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

504595
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Empirical FormulaCAS #
C₂₉H₃₁N₇O • CH₃SO₃H 220127-57-1

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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, STI571, 4-((4-Methyl-1-piperazinyl)methyl)-N-(4-methyl-3-((4-(3-pyridinyl)-2-pyrimidinyl)amino)phenyl)benzamide, Methanesulfonate
      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
      Applications
      Biological Information
      Primary TargetAbl
      Secondary targetPDGFR, c-kit
      Purity≥99% 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 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
      Transport Information
      Supplemental Information
      Specifications

      Documentation

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

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Lin, 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.
      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.

      Revision01-July-2013 JSW
      SynonymsAbl Inhibitor V, PDGFR Tyrosine Kinase Inhibitor XXIV, c-Kit Inhibitor IV, STI571, 4-((4-Methyl-1-piperazinyl)methyl)-N-(4-methyl-3-((4-(3-pyridinyl)-2-pyrimidinyl)amino)phenyl)benzamide, Methanesulfonate
      DescriptionA 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.
      FormWhite solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number220127-57-1
      Structure formulaStructure formula
      Purity≥99% by HPLC
      SolubilityH₂O (100 mg/ml)
      Storage +2°C to +8°C
      Hygroscopic
      Protect from light
      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.
      Toxicity Standard Handling
      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.