Chemical Structure : Fedratinib
CAS No.: 936091-26-8
货号: PC-42569Not For Human Use, Lab Use Only.
Fedratinib (TG-101348, SAR302503) is a potent, selective JAK2 inhibitor with IC50 of 3 nM for both wt JAK2 and JAK2 V617F.
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---|---|---|---|
10 mg | ¥480 | In stock | |
50 mg | ¥780 | In stock | |
100 mg | ¥1180 | In stock | |
250 mg | ¥1880 | In stock | |
500 mg | ¥2980 | In stock | |
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Fedratinib (TG-101348, 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.
分子量 | 524.6782 | |
分子式 | C27H36N6O3S | |
外观性状 | Solid | |
储存条件 |
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Solubility |
DMSO: ≥ 42 mg/mL |
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Chemical Name/SMILES |
Benzenesulfonamide, N-(1,1-dimethylethyl)-3-[[5-methyl-2-[[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]amino]-4-pyrimidinyl]amino]- |
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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