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

A66, CAS 1166227-08-2, is a potent, selective, reversible, ATP-competitive inhibitor of wild-type and oncogenic forms of PI 3-K isoform p110a (IC₅₀ = 32, 30, 43 nM for p110a, p110aE545K, p110H1047R).

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

Synonyms: A-66, (S)-form

Primary Target: wild-type and oncogenic forms of PI 3-K isoform p110α
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Overview

Replacement Information

Key Spec Table

CAS #Empirical Formula
1166227-08-2C₁₇H₂₃N₅O₂S₂
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
Global Trade Item Number
Catalogue Number GTIN
533637 0

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 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 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.