450839-40-4
中文名稱(chēng)
ABT-100
英文名稱(chēng)
ABT-100
CAS
450839-40-4
分子式
C27H19F3N4O3
分子量
504.46
MOL 文件
450839-40-4.mol
450839-40-4 結(jié)構(gòu)式
物理化學(xué)性質(zhì)
沸點(diǎn)722.0±60.0 °C(Predicted)
密度1.29±0.1 g/cm3(Predicted)
儲(chǔ)存條件-20°C, protect from light
酸度系數(shù)(pKa)12.15±0.29(Predicted)
形態(tài)Solid
顏色White to off-white
常見(jiàn)問(wèn)題列表
生物活性
ABT-100 是一種有效的，高選擇性和口服活性的 farnesyltransferase 抑制劑。ABT-100 抑制細(xì)胞增殖 (對(duì)于 EJ-1，DLD-1，MDA-MB-231，HCT-116，MiaPaCa-2，PC-3 和 DU-145 細(xì)胞的 IC50 分別為 2.2 nM，3.8 nM，5.9 nM，6.9 nM，9.2 nM，70 nM 和 818 nM)，可增加細(xì)胞凋亡并減少血管生成。ABT-100 具有廣譜抗腫瘤活性。靶點(diǎn)
Farnesyltransferase
體外研究
ABT-100 (0.1-100 nM; 7 days; EJ-1, DLD-1, MDA-MB-231, HCT-116, MiaPaCa-2, PC-3, and DU-145 cells) treatment shows dose-dependent growth inhibition of human cancer cell lines. Also inhibits colony formation at concentrations comparable with which ABT-100 inhibits anchorage-dependent growth.
Cell Proliferation Assay
| Cell Line: | EJ-1, DLD-1, MDA-MB-231, HCT-116, MiaPaCa-2, PC-3, and DU-145 cells |
| Concentration: | 0.1-100 nM |
| Incubation Time: | 7 days |
| Result: | Demonstrated dose-dependent growth inhibition of human cancer cell lines. |
體內(nèi)研究
ABT-100 (6.25-12.5 mg/kg/day; subcutaneous injection; daily; for 21 days; C.B-17 scid male mice) treatment regresses EJ-1 tumors in mice.
| Animal Model: | C.B-17 scid male mice with EJ-1 cells |
| Dosage: | 6.25 mg/kg/day, 12.5 mg/kg/day |
| Administration: | Subcutaneous injection; daily; for 21 days |
| Result: | Regressed EJ-1 tumors in C.B-17 scid male mice. |