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首页-小分子抑制剂&激动剂-JAK/STAT Signaling-JAK-TG-101348
TG-101348

Chemical Structure : TG-101348

CAS No.: 936091-26-8

TG-101348 (Fedratinib, SAR302503, TG101348)

货号: PC-42569Not For Human Use, Lab Use Only.

TG-101348 (Fedratinib, SAR302503) is a potent, selective JAK2 inhibitor with IC50 of 3 nM for both wt JAK2 and JAK2 V617F.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

TG-101348 (Fedratinib, SAR302503) is a potent, selective JAK2 inhibitor with IC50 of 3 nM for both wt JAK2 and JAK2 V617F.
TG-101348 also inhibits FLT3 (IC50=15 nM) and RET (IC50=48 nM) kinases, weakly inhibits JAK3 (IC50=168 nM), >35-fold selectivity over JAK1/3 and Tyk2.
TG-101348 shows therapeutic efficacy in a murine model of myeloproliferative disease induced by the JAK2V617F mutation.
TG-101348 also potently inhibits BRD4 with Kd of 168 nM.

物理化学性质&存储条件

分子量 524.6782
分子式 C27H36N6O3S
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: ≥ 42 mg/mL

Chemical Name/SMILES

Benzenesulfonamide, N-(1,1-dimethylethyl)-3-[[5-methyl-2-[[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]amino]-4-pyrimidinyl]amino]-

参考文献

1. Pardanani A, et al. Leukemia. 2007 Aug;21(8):1658-68.

2. Ciceri P, et al. Nat Chem Biol. 2014 Apr;10(4):305-12.

3. Wernig G, et al. Cancer Cell. 2008 Apr;13(4):311-20.

4. Geron I, et al. Cancer Cell. 2008 Apr;13(4):321-30.

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