A66
- CAS No.
- 1166227-08-2
- Chemical Name:
- A66
- Synonyms
- CS-435;A 66;A-66;A66 ，S2636;A66 USP/EP/BP;A66（1166227-08-2）;A66, 10 mM in DMSO;A66 PI3K inhibitor A-66;A66, 98%, a potent and specific p110α inhibitor;Phosphoinositide 3-kinase,inhibit,PI3K,A66,Inhibitor,A-66,A 66;(2S)-N1-[2-(tert-Butyl)-4'-methyl[4,5'-bithiazol]-2'-yl]-1,2-pyrrolidinedicarboxamide
- CBNumber:
- CB42553771
- Molecular Formula:
- C17H23N5O2S2
- Molecular Weight:
- 393.53
- MDL Number:
- MFCD22378485
- MOL File:
- 1166227-08-2.mol
- MSDS File:
- SDS
- TDS File:
- TDS
SAFETY
Risk and Safety Statements
| Symbol(GHS) |  GHS07 |
|---|---|
| Signal word | Warning |
| Hazard statements | H302 |
| Precautionary statements | P280-P305+P351+P338 |
| HS Code | 29341000 |
A66 price More Price(53)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich | SML1213 | A66 ≥98% (HPLC) | 1166227-08-2 | 5 mg | $75.2 | 2026-04-30 | Buy |
| Sigma-Aldrich | SML1213 | A66 ≥98% (HPLC) | 1166227-08-2 | 25 mg | $295 | 2026-04-30 | Buy |
| Cayman Chemical | 17382 | A-66 ≥98% | 1166227-08-2 | 1mg | $40 | 2026-04-30 | Buy |
| Cayman Chemical | 17382 | A-66 ≥98% | 1166227-08-2 | 5mg | $105 | 2026-04-30 | Buy |
| Cayman Chemical | 17382 | A-66 ≥98% | 1166227-08-2 | 10mg | $190 | 2026-04-30 | Buy |
A66 Chemical Properties, Uses, Production
Description
A-66 is a potent, selective inhibitor of the PI3K isoform p110α (IC50 = 32 nM in a cell-free assay). It displays over 100-fold selectivity for p110α over other isoforms. A-66 is effective in vivo, suppressing the growth of SK-OV-3 tumor xenografts in mice. It also impairs all measures of in vivo insulin action in mice. A-66 partially suppresses B cell receptor-dependent Akt activation and proliferation.
Uses
A66 is a potent and specific p110α inhibitor. Inhibition of p110α can block phosphoinositide 3-kinase (PI3K) signalling and tumor growth in certain cell types.
Definition
ChEBI: (2S)-N1-[5-(2-tert-butyl-4-thiazolyl)-4-methyl-2-thiazolyl]pyrrolidine-1,2-dicarboxamide is a proline derivative.
Enzyme inhibitor
This potent and highly selective p110α inhibitor (FW = 393.53; CAS 1166227-08-2; Solubility: 79 mg/mL DMSO, 1 mg/mL H2O), also known as (2S)-N1-(5-(2-tert-butylthiazol-4-yl)-4-methylthiazol-2-yl)pyrrolidine-1, 2-dicarboxamide, has a IC50 value of 32 nM for the wild-type phosphoinositide-3 kinase p110 α as well as oncogenic forms of p110α such as p110α E545K (IC50 = 43 nM) and p110α H1047R (IC50 = 43 nM). A66 inhibition also demonstrated that cancer-specific mutations in the iSH2 (inter-SH2) and nSH2 (N-terminal SH2) domains of p85α, the regulatory subunit of phosphatidylinositide 3-kinase (PI3K), show gain of function, inducing oncogenic cellular transformation, stimulating cellular proliferation, and enhancing PI3K signaling.
storage
Store at -20°C
References
[1] STEPHEN JAMIESON. A drug targeting only p110α can block phosphoinositide 3-kinase signalling and tumour growth in certain cell types.[J]. Biochemical Journal, 2011, 438 1: 53-62. DOI: 10.1042/bj20110502
[2] GREG C SMITH. Effects of acutely inhibiting PI3K isoforms and mTOR on regulation of glucose metabolism in vivo.[J]. Biochemical Journal, 2012, 442 1: 161-169. DOI: 10.1042/bj20111913
[3] LOMON SO. Selective inhibition of phosphoinositide 3-kinase p110α preserves lymphocyte function.[J]. The Journal of Biological Chemistry, 2013: 5718-5731. DOI: 10.1074/jbc.m112.379446
A66 Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| Shanghai Boyle Chemical Co., Ltd. | sales@boylechem.com | China | 2915 | 55 | |
| Chembest Research Laboratories Limited | 021-20908456 | sales@BioChemBest.com | China | 5996 | 61 |
| Jinan Trio PharmaTech Co., Ltd. | 0531-88811783 | sales@trio-pharmatech.com | China | 1856 | 62 |
| Dalian Meilun Biotech Co., Ltd. | 0411-62910999 13889544652 | sales@meilune.com | China | 4765 | 58 |
| China Kouting Group Limited | +86 (21) 5811-6473 5811-6475 | sales@koutingchina.com | China | 494 | 60 |
| Haoyuan Chemexpress Co., Ltd. | 021-58950125 | info@chemexpress.com | China | 7545 | 61 |
| Shanghai Aladdin Bio-Chem Technology Co.,LTD | 400-6206333 13167063860 | anhua.mao@aladdin-e.com | China | 29985 | 65 |
| Nanjing Dulai Biotechnology Co., Ltd. | 025-84699383-8003;025-846993838003-8003 18013301590 | njduly@126.com | China | 3293 | 55 |
| AdooQ BioScience, LLC | +1 (866) 930-6790 | info@adooq.com | United States | 2774 | 58 |
| ShangHai Caerulum Pharma Discovery Co., Ltd. | 18149758185 18149758185 | sales-cpd@caerulumpharma.com | China | 3493 | 58 |
