CX-6258 hydrochloride|cas:1353859-00-3|西域试剂

CX-6258 hydrochloride,99.28%

产品编号：Bellancom-18095B| CAS NO：1353859-00-3| 分子式：C₂₆H₂₅Cl₂N₃O₃| 分子量：498.40

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货号	价格	库存与货期
Bellancom-18095B	￥1000.00	杭州北京（现货）
Bellancom-18095B	￥1800.00	杭州北京（现货）
Bellancom-18095B	￥5400.00	杭州北京（现货）

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CX-6258 hydrochloride

产品介绍

CX-6258 hydrochloride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 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.

体外研究

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

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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
(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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

体内研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 10 mg/mL (20.06 mM; Need ultrasonic)

H₂O : 1 mg/mL (2.01 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0064 mL	10.0321 mL	20.0642 mL
5 mM	0.4013 mL	2.0064 mL	4.0128 mL
10 mM	0.2006 mL	1.0032 mL	2.0064 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 (sealed storage, away from moisture)。-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: ≥ 2.5 mg/mL (5.02 mM); Clear solution

此方案可获得 ≥ 2.5 mg/mL (5.02 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 25.0 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