GDC-0077

Research use only, not for human use.

GDC-0077 (RG-6114) is a potent, highly isoform selective inhibitor of PI3Kα, with IC50 of 0.038 nM.

GDC-0077 (RG-6114) is a potent, highly isoform selective inhibitor of PI3Kα, with IC50 of 0.038 nM, >300-fold selective over β, δ, and γ isoforms, as well as PIKK-family proteins such as mTOR, DNA-PK and VPS34; induces depletion of mutant PI3K alpha protein resulting in reduction of PI3K pathway biomarkers such as pAkt and pPRAS40, inhibition of cell proliferation and increased apoptosis in human PIK3CA mutant breast cancer cell lines to a greater extent when compared to PIK3CA wild-type cells; causes tumor regressions in cell-culture-derived and patient derived PIK3CA mutant breast cancer xenograft models.Breast Cancer Phase 1 Clinical

GDC0077;RG-6114;RG6114

PI3K/Akt/mTOR signaling

PI3K

PI3K

Cancer

Breast Cancer

2060571-02-8

407.38

C18H19F2N5O4

>98% (HPLC)

DMSO : ≥ 180 mg/mL. 441.86 mM

C[C@@H](C(N)=O)NC1=CC=C(C2=NC(N3[C@H](C(F)F)COC3=O)=CN2CCO4)C4=C1

(S)-2-((2-((S)-4-(difluoromethyl)-2-oxooxazolidin-3-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)amino)propanamide

(-20℃)

With Ice Pack

≥ 2 years