MilliporeSigma™ Calbiochem™ Bcr-abl Inhibitor IV, Imatinib

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 (IC 50 = 38, 25 and 25nM for v-Abl, Bcr-Abl, and c-Abl, respectively)
• Also shown to block the activity of PDGFR and c-kit (IC 50 = 50 and 100nM)
• Exhibits high selectivity over IR, IGF-1R, EGFR, c-Src, JAK-2, PKA, PKC isozymes, CKI, and CKII (IC 50 >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.