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504595 Bcr-abl Inhibitor IV, Imatinib - CAS 220127-57-1 - Calbiochem

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Key Spec Table

CAS #Empirical Formula
220127-57-1C₂₉H₃₁N₇O • CH₃SO₃H

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      Glasflasche 50 mg
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      Description
      OverviewA 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 25 nM for v-Abl, Bcr-Abl, and c-Abl, respectively). Also shown to block the activity of PDGFR and c-kit (IC50 = 50 and 100 nM). Exhibits high selectivity over IR, IGF-1R, EGFR, c-Src, JAK-2, PKA, PKC isozymes, CKI, and CKII (IC50 >100 µM). Preferentially blocks the proliferation of leukemic immature cobblestone-forming area cells and Bcr-abl transfected cell lines, M07/p210 and Ba/F3/p185 (~1 -10 µM), and suppresses tumor growth in mice (50 mg/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.
      Catalogue Number504595
      Brand Family Calbiochem®
      SynonymsAbl Inhibitor V, PDGFR Tyrosine Kinase Inhibitor XXIV, c-Kit Inhibitor IV, 4-((4-Methyl-1-piperazinyl)methyl)-N-(4-methyl-3-((4-(3-pyridinyl)-2-pyrimidinyl)amino)phenyl)benzamide, Methanesulfonate, STI571
      References
      ReferencesLin, Y.L., et al. 2013. Proc. Natl. acad. Sci. USA 110, 1664.
      Okada, M., et al. 2004. Blood 103, 2299.
      Capdeville, R., et al. 2002. Nat. Rev. Drug. Res. 1, 493.
      Oetzel, C., et al. 2000. Clin Cancer Res. 6, 1958.
      Schindler, T., et al. 2000. Science 289, 1938.
      Buchdunger, E., et al. 2000. J. Pharmacol. Exp. Ther. 295, 139.
      Carroll. M., et al. 1997. Blood 90, 4947.
      Zimmermann, J., et al. 1997. Bioorg. Med. Chem. Lett. 7, 187.
      Druker, B.J., et al. 1996. Nat. Med. 2, 561.
      Product Information
      CAS number220127-57-1
      FormWhite solid
      Hill FormulaC₂₉H₃₁N₇O • CH₃SO₃H
      Hygroscopic Hygroscopic
      ReversibleY
      Structure formula ImageStructure formula Image
      Quality LevelMQ100
      Biological Information
      Primary TargetAbl
      Secondary targetPDGFR, c-kit
      Purity≥99% by HPLC
      Physicochemical Information
      Cell permeableY
      Storage and Shipping Information
      Ship Code Ambient Temperature Only
      Toxicity Standard Handling
      Storage +2°C to +8°C
      Protect from Light Protect from light
      Hygroscopic Hygroscopic
      Do not freeze Ok to freeze
      Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Global Trade Item Number
      Bestellnummer GTIN
      5.04595.0001 04055977243901