GDC-0032

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-0032 是一种有效的下一代保留 β 异构体的 PI3K 抑制剂，靶向 PI3Kα/δ/γ，IC50 为 0.29 nM/0.12 nM/0.97nM，选择性是 PI3Kβ 的 10 倍以上。

GDC-0032 is a potent, next-generation β isoform-sparing PI3K inhibitor targeting PI3Kα/δ/γ with IC50 of 0.29 nM/0.12 nM/0.97nM, >10 fold selective over PI3Kβ.(In Vitro):Taselisib (GDC-0032) (100 nM) inhibits AKT/mTOR signaling in PIK3CA mutant cell lines but not in cells with loss or mutation of PTEN; Taselisib (GDC-0032) enhances radiation-induced apoptosis and inhibits growth in head and neck cancer cell lines that are sensitive to its single-agent activiy. Taselisib (GDC-0032) enhances the effects of MEK1/2 inhibition on both BRAFV600E/PTENNull human melanoma cells autochthonous mouse melanomas.(In Vivo):Taselisib (GDC-0032) (5 mg/kg, p.o.) potently impairs PI3K signaling and enhances the efficacy of fractionated radiotherapy; Taselisib (GDC-0032) and radiation is more effective than either treatment alone in nude mice implanted with subcutaneous Cal-33 xenografts. The vehicle-treated BRAFV600E/PTENNull melanoma-bearing mice experiencs initial tumor regression after treatment with Taselisib (GDC-0032) (22.5 mg/kg, p.o.).

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?Taselisib

PI3K/Akt/mTOR signaling

PI3K

PI3Kα| PI3Kβ| PI3Kγ| PI3Kδ

Cancer

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1282512-48-4

460.53

C24H28N8O2

>98% (HPLC)

Ethanol: 7 mg/mL warmed (15.19 mM); DMSO: 70 mg/mL warmed (151.99 mM)

CC(C)(N1N=CC(C2=CC=C3C4=NC(C5=NC(C)=NN5C(C)C)=CN4CCOC3=C2)=C1)C(N)=O

2-(4-(2-(1-isopropyl-3-methyl-1H-1,2,4-triazol-5-yl)-5,6-dihydrobenzo[f]imidazo[1,2-d][1,4]oxazepin-9-yl)-1H-pyrazol-1-yl)-2-methylpropanamide

(-20℃)

With Ice Pack

≥ 2 years