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

533637
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      Overview

      Replacement Information

      Key Specifications Table

      Empirical FormulaCAS #
      C₁₇H₂₃N₅O₂S₂ 1166227-08-2

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      5.33637.0001
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          Glass bottle 5 mg
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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
          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.