半岛bd体育手机客户端 说明
生化/生理作用
DCC-2618 is an orally active, potent type II switch pocket (SP) inhibitor against c-KIT (IC50= 4 nM/WT, 8 nM/V654A, 18 nM/T670I, 5 nM/D816H, 14 nM/D816V) and PDGFR. DCC-2618 locks c-KIT & PDGFR in an inactive conformation and is effective against multiple clinical forms of mutations resistant to type I ATP (catalytic)-site inhibitors Imatinib and Sunitinib. DCC-2618 inhibits cellular c-KIT activation (IC50= 36 nM/WT, 2 nM/ex 11 del, 7 nM/ex 11 del & V654A, 53 nM/V560D & D820A) and is efficacious against KIT mutants-mediated cancer growth in cultres (IC50= 2 nM; GIST with KIT D816Y) and in micein vivo(50 mg/kg b.i.d. p.o.; GIST with KIT delW557K558/Y823D, AML with KIT N822K).
基本信息
| 经验(实验)分子式 | C26H21F2N5O3 |
| 分子量 | 489.47 |
| MDL编号 | MFCD22571733 |
半岛bd体育手机客户端 性质
| 质量水平 | 100 |
| 测定 | ≥98% (HPLC) |
| 形式 | powder |
| 颜色 | white to beige |
| 溶解性 | DMSO: 2 mg/mL, clear |
| 储存温度 | ?20℃ |
| SMILES string | O=C(NC1=CC=CC=C1)C2(CC2)C(NC(C=C3F)=C(F)C=C3OC4=CC(C5=CN(C)N=C5)=NC=C4)=O |
安全信息
| 储存分类代码 | 11 - Combustible Solids |
| WGK | WGK 3 |
| 闪点(F) | Not applicable |
| 闪点(C) | Not applicable |
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