Immunoway/A66/10mg 50mg 100mg/MC0545
市场价：
¥10240.00
美元价：
5120.00
联系Q Q：
3392242852
电话号码：
4000-520-616
电子邮箱：
info@ebiomall.com
商品介绍
A66
- Catalog No.：MC0545
- Data Sheet
- MSDS
- Support
- Description
- References ( 0 )
- Protocol
- CasNo：
- 1166227-08-2
- MolecularFormula：
- C17H23N5O2S2
- Purity：
- >98%
- Target：
- PI3K
- IC50：
- IC50: 32 nM (p110α), 30 nM (p110α E545K), 43 nM (p110α H1047R), 3480 nM (p110γ)[1]
- In Vitro：
- A66 is a potent inhibitor of the wild-type and oncogenic forms of p110α but not other class-I PI3K isoforms[1]. The p110α-specific inhibitor A66 (0.7 μM) induces a 75-80% reduction in focus formation by the highly transforming iSH2 mutants KS459delN, DKRMNS560del, and K379E. The p110α-specific inhibitor A66 reduced phosphorylation of Akt on T308 by all p85 mutants[2].
- In Vivo：
- The optimal dosing strategy for xenograft studies is determined by investigating the drug pharmacokinetics after a dose of 10 mg/kg of body weight by intraperitoneal injection in CD-1 mice. Despite a short half-life of only 0.42 h, the large Cmax (8247 nM) of A66 S that is reached 30 min after dosing ensured that the AUC0-inf (area under the curve from zero time to infinity) (6809 nM•h) is similar to that of BEZ-235 (7333 nM•h), which has a longer half-life of 2.73 h. Furthermore, the A66 on SK-OV-3 tumour tissue is tested using a single dose of 100 mg/kg of body weight to determine whether a long-lasting effect of the drug could be achieved on target tissues. These studies show that A66 causes a profound reduction in the phosphorylation of Akt/PKB and p70 S6 kinase, but not of ERK (extracellular-signal-regulated kinase), at both 1 and 6 h after dosing. Levels of A66 in plasma are determined to be 21.1±1.2 μM and 9.1±1.1 μM at 1 and 6 h after drug injection, whereas levels of A66 in th
- Fields：
- A66 is a potent and specific p110α inhibitor with IC50 of 32 nM, >100 fold selectivity for p110α over other class-I PI3K isoforms.
- Specificity：
- Target: PI3K. Fields: A66 is a potent and specific p110α inhibitor with IC50 of 32 nM, >100 fold selectivity for p110α over other class-I PI3K isoforms.
- Source：
- Rabbit
- Dilution：
- IC50: 32 nM (p110α), 30 nM (p110α E545K), 43 nM (p110α H1047R), 3480 nM (p110γ)[1]
- Concentration：
- >98%
- Storage Stability：
- 2 years -20°C Powder, 2 weeks4°C in DMSO,6 months-80°C in DMSO
- MolecularWeight(Da)：
- 393.53
- References：
- [1]. Jamieson S, et al. A drug targeting only p110α can block phosphoinositide 3-kinase signalling and tumour growth in certain cell types. Biochem J, 2011, 438(1), 53-62. [2]. Sun M, et al. Cancer-
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