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About This Item

经验公式(希尔记法):
C10H8N2OS
CAS Number:
分子量:
204.25
MDL编号:
UNSPSC代码:
12352200
PubChem化学物质编号:
NACRES:
NA.77
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方案

≥97% (HPLC)

质量水平

表单

solid

制造商/商品名称

Calbiochem®

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°C

SMILES字符串

C1=CC(=CN=C1)NC(=O)C2=CC=CS2

InChI

1S/C10H8N2OS/c13-10(9-4-2-6-14-9)12-8-3-1-5-11-7-8/h1-7H,(H,12,13)

InChI key

UPLHUDRMLWWFRE-UHFFFAOYSA-N

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.

生化/生理作用

Cell permeable: yes
Reversible: yes

包装

Packaged under inert gas

制备说明

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

免责声明

Toxicity: Standard Handling (A)

储存分类代码

11 - Combustible Solids

WGK

WGK 3

闪点(°F)

Not applicable

闪点(°C)

Not applicable


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