TG-101348

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

TG-101348 (Fedratinib, SAR302503) 是一种有效的选择性 JAK2 抑制剂，对 wt JAK2 和 JAK2 V617F 的 IC50 均为 3 nM。

TG-101348 (Fedratinib, SAR302503)?is a potent, selective JAK2 inhibitor with IC50 of 3 nM for both wt JAK2 and JAK2 V617F; 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; shows therapeutic efficacy in a murine model of myeloproliferative disease induced by the JAK2V617F mutation; also potently inhibits BRD4 with Kd of 168 nM.Bone Cancer Phase 3 Clinical.

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Animal Model:C57Bl/6 mice induced by the JAK2V617F mutation Dosage:60 mg/kg, 120 mg/kg Administration:Oral gavage; twice daily; for 42 days Result:Showed a statistically significant reduction in hematocrit and leukocyte count, a dose-dependent reduction/elimination of extramedullary hematopoiesis.

Fedratinib | SAR 302503 | TG101348 | TG 101348

Angiogenesis

JAK

FLT3|JAK2|JAK2(V617F)|RET

Cancer

Bone Cancer

936091-26-8

524.6782

C27H36N6O3S

>98% (HPLC)

DMSO: ≥ 42 mg/mL

O=S(C1=CC=CC(NC2=NC(NC3=CC=C(OCCN4CCCC4)C=C3)=NC=C2C)=C1)(NC(C)(C)C)=O

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

(-20℃)

With Ice Pack

≥ 2 years