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648451 Sigma-AldrichTrk Inhibitor III, GNF-5837 - CAS 1033769-28-6 - Calbiochem

The Trk Inhibitor III, GNF-5837 controls the biological activity of Trk. 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: (Z)-1-(3-((3-((1H-Pyrrol-2-yl)methylene)-2-oxoindolin-6-yl)amino)-4-methylphenyl)-3-(2-fluoro-5-(trifluoromethyl)phenyl)urea

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概述

Replacement Information

重要规格表

CAS #	Empirical Formula
1033769-28-6	C₂₈H₂₁F₄N₅O₂

价格及供货情况

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Description
Overview	An orally bioavailable oxindole compound that and acts as a potent, reversible and type II DFG-out inhibitor of pan-Trk activity (IC₅₀ = 8 and 12 nM for TrkA and TrkB). Shown to target Trk (tropomyosin receptor kinase) ATP binding cleft and an immediately adjacent hydrophobic pocket. Preferentially arrests the proliferation of Ba/F3 cells fused with Tel-TrkA, Tel-TrkB and Tel-TrkC (IC₅₀ = 11, 9 and 7 nM, respectively) and in Ba/F3 and RIE cells expressing both TrkA and NGF (IC₅₀ = 42 and 17 nM, respectively) over Mo7e-c-Kit and Rat-A10-PDGFR (IC₅₀ = 1 and 0.5 µM) and Ba/F3-Tel-KDR and wt-Ba/F3 cells (IC₅₀ = 3.0 and 5.6 µM). Displays ~100-fold greater selectivity among a panel of 59 closely related kinases and in 33 cellular kinase assays. Weakly active against relevant cytochrome P450 isozymes and hERG channel, and exhibit adequate microsomal stability, pharmacokinetic profile and efficacy in mice and rats. Suppresses tumor growth in a mouse RIE-TrkAmNGF xenograft model (50 mg/kg, p.o.).
Catalogue Number	648451
Brand Family	Calbiochem®
Synonyms	(Z)-1-(3-((3-((1H-Pyrrol-2-yl)methylene)-2-oxoindolin-6-yl)amino)-4-methylphenyl)-3-(2-fluoro-5-(trifluoromethyl)phenyl)urea

References
References	Albaugh, P., et al. 2012. ACS Med. Chem. Lett. 3, In press.

Product Information
CAS number	1033769-28-6
Form	Orange powder
Hill Formula	C₂₈H₂₁F₄N₅O₂
Chemical formula	C₂₈H₂₁F₄N₅O₂
Structure formula Image
Quality Level	MQ100

Applications

Biological Information
Purity	≥98% 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	Ambient Temperature Only
Toxicity	Standard Handling
Storage	+2°C to +8°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 at -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
648451-10MGCN	04055977262377

Documentation

Trk Inhibitor III, GNF-5837 - CAS 1033769-28-6 - Calbiochem MSDS

职位
物料安全数据表 (MSDS)

Trk Inhibitor III, GNF-5837 - CAS 1033769-28-6 - Calbiochem 分析证书

标题	批号
648451	输入批号

参考

参考信息概述
Albaugh, P., et al. 2012. ACS Med. Chem. Lett. 3, In press.

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	31-July-2013 JSW
Synonyms	(Z)-1-(3-((3-((1H-Pyrrol-2-yl)methylene)-2-oxoindolin-6-yl)amino)-4-methylphenyl)-3-(2-fluoro-5-(trifluoromethyl)phenyl)urea
Description	An orally bioavailable oxindole compound that and acts as a potent, reversible and type II DFG-out inhibitor of pan-Trk activity (IC₅₀ = 8 and 12 nM for TrkA and TrkB). Shown to target Trk (tropomyosin receptor kinase) ATP binding cleft and an immediately adjacent hydrophobic pocket. Preferentially arrests the proliferation of Ba/F3 cells fused with Tel-TrkA, Tel-TrkB and Tel-TrkC (IC₅₀ = 11, 9 and 7 nM, respectively) and in Ba/F3 and RIE cells expressing both TrkA and NGF (IC₅₀ = 42 and 17 nM, respectively) over Mo7e-c-Kit and Rat-A10-PDGFR (IC₅₀ = 1 and 0.5 µM) and Ba/F3-Tel-KDR and wt-Ba/F3 cells (IC₅₀ = 3.0 and 5.6 µM). Displays ~100-fold greater selectivity among a panel of 59 closely related kinases and in 33 cellular kinase assays. Weakly active against relevant cytochrome P450 isozymes and hERG channel, and exhibit adequate microsomal stability, pharmacokinetic profile and efficacy in mice and rats. Suppresses tumor growth in a mouse RIE-TrkAmNGF xenograft model (50 mg/kg, p.o.).
Form	Orange powder
Intert gas (Yes/No)	Packaged under inert gas
CAS number	1033769-28-6
Chemical formula	C₂₈H₂₁F₄N₅O₂
Structure formula
Purity	≥98% by HPLC
Solubility	DMSO (50 mg/ml)
Storage	Protect from light +2°C to +8°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 at -20°C.
Toxicity	Standard Handling
References	Albaugh, P., et al. 2012. ACS Med. Chem. Lett. 3, In press.

种类

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

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