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448106 Sigma-AldrichMet Kinase Inhibitor VI, SGX523 - CAS 1022150-57-7 - Calbiochem

The Met Kinase Inhibitor VI, SGX523, also referenced under CAS 1022150-57-7, controls the biological activity of Met Kinase. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

MSDS
分析证书
参考
Data Sheet

同义词: 6-(6-(1-Methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-ylthio)quinoline, SGX523

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概述

Replacement Information

重要规格表

CAS #	Empirical Formula
1022150-57-7	C₁₈H₁₃N₇S

价格及供货情况

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Description
Overview	A cell-permeable triazolopyridazine compound that acts as a potent, ATP-competitive (K_i = 2.7 & 23 nM using non-phosphorylated and phosphorylated MET kinase domain, respectively), and highly selective inhibitor against the tyrosine kinase activity of the HGF (hepatocyte growth factor) receptor c-MET (IC₅₀ = 4 nM), while exhibiting little or no activity toward a panel of more than 210 other kinases, including the closely related RTK RON. Shown to inhibit the constitutive (IC₅₀ = 40 nM in GTL16 cells) as well as HGF-stimulated (IC₅₀ = 12 nM in A549 cells) MET autophosphorylation/activation in cultures in vitro and effectively suppress MET-dependent tumor growths in mice in vivo (twice daily oral dosings at 30 mg/kg). X-ray crystallography reveals that SGX523 locks MET in a "DFG-in" conformation with the triazolopyridazine moiety interacting with the hydrophobic side chains of Met¹²²⁹ and Tyr¹²⁴⁸, while Tyr¹²⁴⁸ mutations are found to render MET insensitive to SGX523 inhibition both in cell-free and cell-based assays.
Catalogue Number	448106
Brand Family	Calbiochem®
Synonyms	6-(6-(1-Methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-ylthio)quinoline, SGX523

References
References	Buchanan, S.G., et al. 2009. Mol. Cancer Ther. 8, 3181. Eder, J.P., et al. 2009. Clin. Cancer Res. 15, 2207.

Product Information
CAS number	1022150-57-7
Form	Tan powder
Hill Formula	C₁₈H₁₃N₇S
Chemical formula	C₁₈H₁₃N₇S
Structure formula Image
Quality Level	MQ100

Applications

Biological Information
Purity	≥97% by HPLC

Physicochemical Information

Dimensions

Materials Information

Toxicological Information

Safety Information according to GHS

Safety Information

Product Usage Statements

Storage and Shipping Information
Ship Code	Shipped with Blue Ice or with Dry Ice
Toxicity	Regulatory Review
Storage	-20°C
Protect from Light	Protect from light
Do not freeze	Ok to freeze
Special Instructions	Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months -20°C.

Packaging Information
Packaged under inert gas	Packaged under inert gas

Transport Information

Supplemental Information

Specifications

Global Trade Item Number
产品目录编号	GTIN
448106-5MGCN	04055977204681

Documentation

Met Kinase Inhibitor VI, SGX523 - CAS 1022150-57-7 - Calbiochem MSDS

职位
物料安全数据表 (MSDS)

Met Kinase Inhibitor VI, SGX523 - CAS 1022150-57-7 - Calbiochem 分析证书

标题	批号
448106	输入批号

参考

参考信息概述
Buchanan, S.G., et al. 2009. Mol. Cancer Ther. 8, 3181. Eder, J.P., et al. 2009. Clin. Cancer Res. 15, 2207.

数据表

Note that this data sheet is not lot-specific and is representative of the current specifications for this product. Please consult the vial label and the certificate of analysis for information on specific lots. Also note that shipping conditions may differ from storage conditions.

Revision	24-October-2011 RFH
Synonyms	6-(6-(1-Methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-b]pyridazin-3-ylthio)quinoline, SGX523
Description	A cell-permeable triazolopyridazine compound that acts as a potent, ATP-competitive (K_i = 2.7 & 23 nM using non-phosphorylated and phosphorylated MET kinase domain, respectively), and highly selective inhibitor against the tyrosine kinase activity of the HGF (hepatocyte growth factor) receptor c-MET (IC₅₀ = 4 nM), while exhibiting little or no activity toward a panel of more than 210 other kinases, including the closely related RTK RON. Shown to inhibit the constitutive (IC₅₀ = 40 nM in GTL16 cells) as well as HGF-stimulated (IC₅₀ = 12 nM in A549 cells) MET autophosphorylation/activation in cultures in vitro and effectively suppress MET-dependent tumor growths in mice in vivo (twice daily oral dosings at 30 mg/kg). X-ray crystallography reveals that SGX523 locks MET in a "DFG-in" conformation with the triazolopyridazine moiety interacting with the hydrophobic side chains of Met¹²²⁹ and Tyr¹²⁴⁸, while Tyr¹²⁴⁸ mutations are found to render MET insensitive to SGX523 inhibition both in cell-free and cell-based assays.
Form	Tan powder
Intert gas (Yes/No)	Packaged under inert gas
CAS number	1022150-57-7
Chemical formula	C₁₈H₁₃N₇S
Structure formula
Purity	≥97% by HPLC
Solubility	DMSO (2.5 mg/ml)
Storage	Protect from light -20°C
Do Not Freeze	Ok to freeze
Special Instructions	Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months -20°C.
Toxicity	Regulatory Review
References	Buchanan, S.G., et al. 2009. Mol. Cancer Ther. 8, 3181. Eder, J.P., et al. 2009. Clin. Cancer Res. 15, 2207.

种类

Life Science Research > Inhibitors and Biochemicals > Small Molecules & Inhibitors > Protein Phosphorylation / Dephosphorylation > Protein Tyrosine Kinase (PTK) Inhibitors

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