| 溶解性 | DMSO 24 mg/mL Water <1 mg/mL Ethanol 40 mg/mL |
| 存贮条件 | 储存温度-20°C |
| 应用 | An antagonist to LNCaP AR |
| 产品介绍 | TOK-001 (VN/124-1; Galeterone)是多功能抗雄激素和CYP17抑制剂，IC50为47 nM。 |
| 备注 | Galeterone is a selective CYP17 inhibitor and androgen receptor (AR) antagonist with IC50 of 300 nM and 384 nM, respectively, and is a potent inhibitor of human prostate tumor growth. Phase 2. |
| 生化机理 | Galeterone is effective at preventing binding of [3H]-R1881 to the mutant LNCaP AR (T877A) and to T575A mutant AR in PC3 cells with IC50 values of 845 nM and 454 nM, respectively. The effects on AR significantly reduce cellular phospho-4EBP1 levels. Galeterone potently inhibits the proliferation of LNCaP and LAPC4 cells in the with IC50 values of 2.6 μM and 4 μM, respectively. Galeterone induces the endoplasmic reticulum s.tress response resulting in down-regulation of cyclin D1 protein expression and cyclin E2 mRNA. in vitro. |
| 别名 | TOK001;TOK 001;TOK-001;(3beta)-17-(1H-苯并咪唑-1-基)雄甾-5,16-二烯-3-醇;VN-124-1;VN/124-1;VN 124;3β-Hydroxy-17-(1H-benzimidazole-1-yl)androsta-5,16-diene |
Galeterone,CYP17抑制剂
Galeterone （订货以英文为准）
编号：T127853
CAS号：851983-85-2
分子式：C26H32N2O
分子量：388.56
| 产品名称 | Galeterone |
| 中文名称 | Galeterone,CYP17抑制剂 |
| CAS号 | 851983-85-2 |
| 分子式（M.F.） | C26H32N2O |
| 分子量（M.W.） | 388.56 |
| 储存条件 | -20°C储存 |
| 个人防护设备 | Eyeshields, Gloves, type N95 (US), type P1 (EN143) respirator filter |
| WGK德国 | 3 |
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