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197221 Bcr-abl Inhibitor - CAS 778270-11-4 - Calbiochem

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

Synonyms: (3-(6)-(4-Trifluoromethoxy-phenylamino)-pyrimidin-4-yl)-benzamide, GNF-2, Abl Inhibitor I

Primary Target: Bcr-abl-expressing cells in Ba/F3.p210
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
778270-11-4C₁₈H₁₃F₃N₄O₂
Description
Overview

This product has been discontinued.



A cell-permeable and reverisble pyrimidine compound that binds to the c-abl myristoyl binding pocket and acts as an allosteric, non-ATP-competitive inhibitor of cellular Bcr-abl activity and Bcr-abl-dependent cellular functions. Exhibits little inhibitory effect against a panel of 63 kinases even at concentration as high as 10 µM. Exhibits potent and selective antiproliferative activity toward Bcr-abl-expressing cells (IC50 = 138 nM, 194 nM, 268 nM and 273 nM in Ba/F3.p210, Ba/F3.p185Y253H, SUP-B15 and Ba/F3.p210E255V, and K562, respectively). Brij-35 is reported to mask the inhibitory effect of GNF-2 in cell-free c-abl and Bcr-abl kinase assays.
Catalogue Number197221
Brand Family Calbiochem®
Synonyms(3-(6)-(4-Trifluoromethoxy-phenylamino)-pyrimidin-4-yl)-benzamide, GNF-2, Abl Inhibitor I
References
ReferencesZhang, J., et al. 2010. Nature 463, 501.
Choi, Y., et al. 2009. J. Biol. Chem. 284, 29005.
Adrian, F.J., et al. 2006. Nat. Chem. Biol. 2, 95.
Product Information
CAS number778270-11-4
ATP CompetitiveN
FormWhite solid
Hill FormulaC₁₈H₁₃F₃N₄O₂
Chemical formulaC₁₈H₁₃F₃N₄O₂
ReversibleY
Structure formula ImageStructure formula Image
Quality LevelMQ100
Applications
Biological Information
Primary TargetBcr-abl-expressing cells in Ba/F3.p210
Primary Target IC<sub>50</sub>138 nM, 194 nM, 268 nM and 273 nM in Ba/F3.p210, Ba/F3.p185Y253H, SUP-B15 and Ba/F3.p210E255V, and K562, respectively
Purity≥97% by HPLC
Physicochemical Information
Cell permeableY
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 Irritant
Storage +2°C to +8°C
Protect from Light Protect from light
Do not freeze Ok to freeze
Special InstructionsFollowing 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
Catalogue Number GTIN
197221 0

Documentation

Bcr-abl Inhibitor - CAS 778270-11-4 - Calbiochem SDS

Title

Safety Data Sheet (SDS) 

Bcr-abl Inhibitor - CAS 778270-11-4 - Calbiochem Certificates of Analysis

TitleLot Number
197221

References

Reference overview
Zhang, J., et al. 2010. Nature 463, 501.
Choi, Y., et al. 2009. J. Biol. Chem. 284, 29005.
Adrian, F.J., et al. 2006. Nat. Chem. Biol. 2, 95.
Data Sheet

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.

Revision25-March-2010 RFH
Synonyms(3-(6)-(4-Trifluoromethoxy-phenylamino)-pyrimidin-4-yl)-benzamide, GNF-2, Abl Inhibitor I
DescriptionA cell-permeable and reverisble pyrimidine compound that binds to the c-abl myristoyl binding pocket and acts as an allosteric, non-ATP-competitive inhibitor of cellular Bcr-abl activity and Bcr-abl-dependent cellular functions. Exhibits little inhibitory effect against a panel of 63 kinases even at concentration as high as 10 µM. Exhibits potent and selective antiproliferative activity toward Bcr-abl-expressing cells (IC50 = 138 nM, 194 nM, 268 nM and 273 nM in Ba/F3.p210, Ba/F3.p185Y253H, SUP-B15 and Ba/F3.p210E255V, and K562, respectively). Brij-35 is reported to mask the inhibitory effect of GNF-2 in cell-free c-abl and Bcr-abl kinase assays.
FormWhite solid
Intert gas (Yes/No) Packaged under inert gas
CAS number778270-11-4
Chemical formulaC₁₈H₁₃F₃N₄O₂
Structure formulaStructure formula
Purity≥97% by HPLC
SolubilityDMSO (10 mg/ml) or Ethanol (2 mg/ml)
Storage Protect from light
+2°C to +8°C
Do Not Freeze Ok to freeze
Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
Toxicity Irritant
ReferencesZhang, J., et al. 2010. Nature 463, 501.
Choi, Y., et al. 2009. J. Biol. Chem. 284, 29005.
Adrian, F.J., et al. 2006. Nat. Chem. Biol. 2, 95.