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Merck
CN

197221

Sigma-Aldrich

Bcr-abl Inhibitor

The Bcr-abl Inhibitor, also referenced under CAS 778270-11-4, controls the biological activity of Bcr-abl. This small molecule/inhibitor is primarily used for Phosphorylation & Dephosphorylation applications.

Synonym(s):

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

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About This Item

Empirical Formula (Hill Notation):
C18H13F3N4O2
CAS Number:
778270-11-4
Molecular Weight:
374.32
MDL number:
MFCD09265253
UNSPSC Code:
12352200

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Quality Level

100

Assay

≥97% (HPLC)

form

solid

manufacturer/tradename

Calbiochem®

storage condition

OK to freeze
protect from light

color

white

solubility

DMSO: 10 mg/mL
ethanol: 2 mg/mL

shipped in

ambient

storage temp.

2-8°C

InChI

1S/C18H13F3N4O2/c19-18(20,21)27-14-6-4-13(5-7-14)25-16-9-15(23-10-24-16)11-2-1-3-12(8-11)17(22)26/h1-10H,(H2,22,26)(H,23,24,25)

InChI key

WEVYNIUIFUYDGI-UHFFFAOYSA-N

General description

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.

Biochem/physiol Actions

Cell permeable: yes
Primary Target
Bcr-abl-expressing cells in Ba/F3.p210
Product does not compete with ATP.
Reversible: yes
Target 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

Packaging

Packaged under inert gas

Preparation Note

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

Other Notes

Zhang, J., et al. 2010. Nature463, 501.
Choi, Y., et al. 2009. J. Biol. Chem.284, 29005.
Adrian, F.J., et al. 2006. Nat. Chem. Biol.2, 95.

Legal Information

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

Disclaimer

Toxicity: Irritant (B)

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Certificates of Analysis (COA)

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