CGP 57380 是一种细胞渗透的吡唑-嘧啶类化合物，为具有选择性的 Mnk1 抑制剂

价格： ￥1376

品牌：medchemexpress(MCE)

货号：HY-10520

产品详情

CGP 57380

CGP 57380 是一种细胞渗透的吡唑-嘧啶类化合物，为具有选择性的 Mnk1 抑制剂，IC₅₀ 值为 2.2 μM，但是对 p38，JNK1，ERK1/2，PKC 或 Src-like 激酶等没有抑制作用。

美国medchemexpress（MCE)浙江省一级代理:杭州昊鑫生物科技股份有限公司
MCE中国是全球领先的科研化学品和生物活性化合物供应商，总部位于美国新泽西。我们的产品范围覆盖各种抑制剂、激动剂、API和化合物库。专业、高效的企业灵魂铸造了在行业的卓越地位。热情和充满活力的研发团队拥有着大量的化学和生物科学家。专注于生物活性化合物，拥有着多年的发展历程和丰富的行业经验。从产品的HNMR数据解析到生物活性数据，从客户的询价到产品的售后服务，我们拥有着完善的管理体系，从而保证我们的服务更加高效、准确。努力为中国的医药行业发展注入新的活力，我们将成为您研发工作值得信赖的伙伴。

生物活性

CGP 57380 is a cell-permeable pyrazolo-pyrimidine compound that acts as a selective inhibitor of Mnk1 with IC₅₀ of 2.2 μM, but has no inhibitory activity against p38, JNK1, ERK1/2, PKC, or Src-like kinases.

IC₅₀ & Target^[1]

MNK1

2.2 μM (IC₅₀)

体外研究 (In Vitro)	CGP57380 inhibits phosphorylation of eIF4E in cellular assays with IC₅₀ of about 3 μM. CGP57380 causes dephosphorylation of eIF4E, and induces a further increase in the cap-dependent reporter in 293 cells^[1]. CGP57380 results in dose-dependent decreases in Ang II-stimulated phosphorylation of eIF4E, protein synthesis, and VSMC hypertrophy^[2]. CGP57380 sensitizes wild-type cells for serum-withdrawal induced apoptosis in mouse embryo fibroblasts (MEFs)^[3]. CGP57380 prevents the serial replating function of BC progenitors^[4].

体外研究
(In Vitro)

CGP57380 inhibits phosphorylation of eIF4E in cellular assays with IC₅₀ of about 3 μM. CGP57380 causes dephosphorylation of eIF4E, and induces a further increase in the cap-dependent reporter in 293 cells^[1]. CGP57380 results in dose-dependent decreases in Ang II-stimulated phosphorylation of eIF4E, protein synthesis, and VSMC hypertrophy^[2]. CGP57380 sensitizes wild-type cells for serum-withdrawal induced apoptosis in mouse embryo fibroblasts (MEFs)^[3]. CGP57380 prevents the serial replating function of BC progenitors^[4].

体内研究 (In Vivo)	CGP57380 (40 mg/kg/d i.p.) potently extinguishes the ability of BC CML cells to serially transplant-immunodeficient mice and function as LSCs^[4].

分子量

244.23

性状

Solid

Formula

C₁₁H₉FN₆

CAS 号

522629-08-9

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 : 6 mg/mL (24.57 mM; Need ultrasonic and warming)

H₂O : < 0.1 mg/mL (ultrasonic;warming;heat to 60°C) (insoluble)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	4.0945 mL	20.4725 mL	40.9450 mL
5 mM	0.8189 mL	4.0945 mL	8.1890 mL
10 mM	0.4095 mL	2.0473 mL	4.0945 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: ≥ 2.5 mg/mL (10.24 mM); Clear solution
2.
请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in saline)

Solubility: ≥ 2.5 mg/mL (10.24 mM); Clear solution

参考文献	[1]. Knauf U, et al. Negative regulation of protein translation by mitogen-activated protein kinase-interacting kinases 1 and 2. Mol Cell Biol. 2001 Aug;21(16):5500-11. [Content Brief] [2]. Ishida M, et al. Mnk1 is required for angiotensin II-induced protein synthesis in vascular smooth muscle cells. Circ Res. 2003 Dec 12;93(12):1218-24. Epub 2003 Nov 6 [Content Brief] [3]. Chrestensen CA, et al. Loss of MNK function sensitizes fibroblasts to serum-withdrawal induced apoptosis. Genes Cells. 2007 Oct;12(10):1133-40. [Content Brief] [4]. Lim S, et al. Targeting of the MNK-eIF4E axis in blast crisis chronic myeloid leukemia inhibits leukemia stem cell function. Proc Natl Acad Sci U S A. 2013 Jun 18;110(25):E2298-307 [Content Brief]

参考文献