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

504595
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₉H₃₁N₇O • CH₃SO₃H 220127-57-1

      Pricing & Availability

      Catalog NumberAvailability Packaging Qty/Pack Price Quantity
      5.04595.0001
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          Glass bottle 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®
          SynonymsSTI571, 4-((4-Methyl-1-piperazinyl)methyl)-N-(4-methyl-3-((4-(3-pyridinyl)-2-pyrimidinyl)amino)phenyl)benzamide, Methanesulfonate, Abl Inhibitor V, PDGFR Tyrosine Kinase Inhibitor XXIV, c-Kit Inhibitor IV
          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 Image
          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

          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
          SynonymsSTI571, 4-((4-Methyl-1-piperazinyl)methyl)-N-(4-methyl-3-((4-(3-pyridinyl)-2-pyrimidinyl)amino)phenyl)benzamide, Methanesulfonate, Abl Inhibitor V, PDGFR Tyrosine Kinase Inhibitor XXIV, c-Kit Inhibitor IV
          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 formula
          Purity≥99% by HPLC
          SolubilityH₂O (100 mg/ml)
          Storage +2°C to +8°C
          Protect from light
          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.
          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.