GDC-0077

本公司产品仅用于科研实验，不得用于人体或动物的临床与诊断

GDC-0077 (RG-6114) 是一种有效的、高度异构体选择性的 PI3Kα 抑制剂，IC50 为 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.

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GDC0077 | RG-6114 | RG6114

PI3K/Akt/mTOR signaling

PI3K

PI3K

Cancer

Breast Cancer

2060571-02-8

407.378

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