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| 品牌 | absin | CAS | 1353859-00-3 |
|---|---|---|---|
| 分子式 | C26H24ClN3O3.HCl | 纯度 | 98% |
| 分子量 | 498.40 | 货号 | abs47028267 |
| 规格 | 5mg | 供货周期 | 现货 |
| 主要用途 | is a potent, orally efficacious pan-Pim | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
CX-6258 hydrochloride 1353859-00-3
| 产品描述 | |
| 描述 | CX-6258 hydrochloride is a potent, orally efficacious pan-Pim kinase inhibitor with IC50 of 5 nM, 25 nM and 16 nM for Pim1, Pim2, and Pim3, respectively. |
| 纯度 | 98% |
| 储存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 可溶性/溶解性 | DMSO : 10 mg/mL (20.06 mM; Need ultrasonic) |
| 生物活性 | |
| 靶点 | Pim1；Pim3；Pim2 |
| In vitro(体外研究) | CX-6258 shows antiproliferative activity against a panel of human cancer cell lines with IC50 of 0.02-3.7 μM, mostly sensitive to acute leukemia cell lines. Combinations of CX-6258 with doxorubicin (10:1 molar ratio) and CX-6258 with paclitaxel (100:1 molar ratio) produces synergistic cell killing with combination index (CI50) values equal to 0.4 and 0.56, respectively. CX-6258 causes dose dependent inhibition of the phosphorylation of two pro-survival proteins, Bad and 4E-BP1, at the Pim kinase specific sites S112 and S65 and T37/46, respectively. |
| In vivo(体内研究) | CX-6258 exhibits dose dependent efficacy in suppressing tumor growth in mice carrying MV-4-11 xenografts, with a 50 mg/kg dose producing 45% tumor growth inhibition (TGI) and a 100 mg/kg dose producing 75% TGI |
| 研究领域 | |
| 研究领域 | CancerOncoproteins/suppressorsOncoproteinsSignal transducers CancerSignal transductionProtein phosphorylationSerine/threonine kinasesOther EpigeneticsChromatin RemodelingPolycomb SilencingOther NeuroscienceProcesses Signal TransductionProtein PhosphorylationSer / Thr KinasesOther Kinases Stem CellsHematopoietic ProgenitorsIntracellular Molecules Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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