DCC-2036 (Rebastinib),抑制剂

DCC-2036 (Rebastinib) (订货以英文为准)

编号:D126373
CAS号:1020172-07-9
分子式:C30H28FN7O3
分子量:553.59
货号 品牌 包装 目录价 您的价格 库存 数量 购买
D126373-10mg 阿拉丁 10mg ¥926.90
D126373-50mg 阿拉丁 50mg ¥4170.90
D126373-5mg 阿拉丁 5mg ¥579.90
产品名称 DCC-2036 (Rebastinib)
中文名称 DCC-2036 (Rebastinib),抑制剂
CAS号 1020172-07-9
分子式(M.F.) C30H28FN7O3
分子量(M.W.) 553.59
储存条件 -20°C储存
溶解性DMSO 111 mg/mL Water <1 mg/mL Ethanol 16 mg/mL
存贮条件储存温度-20°C
备注DCC-2036 is a conformational control Bcr-Abl inhibitor for Abl1(WT) and Abl1(T315I) with IC50 of 0.8 nM and 4 nM, also inhibits SRC, LYN, FGR, HCK, KDR, FLT3, and Tie-2, and low activity to seen towards c-Kit. Phase 1/2.
生化机理The lead "switch-control" inhibitor, DCC-2036, potently inhibits both unphosphorylated and phosphorylated ABL1 by inducing a type II inactive conformation, and retains efficacy against the majority of clinically relevant CML-resistance mutants, including T315I. DCC-2036 inhibits autophosphorylation of ABL and ABLT315I enzymes, and this activity was consistent with selective efficacy against Ba/F3 cells expressing BCR-ABL (IC50: 19 nmol/L), BCR-ABLT315I (IC50: 63 nmol/L), and most kinase domain mutants. These findings support continued evaluation of DCC-2036 as an important new agent for treatment-refractory CML.
别名1-(3-tert-butyl-1-(quinolin-6-yl)-1H-pyrazol-5-yl)-3-(2-fluoro-4-(2-(methylcarbamoyl)pyridin-4-yloxy)phenyl)urea;1-(3-tert-butyl-1-(quinolin-6-yl)-1H-pyrazol-5-yl)-3-(2-fluoro-4-(2-(methylcarbamoyl)pyridin-4-yloxy)phenyl)urea
标识符号https://www.aladdin-e.com/images/ghs/ghs07.jpg
信号词Warning
危害声明H315-H319-H335
警示性声明P261-P305 + P351 + P338
个人防护设备dust mask type N95 (US), Eyeshields, Gloves
WGK德国3
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