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 |
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
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 |
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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