GDC-0068; RG7440 MedChemExpress (MCE)

Product Name	GDC-0068
Synonyms	RG7440 RG 7440 RG-7440 GDC0068 GDC-0068 GDC 0068 Ipatasertib Synonyms RG7440 RG 7440 RG-7440 GDC0068 GDC-0068 GDC 0068 Ipatasertib GDC-0068(RG7440) Ipatasertib (GDC-0068) (S)-2-(4-chlorophenyl)-1-(4-((5R,7R)-7-hydroxy-5-methyl-6,7-dihydro-5H-cyclopenta[d]pyrimidin-4-yl)piperazin-1-yl)-3-(isopropylamino)propan-1-one (2S)-2-(4-Chlorophenyl)-1-[4-[(5R,7R)-6,7-dihydro-7-hydroxy-5-methyl-5H-cyclopentapyrimidin-4-yl]-1-piperazinyl]-3-[(1-methylethyl)amino]-1-propanone
CAS	1001264-89-6
EINECS
Chemical Formula	C24H32ClN5O2
Molecular Weight	458
inchi
Package	10 mM * 1 mL;1 mg;2 mg;5 mg;10 mg;25 mg;50 mg
Price	Email to quote
Descriptions	Ipatasertib Ipatasertib MedChemExpress (MCE) HY-15186 1001264-89-6 GDC-0068 Descriptions Ipatasertib Ipatasertib MedChemExpress (MCE) HY-15186 1001264-89-6 GDC-0068 RG7440 99.79% Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year Room temperature in continental US may vary elsewhere. Ipatasertib (GDC-0068) is an orally active, highly selective and ATP-competitive pan-Akt inhibitor with IC50 values of 5, 18, 8 nM for Akt1/2/3, respectively. Ipatasertib synchronously activates FoxO3a and NF-κB through inhibition of Akt leading to p53-independent activation of PUMA. Ipatasertib also induces apoptosis in cancer cells and inhibits tumor growth in xenograft mouse models. Ipatasertib (10 µM 12, 24 h) suppresses colon cancer cell proliferation by p53 irrespectively activating PUMA in vitro[1]. Ipatasertib (1, 5, 10, 20 μM 24 h/10 μM 3, 6, 12, 24 h) up-regulates the expression level of PUMA in a concentration and time dependent manner in HCT116 cells[1]. Ipatasertib increases the mRNA level of PUMA in HCT116 WT, p53−/−, and DLD1 (p53 mutant) cells[1]. Ipatasertib (10 µM 24 h) induces apoptosis through PUMA/Bax pathway in HCT116 cells[1]. Ipatasertib (30 mg/kg p.o. single daily for 15 consecutive days) exhibits PUMA-dependent antitumor activity in HCT116 WT and PUMA−/− cells xenograft nude mice model[1]. Akt1 5 nM (IC50) Akt3 8 nM (IC50) Akt2 18 nM (IC50) PKA 3100 nM (IC50) \| \| \| \| \| \| \| \| \| \| [1]. Sun L, et al. Ipatasertib, a novel Akt inhibitor, induces transcription factor FoxO3a and NF-κB directly regulates PUMA-dependent apoptosis. Cell Death Dis. 2018 Sep 5 9(9):911. [Content Brief] [2]. Blake JF, et al. Discovery and preclinical pharmacology of a selective ATP-competitive Akt inhibitor (GDC-0068) for the treatment of human tumors. J Med Chem. 2012 Sep 27 55(18):8110-27. [Content Brief]
Last Update	2025-04-01 14:45:47

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