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A66

Catalog No. T2418   CAS 1166227-08-2

A66 is a specific and effective p110α inhibitor(IC50=32 nM).

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A66 Chemical Structure
A66, CAS 1166227-08-2
Pack Size Availability Price/USD Quantity
1 mg In stock $ 34.00
2 mg In stock $ 47.00
5 mg In stock $ 77.00
10 mg In stock $ 127.00
25 mg In stock $ 245.00
50 mg In stock $ 432.00
100 mg In stock $ 639.00
500 mg In stock $ 1,330.00
1 mL * 10 mM (in DMSO) In stock $ 85.00
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Purity: 99.33%
Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description A66 is a specific and effective p110α inhibitor(IC50=32 nM).
Targets&IC50 p110α:32 nM
In vitro In male CD1 mice, A66 (10 mg/kg) increased glucose production during the pyruvate tolerance test. In SK-OV-3 tumor tissues, A66 (100 mg/kg) effectively reduced the phosphorylation of Akt/PKB and p70 S6 kinase, inhibiting tumor cell growth.
In vivo A66 significantly inhibits the oncogenic forms of p110α, such as p110αE545K (IC50=30 nM) and p110αH1047R (IC50=43 nM), effectively reducing their activity.
Kinase Assay IC50 values are evaluated using the PI3K (human) HTRF Assay. p85α/p110δ is obtained from Invitrogen. All other isoforms are produced in-house by co-expressing full-length human p85α with the indicated human full-length catalytic subunit containing a histidine tag at the N-terminus to allow purification. The PI3Ks are titrated and used at a concentration between their EC65-EC80 values. PI3K activity in immunoprecipitates is assayed using an antibody to the N-SH2 (N-Src homology 2) domain of p85α. Assays for other lipid kinases and protein kinases are performed by the National Centre for Protein Kinase Profiling and Invitrogen Drug Discovery Services[1].
Molecular Weight 393.53
Formula C17H23N5O2S2
CAS No. 1166227-08-2

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 1 mg/mL (2.54 mM)

DMSO: 79 mg/mL (200.74 mM)

TargetMolReferences and Literature

1. Jamieson S, et al. Biochem J, 2011, 438(1), 53-62. 2. Sun M, et al. Proc Natl Acad Sci U S A, 2010, 107(35), 15547-15552. 3. Smith GC, et al. Biochem J, 2012, 442(1), 161-169.

Related compound libraries

This product is contained In the following compound libraries:
Kinase Inhibitor Library Highly Selective Inhibitor Library Inhibitor Library PI3K-AKT-mTOR Compound Library Anti-Aging Compound Library NO PAINS Compound Library Anti-Colorectal Cancer Compound Library Autophagy Compound Library Anti-Prostate Cancer Compound Library Antioxidant Compound Library

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Keywords

A66 1166227-08-2 PI3K/Akt/mTOR signaling PI3K Phosphoinositide 3-kinase inhibit Inhibitor A-66 A 66 inhibitor

 

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