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MPNST Inhibitor, Cpd21-Calbiochem

品牌
Sigma-Aldrich
货号
5.31126
规格纯度
A cell-permeable. Reversible, selective inhibitor of the growth of malignant peripheral nerve sheath tumors (EC50 = 439 nM, 754 nM, and 1.0 μM in S462, SNF96.2, and sMPNST cells).
参考价格
2394.05 *本价格含增值税费
促销
服务
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  • 包邮
  • 增值税票
数量
-+
产品名称:
MPNST Inhibitor, Cpd21-Calbiochem
N-(Pyridin-3-yl)thiophene-2-carboxamide, Malignant Peripheral Nerve Sheath Tumors Inhibitor, Cpd 21
产品介绍:

产品说明

一般描述

A cell-permeable, bioavailable, non-toxic pyridinylthiophene-carboxamide compound that preferentially and reversibly inhibits the growth of malignant peripheral nerve sheath tumors (MPNSTs) in both human and murine models in a dose-dependent manner (EC50 = 439 nM, 754 nM, and 1.0 µM in S462, SNF96.2, and sMPNST cells). Exhibits toxicity towards neurofibromatosis type 1 (Nf1) and p53 deficient MPNST cells, but does not affect normally dividing Schwann cells and mouse embryonic fibroblasts. Shown to reduce ATP consumption by all MPNST cells studied (EC50 = 1.0 µM). Synergizes with PI-3 Kinase inhibitor, LY-294002 (Cat. Nos. 440202 & 440204) to block the growth of MPNST cells. Reduces the expression of cyclin A2, B1, D1, E, cdk4, and cdk6 and increases the expression of cdkn1a and cdkn2a in a dose dependent manner. Blocks cell cycle at G1/S phase leading to apoptosis in cancer cells. Displays favorable pharmacokinetic profile and is rapidly distributed from the plasma into sMPNST tissues and has a half-life of 6-8 hours in sMPNST tissue following its complete distribution. Reduces MPNST burden in a mouse allograft model and enhances survival (~40 mg/kg, i.p. in mice for 4 weeks).

Please note that the molecular weight for this compound is batch-specific due to variable water content.
A cell-permeable, bioavailable, non-toxic pyridinylthiophene-carboxamide compound that preferentially and reversibly inhibits the growth of malignant peripheral nerve sheath tumors (MPNSTs) in both human and murine models in a dose-dependent manner (EC50 = 439 nM, 754 nM, and 1.0 µM in S462, SNF96.2, and sMPNST cells). Exhibits toxicity towards neurofibromatosis type 1 (Nf1) and p53 deficient MPNST cells, but does not affect normally dividing Schwann cells and mouse embryonic fibroblasts. Shown to reduce ATP consumption by all MPNST cells studied (EC50 = 1.0 µM). Synergizes with PI-3 Kinase inhibitor, LY-294002 (Cat. Nos. 440202 & 440204) to block the growth of MPNST cells. Reduces the expression of cyclin A2, B1, D1, E, cdk4, and cdk6 and increases the expression of cdkn1a and cdkn2a in a dose dependent manner. Blocks cell cycle at G1/S phase leading to apoptosis in cancer cells. Displays favorable pharmacokinetic profile and is rapidly distributed from the plasma into sMPNST tissues and has a half-life of 6-8 hours in sMPNST tissue following its complete distribution. Reduces MPNST burden in a mouse allograft model and enhances survival (~40 mg/kg, i.p. in mice for 4 weeks).

生化/生理作用

Cell permeable: yes
Reversible: yes

包装

Packaged under inert gas

警告

Toxicity: Standard Handling (A)

重悬

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.

其他说明

Chau, V., et al. 2013. Cancer Res. 74, 586.

法律信息

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

基本信息

经验(实验)分子式C10H8N2OS
分子量204.25

产品性质

质量水平100
测定≥97% (HPLC)
形式solid
manufacturer/tradenameCalbiochem®
储存条件OK to freeze
protect from light
颜色light beige
溶解性DMSO: 100 mg/mL
储存温度2-8℃

安全信息

储存分类代码11 - Combustible Solids
WGKWGK 3
闪点(F)Not applicable
闪点(C)Not applicable

Sigma-Aldrich

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