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MilliporeSigma™ Calbiochem™ Bcr-abl Inhibitor IV, Imatinib

Catalog No. 5045950001 Shop All MilliporeSigma Products
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50-459-50001 50 mg
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Catalog No. 50-459-50001 Supplier MilliporeSigma™ Supplier No. 5045950001
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Description

A cell-permeable, orally bioavailable 2-phenylaminopyrimidine derived compound that competitively binds to ATP-binding site of Abl and stabilizes the inactive conformation, and acts as a highly potent and reversible inhibitor of Abl (IC50 = 38, 25 and 25nM for v-Abl, Bcr-Abl, and c-Abl, respective

A cell-permeable, orally bioavailable 2-phenylaminopyrimidine derived compound that competitively binds to ATP-binding site of Abl and stabilizes the inactive conformation, and acts as a highly potent and reversible inhibitor of Abl (IC50 = 38, 25 and 25nM for v-Abl, Bcr-Abl, and c-Abl, respectively). Also shown to block the activity of PDGFR and c-kit (IC50 = 50 and 100nM). Exhibits high selectivity over IR, IGF-1R, EGFR, c-Src, JAK-2, PKA, PKC isozymes, CKI, and CKII (IC50 >100μM). Preferentially blocks the proliferation of leukemic immature cobblestone-forming area cells and Bcr-abl transfected cell lines, M07/p210 and Ba/F3/p185 (∽1 -10μM), and suppresses tumor growth in mice (50mg/kg, i.p.). Induces apoptosis in Bcr-abl positive cells via intrinsic mitochondrial pathway by down-regulating Bcl-X, promoting cytochrome c release, and activating caspase-9. Does not affect the levels of Bcl-2. Also reported to induce a caspase-independent, necrosis-like programmed cell death mediated by the serine protease activity of Omi/HtrA2.
TRUSTED_SUSTAINABILITY

Specifications

Color White
Description 99% by HPLC
Target Proteins Abl
Solubility H2O
Content And Storage Hygroscopic, Protect from light
Form Solid
Quantity 50 mg
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