| Identification | Back Directory | [Name]
A66 | [CAS]
1166227-08-2 | [Synonyms]
CS-435
A 66;A-66
A66 USP/EP/BP
A66, 98%, a potent and specific p110α inhibitor
(2S)-N1-[2-(tert-Butyl)-4'-methyl[4,5'-bithiazol]-2'-yl]-1,2-pyrrolidinedicarboxamide
(2S)-N1-(5-(2-tert-butylthiazol-4-yl)-4-methylthiazol-2-yl)pyrrolidine-1,2-dicarboxamide
(2S)-N1-[2-(1,1-Dimethylethyl)-4'-methyl[4,5'-bithiazol]-2'-yl]-1,2-pyrrolidinedicarboxamide
1,2-Pyrrolidinedicarboxamide, N1-[2-(1,1-dimethylethyl)-4'-methyl[4,5'-bithiazol]-2'-yl]-, (2S)-
(2S)-N1-[2-(tert-Butyl)-4'-methyl[4,5'-bithiazol]-2'-yl]-1,2-pyrrolidinedicarboxamide A 66 | [Molecular Formula]
C17H23N5O2S2 | [MDL Number]
MFCD22378485 | [MOL File]
1166227-08-2.mol | [Molecular Weight]
393.53 |
| Chemical Properties | Back Directory | [density ]
1.354 | [storage temp. ]
Sealed in dry,Store in freezer, under -20°C | [solubility ]
insoluble in H2O; ≥19.7 mg/mL in DMSO; ≥2.63 mg/mL in EtOH with gentle warming | [form ]
solid | [pka]
6.27±0.70(Predicted) | [color ]
Off-white to light yellow |
| Hazard Information | Back Directory | [Description]
A-66 is a potent, selective inhibitor of the PI3K isoform p110α (IC50 = 32 nM in a cell-free assay).1 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.1 It also impairs all measures of in vivo insulin action in mice.2 A-66 partially suppresses B cell receptor-dependent Akt activation and proliferation.3 | [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 |
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| Company Name: |
LETOPHARM LIMITED
|
| Telephone: |
+86-21-5821 5861 |
| Website: |
www.letopharm.com |
| Company Name: |
D&C Chemicals
|
| Telephone: |
+86-21-58447131 |
| Website: |
www.chemicalbook.com/ShowSupplierProductsList16963/0_EN.htm |
| Company Name: |
SPIRO PHARMA
|
| Telephone: |
|
| Website: |
www.spiropharma.com.cn |
|