PI 3-K Inhibitor XXI, GDC-0941 – CAS 957054-30-7 – Calbiochem

Descrição detalhada : A cell-permeable thienopyrimidine compound that acts as a potent, ATP-competitive inhibitor against class IA (IC50 = 3 nM/p110alpha, 33 nM/p110beta, 3 nM/p110delta) & IB (IC50 = 75 nM/p110gamma) PI 3-K kinases, including the two known p110alpha hot spot mutants E454K & H1047R (IC50 = 3 nM), while exhibiting much reduced or little potency against more than 200 other kinases, including TrkA, class II C2beta, class IV mTOR & DNA-PK (IC50 = 2.85, 0.67, 0.58, and 1.23 µM, respectively) and class III Vps34 (IC50 >10 µM). Effectively inhibits cellular Akt S473 phosphorylation (IC50 = 46 nM/U87MG, 37 nM/PC3, and 28 nM/MDA-MB-361) as well as proliferation in cancer cultures in vitro (GI50 = 950/U87MG, 280/PC3, and 720 nM/MDA-MB-361) and greatly prevents the expansion of U87MG glioblastoma xenograft in mice in vivo (by 83%; 75 mg/kg/d p.o. for 21 days). Oral bioavailability is reported in human, dog, mouse, and rat., A cell-permeable thienopyrimidine compound that acts as a potent, ATP-competitive inhibitor against class IA (IC50 = 3 nM/p110alpha, 33 nM/p110beta, 3 nM/p110delta) & IB (IC50 = 75 nM/p110gamma) PI 3-K kinases, including the two known p110alpha hot spot mutants E454K & H1047R (IC50 = 3 nM), while exhibiting much reduced or little potency against more than 200 other kinases, including TrkA, class II C2beta, class IV mTOR & DNA-PK (IC50 = 2.85, 0.67, 0.58, and 1.23 µM, respectively) and class III Vps34 (IC50 >10 µM). Effectively inhibits cellular Akt S473 phosphorylation (IC50 = 28 to 46 nM) as well as proliferation in cancer cultures in vitro (GI50 = 280 to 950 nM) and completely prevents the expansion of U87MG glioblastoma xenograft in mice in vivo (by 83%; 75 mg/kg/d p.o. for 21 days). Oral bioavailability is reported in human, dog, mouse, and rat.
Sinónimos : PI 3-K Inhibitor XXI, GDC-0941 - CAS 957054-30-7 - Calbiochem; GDC0941, 2-(1H-Indazol-4-yl)-6-(4-methylsulfonyl-piperazin-1-ylmethyl)-4-morpholin-4-yl-thieno[3,2- d]pyrimidine, 4-(2-(1H-Indazol-4-yl)-6-((4-(methylsulfonyl)piperazin-1-yl)methyl)thieno[3,2-d]pyrimidin-4-yl)morpholine
Fórmula molecula r: C23H27N7O3S2
Armazenamento : 2-8C; 2-8C
Embalagem : 1X1EA