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PIM-Kinase Inhibitor X, CX-6258-Calbiochem
| 产品编号： | 4168410 |
| 规格： | The PIM-Kinase Inhibitor X, CX-6258 controls the biological activity of PIM-Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications. |
| 包装规格： | 10 MG |
| 产品类别： | 进口试剂 |
| 品牌： | Sigma-Aldrich |
| 优惠价： | 立即咨询 |
产品别名
PIM-Kinase Inhibitor X, CX-6258-Calbiochem
( E)-5-Chloro-3-((5-(3-(4-methyl-1,4-diazepane-1-carbonyl)phenyl)furan-2-yl)methylene)indolin-2-one, HCl
结构式
基本信息
| Empirical Formula【经验(实验)分子式】 | C26H24ClN3O3 · xHCl |
| Molecular weight | 461.94 (free base basis) |
| General description【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. |
| Biochem/physiol Actions【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 |
| Warning【警告】 | Toxicity: Standard Handling (A) |
| Reconstitution【重悬】 | Following reconstitution, aliquot and freeze (-70°C). Stock solutions are stable for up to 6 months at -70°C. |
| Other Notes【其他说明】 | Haddach, M., et al. 2012. ACS Med. Chem. Lett.3, 135. |
| Legal Information【法律信息】 | CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany |
产品性质
| Quality Level【质量水平】 | 100 |
| Assay【测定】 | ≥99% (HPLC) |
| form【形式】 | powder |
| manufacturer/tradename | Calbiochem® |
| storage condition【储存条件】 | OK to freeze desiccated (hygroscopic) protect from light |
| color【颜色】 | orange |
| solubility【溶解性】 | DMSO: 25 mg/mL |
| shipped in【运输】 | ambient |
| storage temp.【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] |
| packaging【包装】 | 10 mg in Glass bottle Packaged under inert gas |
安全信息
| Storage Class Code【储存分类代码】 | 11 - Combustible Solids |
| WGK | WGK 3 |
