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。
| 生物活性 | CX-6258 is a potent and kinase selectivepan-Pim kinasesinhibitor, withIC50s 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].
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. |
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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].
| 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. |
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| 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 |
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| 溶解性数据 | In Vitro: DMSO : ≥ 50 mg/mL(108.24 mM) *"≥" means soluble, but saturation unknown. 配制储备液 | 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℃, 6 months; -20℃, 1 month。-80℃ 储存时，请在 6 个月内使用，-20℃ 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。 *以上所有助溶剂都可在本网站选购。
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