Inavolisib (GDC-0077, RG-6114) |CAS:2060571-02-8 Probechem Biochemicals

Chemical Structure : Inavolisib

CAS No.: 2060571-02-8

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Inavolisib (GDC-0077, RG-6114, GDC0077, RG6114)

货号: PC-63379Not For Human Use, Lab Use Only.

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

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5 mg	￥2580	In stock
10 mg	￥3980	In stock
25 mg	￥5980	In stock
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100 mg		Get quote

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生物&药学活性

GDC-0077 (Inavolisib, RG-6114) is a potent, highly isoform selective inhibitor of PI3Kα, with IC50 of 0.038 nM.
GDC-0077 displays >300-fold selective over β, δ, and γ isoforms, as well as PIKK-family proteins such as mTOR, DNA-PK and VPS34.
GDC-0077 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.
GDC-0077 causes tumor regressions in cell-culture-derived and patient derived PIK3CA mutant breast cancer xenograft models.

物理化学性质&存储条件

分子量	407.378
分子式	C18H19F2N5O4
外观性状	Solid
CAS No.
储存条件	固体粉末 -20 °C 12 个月; 4°C 6 个月	配置液 -80 °C 6 个月; -20°C 6 个月
Shipping
Solubility	DMSO: 100 mg/mL
Chemical Name/SMILES	(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

参考文献

1. Kyle Edgar, et al. Abstract 156: Preclinical characterization of GDC-0077, a specific PI3K alpha inhibitor in early clinical development. AACR July 2017.

Inavolisib (GDC-0077, RG-6114, GDC0077, RG6114)

生物&药学活性

物理化学性质&存储条件

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Inavolisib (GDC-0077, RG-6114, GDC0077, RG6114)

生物&药学活性

物理化学性质&存储条件

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