532384 PI3K Inhibitor, HS-173 - Calbiochem

532384
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Overview

Replacement Information

Key Specifications Table

Empirical FormulaCAS #
C₂₁H₁₈N₄O₄S 1276110-06-5

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      Glass bottle 10 mg
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      Description
      OverviewA cell permeable imidazopyridine-carboxylate derived compound that acts as a potent and selective inhibitor of phosphatidylinositol 3-kinase a (PI3Ka; IC50 = 800 pM). Blocks the proliferation of several cancer cells (IC50 = 600 nM; 1.5 µM, and 7.8 µM for T47D, SK-BR3, and MCF-7 cells, respectively). Suppresses the growth and proliferation of hepatic stellate cells (HSC-T6 and LX-2 cells) and induces cell cycle arrest at G2/M phase in a dose and time-dependent manner. Induces apoptosis in HSC-T6 cells (~5 µM) as evidenced by morphological changes, activation of caspase-3, reduction in Bcl-2 levels, and loss of mitochondrial transmembrane potential. Exhibits anti-fibrolytic activity and diminishes the expression of profibrotic mediators, such as fibronectin and vimentin (~ 1 µM) and weakens the severity of hepatic damage in a murine model of carbon tetrachloride-induced fibrosis and reduces the phosphorylation of Akt and p70S6 kinase (10 mg/kg, p.o., 6d/week for 1 month).

      Please note that the molecular weight for this compound is batch-specific due to variable water content.
      Catalogue Number532384
      Brand Family Calbiochem®
      SynonymsPI3Kα Inhibitor, Phosphatidylinositol 3-kinase α Inhibitor
      References
      ReferencesSon, M.K., et al. 2013. Sci. Rep. 3, 3470.
      Lee, H., et al. 2013. Onc. Rep. 30, 863.
      Kim, O., et al. 2011. J. Med. Chem. 54, 2455.
      Product Information
      CAS number1276110-06-5
      FormLight beige powder
      Hill FormulaC₂₁H₁₈N₄O₄S
      Chemical formulaC₂₁H₁₈N₄O₄S
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary TargetPI3Ka
      Primary Target IC<sub>50</sub>800 pM
      Purity≥96% 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 Shipped at Ambient Temperature or with Blue Ice or with Dry Ice
      Toxicity Standard Handling
      Storage -20°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 3 months at -20°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      PI3K Inhibitor, HS-173 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Son, M.K., et al. 2013. Sci. Rep. 3, 3470.
      Lee, H., et al. 2013. Onc. Rep. 30, 863.
      Kim, O., et al. 2011. J. Med. Chem. 54, 2455.

      Technical Info

      Title
      White Paper: Further considerations of antibody validation and usage. (EMD)
      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.

      Revision27-February-2015 JSW
      SynonymsPI3Kα Inhibitor, Phosphatidylinositol 3-kinase α Inhibitor
      DescriptionA cell permeable imidazopyridine-carboxylate derived compound that acts as a potent and selective inhibitor of phosphatidylinositol 3-kinase a (PI3Ka; IC50 = 800 pM). Blocks the proliferation of several cancer cells (IC50 = 600 nM; 1.5 µM, and 7.8 µM for T47D, SK-BR3, and MCF-7 cells, respectively). Suppresses the growth and proliferation of hepatic stellate cells (HSC-T6 and LX-2 cells) and induces cell cycle arrest at G2/M phase in a dose and time-dependent manner. Induces apoptosis in HSC-T6 cells (~5 µM) as evidenced by morphological changes, activation of caspase-3, reduction in Bcl-2 levels, and loss of mitochondrial transmembrane potential. Exhibits anti-fibrolytic activity and diminishes the expression of profibrotic mediators, such as fibronectin and vimentin (~ 1 µM) and weakens the severity of hepatic damage in a murine model of carbon tetrachloride-induced fibrosis and reduces the phosphorylation of Akt and p70S6 kinase (10 mg/kg, p.o., 6d/week for 1 month).
      FormLight beige powder
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1276110-06-5
      Chemical formulaC₂₁H₁₈N₄O₄S
      Purity≥96% by HPLC
      SolubilityDMSO (50 mg/ml)
      Storage -20°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 3 months at -20°C.
      Toxicity Standard Handling
      ReferencesSon, M.K., et al. 2013. Sci. Rep. 3, 3470.
      Lee, H., et al. 2013. Onc. Rep. 30, 863.
      Kim, O., et al. 2011. J. Med. Chem. 54, 2455.