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首页-小分子抑制剂&激动剂-JAK/STAT Signaling-JAK-Tofacitinib
Tofacitinib

Chemical Structure : Tofacitinib

CAS No.: 477600-75-2

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Tofacitinib (CP-690550, CP690550, Tasocitinib)

货号: PC-45816Not For Human Use, Lab Use Only.

Tofacitinib (CP-690550) is a potent, specific, orally active inhibitor of JAK3 with IC50 of 1 nM in cell-free assays.

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50 mg ￥1480 In stock
100 mg ￥2280 In stock
250 mg ￥3580 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Tofacitinib (CP-690550) is a potent, specific, orally active inhibitor of JAK3 with IC50 of 1 nM in cell-free assays.
Tofacitinib (CP-690550) displays 20- to 100-fold less potency for JAK2 and JAK1 (IC50=20 nM and 112 nM, respectively), and shows no potent activity against 30 other kinases at >3 uM (CaMK1, ROCK2, Lck, MST2, etc.).
Tofacitinib (CP-690550) effectively inhibits a murine mixed lymphocyte reaction (MLR) with IC50 of 91 nM.
Tofacitinib (CP-690550) significantly prolonges survival in a murine model of heart transplantation and in cynomolgus monkeys receiving kidney transplants.

物理化学性质&存储条件

分子量 312.37
分子式 C16H20N6O
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping
Solubility

DMSO: 100 mM (31.2 mg/mL); H2O: <1 mM (<0.3 mg/mL)
Chemical Name/SMILES

1-Piperidinepropanenitrile, 4-methyl-3-(methyl-7H-pyrrolo[2,3-d]pyrimidin-4-ylamino)-.beta.-oxo-, (3R,4R)-

参考文献

1. Changelian PS, et al. Science. 2003 Oct 31;302(5646):875-8.

2. Jiang JK, et al. J Med Chem. 2008 Dec 25;51(24):8012-8.

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

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