Description
GDC-0941 can inhibit p110-alpha with IC50 of less than 10 nM.
Storage
2 years at -20centigrade Powder
Molecular Formula
C23H27N7O3S2
Chemical Name
2-(1H-indazol-4-yl)-6-((4-(methylsulfonyl)piperazin-1-yl)methyl)-4-morpholinothieno[3,2-d]pyrimidine
Solubility
DMSO 44 mg/mL Water
In vitro
GDC-0941, a class I selective PI3K inhibitor, can inhibit p110-alpha with IC50 of less than 10 nM. GDC-0941 showed a high efficacy of antitumor activity in two gefitinib-resistant non-small cell lung cancer (NSCLC) cell lines, A549 and H460,as H460 cells with activating mutations of PIK3CA were relatively more sensitive to GDC-0941 than A549 cells with wild-type PIK3CA.
In vivo
In GIST xenograft models, GDC-0941 causes tumor growth stabilization, inhibiting tumor cell proliferation, but did not induce apoptosis. Combination of DOX with the specific PI3K inhibitor GDC-0941 can lead to caspase 3 activation in xenografts of sarcoma cells.
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