533637 PI 3-Kα Inhibitor XXIV, A66 - CAS 1166227-08-2 - Calbiochem

533637
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Empirical FormulaCAS #
C₁₇H₂₃N₅O₂S₂ 1166227-08-2

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      Description
      OverviewA cell-permeable, bioavailable aminothiazole compound that acts as a potent, selective, reversible, and ATP-competitive inhibitor of both wild-type and oncogenic forms of PI 3-K isoform p110α (IC50 = 32, 30 and 43 nM for p110α, p110αE545K and p110H1047R, respectively). Does not affect the activity of p110β, p110δ & p110γ (IC50 = 12.5, 1.25, and 3.4 µM, respectively). Exhibits greater selectivity over other PI 3-Ks (IC50 = 5.0, 0.462, 5.0, 5.0, 5.0, 5.0, and 0.236 µM for PI 3-KC2α, PI 3-KC2β, PI 3-K class-III, mTOR, DNA-PK, PI 4-Kα and PI 4-Kβ, respectively) and 318 other protein kinases. Displays greater selectivity than PIK-75 (Cat. No. 528116) and reduces Akt and p70S6 kinase phosphorylation. Shown to retard the growth of SK-OV-3 and HCT-116 xenografted tumors in mice (75 mg/kg, i.p, q.d). Exhibits desirable pharmacokinetic properties (Tmax = 30 min; t1/2= 0.42 h; Cmax: 8.247 µM; and AUC0-inf = 6.8 µM/h; at 10 mg/kg). Also, reported to increase plasma insulin levels and enhance production of glucose from pyruvate in CD1 mice (10 mg/kg, i.p.).

      Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.
      Catalogue Number533637
      Brand Family Calbiochem®
      SynonymsA-66, (S)-form
      References
      ReferencesHoland, K., et al. 2014. PLoS ONE. 9, e94132.
      Smith, G.C., et al. 2012. Biochem. J., 442, 161.
      Jamieson, S., et al. 2011. Biochem. J., 438, 53.
      Waardenberg, A.J., et al. 2011. J. Biol. Chem. 286, 30837.
      Sun, M., et al. 2010. Proc. Natl. Acad. Sci. USA. 35, 15547.
      Product Information
      CAS number1166227-08-2
      FormWhite solid
      Hill FormulaC₁₇H₂₃N₅O₂S₂
      Chemical formulaC₁₇H₂₃N₅O₂S₂
      ReversibleY
      Quality LevelMQ100
      Applications
      Biological Information
      Primary Targetwild-type and oncogenic forms of PI 3-K isoform p110α
      Primary Target IC<sub>50</sub>32, 30 and 43 nM for p110&alpha
      Purity≥98% 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 3 months at -20-°C.
      Packaging Information
      Packaged under inert gas Packaged under inert gas
      Transport Information
      Supplemental Information
      Specifications

      Documentation

      PI 3-Kα Inhibitor XXIV, A66 - CAS 1166227-08-2 - Calbiochem SDS

      Title

      Safety Data Sheet (SDS) 

      References

      Reference overview
      Holand, K., et al. 2014. PLoS ONE. 9, e94132.
      Smith, G.C., et al. 2012. Biochem. J., 442, 161.
      Jamieson, S., et al. 2011. Biochem. J., 438, 53.
      Waardenberg, A.J., et al. 2011. J. Biol. Chem. 286, 30837.
      Sun, M., et al. 2010. Proc. Natl. Acad. Sci. USA. 35, 15547.
      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.

      Revision20-November-2015 JSW
      SynonymsA-66, (S)-form
      DescriptionA cell-permeable, bioavailable aminothiazole compound that acts as a potent, selective, reversible, and ATP-competitive inhibitor of both wild-type and oncogenic forms of PI 3-K isoform p110α (IC50 = 32, 30 and 43 nM for p110α, p110αE545K and p110H1047R, respectively). Does not affect the activity of p110β, p110δ & p110γ (IC50 = 12.5, 1.25, and 3.4 µM, respectively). Exhibits greater selectivity over other PI 3-Ks (IC50 = 5.0, 0.462, 5.0, 5.0, 5.0, 5.0, and 0.236 µM for PI 3-KC2α, PI 3-KC2β, PI 3-K class-III, mTOR, DNA-PK, PI 4-Kα and PI 4-Kβ, respectively) and 318 other protein kinases. Displays greater selectivity than PIK-75 (Cat. No. 528116) and reduces Akt and p70S6 kinase phosphorylation. Shown to retard the growth of SK-OV-3 and HCT-116 xenografted tumors in mice (75 mg/kg, i.p, q.d). Exhibits desirable pharmacokinetic properties (Tmax = 30 min; t1/2= 0.42 h; Cmax: 8.247 µM; and AUC0-inf = 6.8 µM/h; at 10 mg/kg). Also, reported to increase plasma insulin levels and enhance production of glucose from pyruvate in CD1 mice (10 mg/kg, i.p.).
      FormWhite solid
      Intert gas (Yes/No) Packaged under inert gas
      CAS number1166227-08-2
      Chemical formulaC₁₇H₂₃N₅O₂S₂
      Purity≥98% by HPLC
      SolubilityDMSO (50 mg/ml)
      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 3 months at -20-°C.
      Toxicity Standard Handling
      ReferencesHoland, K., et al. 2014. PLoS ONE. 9, e94132.
      Smith, G.C., et al. 2012. Biochem. J., 442, 161.
      Jamieson, S., et al. 2011. Biochem. J., 438, 53.
      Waardenberg, A.J., et al. 2011. J. Biol. Chem. 286, 30837.
      Sun, M., et al. 2010. Proc. Natl. Acad. Sci. USA. 35, 15547.