CX-6258

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白,专注于信号通路和疾病研究领域。

CX-6258  纯度: 99.73%

CX-6258是一种强效的、激酶选择性的 pan-Pim 激酶抑制剂,对 Pim-1, Pim-2 和 Pim-3 作用的 IC50 值分别为 5 nM、25 nM 和 16 nM。

CX-6258

CX-6258 Chemical Structure

CAS No. : 1202916-90-2

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ¥990 In-stock
5 mg ¥900 In-stock
10 mg ¥1440 In-stock
25 mg ¥2790 In-stock
50 mg ¥4500 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

CX-6258 相关产品

相关化合物库:

  • Bioactive Compound Library Plus
  • Epigenetics Compound Library
  • Immunology/Inflammation Compound Library
  • JAK/STAT Compound Library
  • Kinase Inhibitor Library
  • Anti-Cancer Compound Library
  • Orally Active Compound Library
  • Anti-Pancreatic Cancer Compound Library
  • Targeted Diversity Library

生物活性

CX-6258 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[1].

IC50 & Target

IC50: 5 nM (Pim-1), 25 nM (Pim-2), 16 nM (Pim-3)[1]

体外研究
(In Vitro)

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[1].
CX-6258 treatment (12 mM, 3 h) treatment diminishes steady-state levels of ectopic NKX3.1 in PC3 cells[2].
CX-6258 treatment results in a significant reduction in NKX3.1 half-life[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

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
(In Vivo)

CX-6258 (50-100 mg/kg; p.o; daily; over a period of 21 days) exhibits robust in vivo efficacy in two Pim kinases driven tumor models[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Nude mice, MV-4-11 xenograft models[1]
Dosage: 50 mg/kg, 100 mg/kg
Administration: Oral administration; once daily; over a period of 21 days
Result: Exhibited dose dependent efficacy, with a 50 mg/kg dose producing 45% tumor growth inhibition (TGI) and a 100 mg/kg dose producing 75% TGI.

分子量

461.94

Formula

C26H24ClN3O3

CAS 号

1202916-90-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 50 mg/mL (108.24 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.1648 mL 10.8239 mL 21.6478 mL
5 mM 0.4330 mL 2.1648 mL 4.3296 mL
10 mM 0.2165 mL 1.0824 mL 2.1648 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液,再依次添加助溶剂:

——为保证实验结果的可靠性,澄清的储备液可以根据储存条件,适当保存;体内实验的工作液,建议您现用现配,当天使用; 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比;如在配制过程中出现沉淀、析出现象,可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂: 10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.75 mg/mL (5.95 mM); Clear solution

    此方案可获得 ≥ 2.75 mg/mL (5.95 mM,饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例,取 100 μL 27.5 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中,混合均匀;向上述体系中加入50 μL Tween-80,混合均匀;然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH₂O 中,得到澄清透明的生理盐水溶液

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
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.

所有产品仅用作科学研究或药证申报,我们不为任何个人用途提供产品和服务