产品说明
一般描述
An orally bioavailable oxindolo-furanyl compound that acts as a potent, reversible and ATP-competitive inhibitor of pan PIM-kinases (IC50 = 5, 25 and 16 nM for PIM-1, PIM-2 and PIM-3, respectively; Ki = 5 nM for PIM-1) with excellent selectivity over 107 kinases (IC80 >500 nM). Shown to arrest the proliferation of several human cancer cells (IC50 = 20 and 452 nM for MV-4-11 and PC3 cells) and block phosphorylation of Bad-Ser112, 4E-BP1-Ser65 and Thr37/46 with an IC50 of ~ 1.0 µM. Displays favorable pharmacokinetic profile and efficacy in mice, and suppresses tumor growth in MV-4-11 and PC3 xenograft murine model (50 mg/kg, p.o.). Further, potentiates doxorubicin (Cat. No. 324380) and paclitaxel (Cat. No. 580555) toxicity in PC3 cells.
包装
10 mg in Glass bottle
Packaged under inert gas
生化/生理作用
Cell permeable: yes
Primary Target
PIM Kimases
Target IC50: 5, 25 and 16 nM for PIM-1, PIM-2 and PIM-3
Reversible: yes
Secondary Target
Flt3
警告
Toxicity: Standard Handling (A)
重悬
Following reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 6 months at -70°C.
其他说明
Haddach, M., et al. 2012. ACS Med. Chem. Lett.3, 135.
法律信息
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
基本信息
| 经验(实验)分子式 | C26H24ClN3O3 · xHCl |
| 分子量 | 461.94 (free base basis) |
产品性质
| 质量水平 | 100 |
| 测定 | ≥99% (HPLC) |
| 形式 | powder |
| manufacturer/tradename | Calbiochem® |
| 储存条件 | OK to freeze desiccated (hygroscopic) protect from light |
| 颜色 | orange |
| 溶解性 | DMSO: 25 mg/mL |
| 运输 | ambient |
| 储存温度 | 2-8℃ |
| SMILES string | O=C(/C1=C/C2=CC=C(C3=CC=CC(C(N4CCCN(C)CC4)=O)=C3)O2)NC5=C1C=C(Cl)C=C5.[xHCl] |
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 |
