Fedratinib
Cat. No.:YN340054
CAS No. :936091-26-8
产品名称: | Fedratinib |
CAS No.: | 936091-26-8 |
Chemical Name: | N-(1,1-dimethylethyl)-3-[[5-methyl-2-[[4-[2-(1-pyrrolidinyl)ethoxy]phenyl]amino]-4-pyrimidinyl]amino]-benzenesulfonamide |
Synonyms: | TG-101348; SAR 302503 |
分子量: | 524.68 |
分子式: | C₂₇H₃₆N₆O₃S |
SMILES: | O=S(C1=CC=CC(NC2=NC(NC3=CC=C(C=C3)OCCN4CCCC4)=NC=C2C)=C1)(NC(C)(C)C)=O |
存储: | Please store the product under the recommended conditions in theCertificate of Analysis. |
运输: | Room temperature in continental US; may vary elsewhere. |
产品描述: | Fedratinib (TG-101348) 是一种有效的,选择性的,ATP 竞争性和具有口服活性的JAK2抑制剂,对于JAK2和JAK2V617F激酶的IC50均为 3 nM。Fedratinib 对JAK2的选择性分别比 JAK1 和 JAK3 高 35 倍和 334 倍。Fedratinib 可诱导癌细胞凋亡 (apoptosis),并可用于骨髓增生性疾病的研究。 |
IC50和靶点: | [{name:"JAK2:3 nM (IC50)"},{name: "JAK2(V617F):3 nM (IC50)"},{name: "Flt3:15 nM (IC50)"},{name: "Ret:48 nM (IC50)"}] |
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Wernig, G., Kharas, M.G., Okabe, R.O., et al.Efficacy of TG101348, a selective JAK2 inhibitor, in treatment of a murine model of JAK2V617F-induced polycythemia veraCancer Cell13(4),311-320(2008)
Geron, I., Abrahamsson, A.E., Barroga, C.F., et al.Selective inhibition of JAK2-driven erythroid differentiation of polycythemia vera progenitorsCancer Cell13(4),321-330(2008)