Avapritinib
Cat. No.:YN440036
产品名称: | Avapritinib |
CAS No.: | 1703793-34-3 |
Chemical Name: | (αS)-(4-fluorophenyl)-α-methyl-2-[4-[6-(1-methyl-1H-pyrazol-4-yl)pyrrolo[2,1-f][1,2,4]triazin-4-yl]-1-piperazinyl]-5-pyrimidinemethanamine |
Synonyms: | BLU-285 |
分子量: | 498.56 |
分子式: | C₂₆H₂₇FN₁₀ |
SMILES: | CN1N=CC(C2=CN3C(C(N4CCN(C5=NC=C([C@@](C)(N)C6=CC=C(F)C=C6)C=N5)CC4)=NC=N3)=C2)=C1 |
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: | Avapritinib (BLU-285) 是一种高效、选择性、口服生活性的KIT和PDGFRA激活环突变激酶抑制剂,其对KIT D816V和PDGFRA D842V的IC50值分别为 0.27 和 0.24 nM。Avapritinib (BLU-285) 与激酶的活性构象结合,并显示抗肿瘤活性。Avapritinib (BLU-285) 减弱 ABCB1 和 ABCG2 的传输功能。 |
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Evans, E.K., Gardino, A.K., Kim, J.L., et al.A precision therapy against cancers driven by KIT/PDGFRA mutationsSci. Transl. Med.9(414),eaao1690(2017)