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509226 | PI 3-K Inhibitor XXI, GDC-0941 - CAS 957054-30-7 - Calbiochem

509226
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₂₃H₂₇N₇O₃S₂ 957054-30-7

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      5.09226.0001
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          Glass bottle 10 mg
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          Description
          OverviewA cell-permeable thienopyrimidine compound that acts as a potent, ATP-competitive inhibitor against class IA (IC50 = 3 nM/p110α, 33 nM/p110β, 3 nM/p110δ) & IB (IC50 = 75 nM/p110γ) PI 3-K kinases, including the two known p110α hot spot mutants E454K & H1047R (IC50 = 3 nM), while exhibiting much reduced or little potency against more than 200 other kinases, including TrkA, class II C2β, class IV mTOR & DNA-PK (IC50 = 2.85, 0.67, 0.58, and 1.23 µM, respectively) and class III Vps34 (IC50 >10 µM). Effectively inhibits cellular Akt S473 phosphorylation (IC50 = 28 to 46 nM) as well as proliferation in cancer cultures in vitro (GI50 = 280 to 950 nM) and completely prevents the expansion of U87MG glioblastoma xenograft in mice in vivo (by 83%; 75 mg/kg/d p.o. for 21 days). Oral bioavailability is reported in human, dog, mouse, and rat.
          Catalogue Number509226
          Brand Family Calbiochem®
          SynonymsGDC0941, 2-(1H-Indazol-4-yl)-6-(4-methylsulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2- d]pyrimidine, 4-(2-(1H-Indazol-4-yl)-6-((4-(methylsulfonyl)piperazin-1-yl)methyl)thieno[3,2-d]pyrimidin-4-yl)morpholine
          References
          ReferencesTabe, Y., et al. 2014. Acta Haematol. 131, 59.
          Ware, J.A., et al. 2013. Mol. Pharm. 10, 4047.
          Junttila,.T., et al. 2009. Cancer Cell 15, 429.
          Raynaud, F.I., et al. 2009. Mol Cancer Ther. 8, 1725.
          Folkes, A. J., et al. 2008. J. Med. Chem. 51, 5522.
          Product Information
          CAS number957054-30-7
          FormWhite solid
          Hill FormulaC₂₃H₂₇N₇O₃S₂
          Chemical formulaC₂₃H₂₇N₇O₃S₂
          ReversibleY
          Structure formula Image
          Applications
          Biological Information
          Primary TargetPI 3-K
          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
          Do not freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
          Packaging Information
          Packaged under inert gas Packaged under inert gas
          Transport Information
          Supplemental Information
          Specifications

          Documentation

          References

          Reference overview
          Tabe, Y., et al. 2014. Acta Haematol. 131, 59.
          Ware, J.A., et al. 2013. Mol. Pharm. 10, 4047.
          Junttila,.T., et al. 2009. Cancer Cell 15, 429.
          Raynaud, F.I., et al. 2009. Mol Cancer Ther. 8, 1725.
          Folkes, A. J., et al. 2008. J. Med. Chem. 51, 5522.
          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.

          Revision14-February-2014 JSW
          SynonymsGDC0941, 2-(1H-Indazol-4-yl)-6-(4-methylsulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2- d]pyrimidine, 4-(2-(1H-Indazol-4-yl)-6-((4-(methylsulfonyl)piperazin-1-yl)methyl)thieno[3,2-d]pyrimidin-4-yl)morpholine
          DescriptionA cell-permeable thienopyrimidine compound that acts as a potent, ATP-competitive inhibitor against class IA (IC50 = 3 nM/p110α, 33 nM/p110β, 3 nM/p110δ) & IB (IC50 = 75 nM/p110γ) PI 3-K kinases, including the two known p110α hot spot mutants E454K & H1047R (IC50 = 3 nM), while exhibiting much reduced or little potency against more than 200 other kinases, including TrkA, class II C2β, class IV mTOR & DNA-PK (IC50 = 2.85, 0.67, 0.58, and 1.23 µM, respectively) and class III Vps34 (IC50 >10 µM). Effectively inhibits cellular Akt S473 phosphorylation (IC50 = 46 nM/U87MG, 37 nM/PC3, and 28 nM/MDA-MB-361) as well as proliferation in cancer cultures in vitro (GI50 = 950/U87MG, 280/PC3, and 720 nM/MDA-MB-361) and greatly prevents the expansion of U87MG glioblastoma xenograft in mice in vivo (by 83%; 75 mg/kg/d p.o. for 21 days). Oral bioavailability is reported in human, dog, mouse, and rat.
          FormWhite solid
          Intert gas (Yes/No) Packaged under inert gas
          CAS number957054-30-7
          Chemical formulaC₂₃H₂₇N₇O₃S₂
          Structure formula
          Purity≥99% by HPLC
          SolubilityDMSO (50 mg/ml). Use only fresh DMSO for reconstitution.
          Storage +2°C to +8°C
          Protect from light
          Do Not Freeze Ok to freeze
          Special InstructionsFollowing reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 6 months at -20°C.
          Toxicity Standard Handling
          ReferencesTabe, Y., et al. 2014. Acta Haematol. 131, 59.
          Ware, J.A., et al. 2013. Mol. Pharm. 10, 4047.
          Junttila,.T., et al. 2009. Cancer Cell 15, 429.
          Raynaud, F.I., et al. 2009. Mol Cancer Ther. 8, 1725.
          Folkes, A. J., et al. 2008. J. Med. Chem. 51, 5522.