞和单核细胞中，Tofacitinib对IL-2、IL-4、IL-15和IL-21信号传导的STAT抑制率高于Baricitinib。
Mclnnes IB, et al. Arthritis Res Ther. 2019 Aug 2;21(1):183.
Tofacitinib (CP-690550) Citrate相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| 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 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Tofacitinib citrate (CP-690550, Tasocitinib)是一种新型JAK抑制剂，对JAK3，JAK2，JAK1的IC50分别为1 nM, 20 nM 和112 nM。Tofacitinib citrate 还具有抗感染的活性。 | ||||
|---|---|---|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | CP-690550抑制IL-2调节的人T细胞爆发式增殖，和IL-15诱导的CD69表达，IC50分别为11和48 nM。CP-690550抑制混合淋巴细胞反应，IC50为87 nM。CPCP-690550 处理含人野生型或V617F JAK2的鼠因子依赖的细胞Patersen–促红细胞生成素受体(FDCP-EpoR) 细胞，抑制细胞增殖，IC50分别为2.1 µM 和0.25 µM。CP-690550 抑制白细胞介素-6诱导的STAT1 和STAT3磷酸化，IC50分别为23和77 nM。而且, CP-690550作用于携带JAK2V617F的小鼠 FDCP-EpoR细胞，具有显著的促凋亡作用,然而效果比作用于携带野生型JAK2的细胞低。伴随着抑制关键JAK2V617F依赖的下游信号效应器信号转导的磷酸化，及(STAT)3, STAT5, 和v-akt小鼠胸腺瘤病毒癌基因同源(AKT)的转录激活。[2] 此外, CP-690550 在体外作用于人猕猴 NK 和CD8+ T 细胞，抑制IL-15诱导的CD69表达。[3] | |||
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| 激酶实验 | 酶实验 | |||
| 进行JAK1, JAK2, 和JAK3 激酶实验，使用在杆状病毒感染的 SF9细胞中表达的蛋白(GST 和人类JAK酶催化结构域的融合蛋白)，通过亲和层析在谷胱甘肽-琼脂糖凝胶中纯化。反应底物是聚谷氨酸-酪氨酸 [PGT (4:1)], 按100 μg/mL包被到Nunc Maxi Sorp板上，在 37oC下过夜。然后冲洗板三次, 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 钒酸钠)。按不同剂量加入CP-690550，进行激酶实验。然后在室温下温育30分钟，再冲洗实验板三次。通过标准ELISA实验，使用 磷酸化抗体测定一个给定孔中的磷酸化的酪氨酸水平。 | ||||
| 细胞实验 | 细胞系 | HEL细胞, 扩增的红系祖细胞 | ||
| 浓度 | 0.1 μM,1 μM | |||
| 孵育时间 | 40分钟 | |||
| 方法 | HEL细胞, 从正常供着，两个PV病人体内获得的扩大红系祖细胞，和 FDCP-EpoR受体细胞(每组样本2 × 107 个细胞),使用浓度不断增高的 CP-690550处理, 然后在不同时间点收集。细胞制成颗粒，使用冷磷酸盐缓冲液冲洗三次，然后悬浮在300 µL裂解液中 ，再在冰上处理1小时。细胞裂解液按20 000g转速在 4oC下离心20分钟,取出上清液。在上清液中加入15 µL anti-JAK2 (处理细胞) 或 anti-JAK3 兔抗体(未处理细胞)，然后在冰上再处理1小时。最后, 在上清液中加入50 µL 蛋白A/G琼脂糖浆，然后在 4oC下不断旋转温育过夜。冲洗抗体-蛋白复合体三次, 再使用放射免疫沉淀法(RIPA) buffer冲洗一次,使用冲洗冲洗一次,最后使用50 mM Tris-HCl buffer pH 为7.5冲洗一次。通过 Western blotting 分析免疫沉淀复合物，使用磷酸酪氨酸抗体，除去，再使用anti-JAK2和anti-JAK3抗体做探针，来分析免疫沉淀复合物。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | JAK3 / p-JAK3 / STAT3 LMP1 / EBNA1 / BZLF1 JAK3 / STAT5 / p-STAT5 |
|
26082451 | |
| Growth inhibition assay | Cell number |
|
27732937 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | CP-690550 作用于小鼠模型，降低迟发型超敏感反应和延长心脏移植存活。而且, CP-690550 处理来自JAK2V617F阳性 PV患者体内外膨胀的红系祖细胞，产生特定的抗增殖(IC50 = 0.2 µM) 和促凋亡活性。 相反, 在增殖(IC50 > 1.0 µM)和凋亡检测时，从健康对照组中的膨胀祖细胞对CP-690550敏感性低很多。 [2] CP-690550按 10和30 mg/kg剂量每天处理NK细胞，持续处理2周，与对照组相比，细胞数显著降低,这种作用存在时间依赖性。 CP-690550处理实验组的动物效应小样记忆CD8+ 细胞数比对照组低55% 。[3] | |
|---|---|---|
| 动物实验 | Animal Models | 毛里求斯成年猕猴 |
| Dosages | 10, 30 mg/kg/d | |
| Administration | 口服饲喂 | |
| 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 |
化学信息&溶解度
| 分子量 | 504.49 | 分子式 | C16H20N6O.C6H8O7 |
| CAS号 | 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 | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 100 mg/mL ( (198.21 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble Ethanol : Insoluble |
摩尔浓度计算器 |
|
体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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常见问题及建议解决方法
问题 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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