产品说明
生化/生理作用
TC-A2317 (TC-A 2317) is an orally active, potent and selective aurora A kinase inhibitor (Ki = 1.2 nM; Aurora B Ki = 101 nM; IC50 >1 μM toward 60 other kinases). TC-A2317 inhibits the proliferation of human colorectal carcinoma HCT116 cells in cultures (IC50 = 115 nM) and suppresses HCT116 xenograft-derived tumor growth in mice in vivo (by 59% on day 14; 30 mg/kg/day p.o.) with good pharmacokinectic properties, oral bioavailability (Tmax = 1.2 h, T1/2 = 3.3 h, Cmax = 4930 nM, C60 min = 52 nM in rat serum post 30 mg/kg p.o.), and no adverse effects to the animals. TC-A231 is a racemate with its (S)-enantiomer being more active than the (R)-enantiomer (respective Ki = 0.59 vs. 66 nM).
Orally active, potent and selective aurora A kinase inhibitor with anti-cancer activity in vitro and in vivo.
基本信息
| 经验(实验)分子式 | C19H28N6O · HCl |
| 分子量 | 392.93 |
| MDL编号 | MFCD19690936 |
产品性质
| 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 | CC1=CC(NC2=NNC(C)=C2)=NC(NC(C)CCCC(C)(C)O)=C1C#N.Cl |
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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