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

A cell-permeable, potent, ATP-competitive inhibitor of class IA (IC₅₀ = 3 nM/p110α, 33 nM/p110&beta, 3 nM/p110δ) and IB PI 3-kinases (IC₅₀ = 75 nM/p110γ).

MSDS (material safety data sheet) or SDS, CoA and CoQ, dossiers, brochures and other available documents.

Synonyms: GDC0941, 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

Primary Target: PI 3-K
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509226
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Overview

Replacement Information

Key Specifications Table

CAS #Empirical Formula
957054-30-7C₂₃H₂₇N₇O₃S₂

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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 ImageStructure formula Image
      Quality LevelMQ100
      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
      Global Trade Item Number
      Catalog Number GTIN
      5.09226.0001 04055977241693

      Documentation

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

      Title

      Safety Data Sheet (SDS) 

      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 formulaStructure formula
      Purity≥99% by HPLC
      SolubilityDMSO (50 mg/ml). Use only fresh DMSO for reconstitution.
      Storage Protect from light
      +2°C to +8°C
      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.