T16872 |
CX-6258 hydrochloride |
| 源叶(MedMol) | 98% |
- 产品描述： CX-6258 hydrochloride is a potent and kinase selective pan-Pim kinases inhibitor, with IC50s of 5 nM, 25 nM and 16 nM for Pim-1, Pim-2 and Pim-3, respectively
- 靶点： IC50: 5 nM (Pim-1), 25 nM (Pim-2), 16 nM (Pim-3)
- 体外研究：
CX-6258 hydrochloride 分别在 Pim 激酶特异性位点 S112 和 S65 以及 T37/46 引起剂量依赖性抑制两种促存活蛋白 Bad 和 4E-BP1 的磷酸化。 CX-6258 hydrochloride 处理 (12 mM，3 小时) 处理降低了 PC3 细胞中异位 NKX3.1 的稳态水平。 CX-6258 hydrochloride 处理导致 NKX3.1 半衰期显著缩短。 Western Blot Analysis Cell Line: MV-4-11 human AML cells. Concentration: 0.1 μM, 1 μM, 10 μM. Incubation Time: 2 hours. Result: Caused 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.
- 体内研究：
CX-6258 hydrochloride (50-100 mg/kg；口服；每日一次；为期 21 天) 在两种 Pim 激酶驱动的肿瘤模型中表现出强大的体内功效。 Animal Model: Nude mice, MV-4-11 xenograft models Dosage: 50 mg/kg, 100 mg/kg. Administration: Oral administration; once daily; over a period of 21 days. Result: Exhibitd dose dependent efficacy, with a 50 mg/kg dose producing 45% tumor growth inhibition (TGI) and a 100 mg/kg dose producing 75% TGI.
- 参考文献：
1. Mustapha Haddach, Jerome Michaux, Michael K, Discovery of CX-6258. A Potent, Selective, and Orally Efficacious pan-Pim Kinases Inhibitor. ACS Med. Chem. Lett., 2012, 3 (2), pp 135-139. 2. Padmanabhan A, Gosc EB, Bieberich CJ. Stabilization of the prostate-specific tumor suppressor NKX3.1 by the oncogenic protein kinase Pim-1 in prostate cancer cells. J Cell Biochem. 2013 May;114(5):1050-7.
- 溶解性： Soluble in DMSO、H2O
- 保存条件： -20°C
- 配置溶液浓度参考：
1mg 5mg 10mg 1 mM 2.006 ml 10.032 ml 20.064 ml 5 mM 0.401 ml 2.006 ml 4.013 ml 10 mM 0.201 ml 1.003 ml 2.006 ml 50 mM 0.04 ml 0.201 ml 0.401 ml
- 注意：部分产品我司仅能提供部分信息，我司不保证所提供信息的权威性，仅供客户参考交流研究之用。
输入产品批号：
本计算器可帮助您计算出特定溶液中溶质的质量、溶液浓度和体积之间的关系，公式为：
质量 (mg) = 浓度 (mM) x 体积 (mL) x 分子量 (g/mol)
