CS-435;A 66;A-66;A66 USP/EP/BP;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;(S)-N1-(2-(tert-Butyl)-4'-methyl-[4,5'-bithiazol]-2'-yl)pyrrolidine-1,2-dicarboxamide;(2S)-N1-(5-(2-tert-butylthiazol-4-yl)-4-methylthiazol-2-yl)pyrrolidine-1,2-dicarboxamide
insoluble in H2O; ≥19.7 mg/mL in DMSO; ≥2.63 mg/mL in EtOH with gentle warming
물리적 상태
고체
물리적 상태
단단한 모양
산도 계수 (pKa)
6.27±0.70(Predicted)
색상
Off-white to light yellow
안전
위험 및 안전 성명
위험 및 사전주의 사항 (GHS)
HS 번호
29341000
그림문자(GHS):
신호 어:
Warning
유해·위험 문구:
암호
유해·위험 문구
위험 등급
범주
신호 어
그림 문자
P- 코드
H302
삼키면 유해함
급성 독성 물질 - 경구
구분 4
경고
P264, P270, P301+P312, P330, P501
예방조치문구:
P280
보호장갑/보호의/보안경/안면보호구를 착용하시오.
P305+P351+P338
눈에 묻으면 몇 분간 물로 조심해서 씻으시오. 가능하면 콘택트렌즈를 제거하시오. 계속 씻으시오.
A66 C화학적 특성, 용도, 생산
개요
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.
효소 저해제
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.
