GDC0068 Inhibitor CAS No. 1001264-89-6

Cat. No.	Name	Size	Price
KI0087	GDC0068	5 mg	$220
	GDC0068	10 mg	$352
	GDC0068	50 mg	$1602
	GDC0068	100 mg	$2672

Chemical Characteristic

Product Name	GDC0068
Synonyms	Ipatasertib
CAS No.	1001264-89-6
Molecular Weight	458
Formula	C₂₄H₃₂ClN₅O₂
Chemical Name	(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
Smiles	C(=O)([C@H](CNC(C)C)c1ccc(cc1)Cl)N1CCN(CC1)c1c2c(ncn1)[C@@H](C[C@H]2C)O
Chemical Structure

Biological activities

GDC0068 is a selective ATP-competitive Akt inhibitor. The IC50 of GDC0068 is 5, 18 and 8 nM against Akt1, Akt2 and Akt3, respectively. Therefore, GDC0068 potently inhibits Akt signaling in LNCaP cells. GDC0068 have a potent antiproliferative effect on LNCaP cells with an IC50 of 95 nM. GDC0068 reduces p-PRAS40 levels in LNCaP cells with IC50 of 157 nM while GDC0068 inhibits PKA (protein kinase A) with an IC50 of 3.1 µM. Additionally, GDC0068 is able to inhibit overall viability of other cells including PC3, MCF7-neo/HER2, and BT474M1 cells with IC50 ranging from 1 µM to 4 µM. GDC0068 induces a dose-dependent block of the cell-cycle progression at the G1 phase and a dose- and time-dependent increase in apoptosis and necrosis in MCF7-neo/HER2 and BT474M1 cells.^[1] Both of single or multiple doses of GDC0068 are administered daily (qd) or twice daily (bid) in nude mice bearing PC3 prostate cancer xenografts. In addition, half-maximal doses of GDC0068 (50 mg/kg) given orally bid results in a nearly equivalent tumor growth inhibition of 81% when compared with qd dosing of 100 mg/kg. Systemic exposure of GDC0068 increases in a more than dose-proportional fashion with increasing dose, leading to good exposures. Plasma concentrations are at or above 200 nM for the 12.5 and 50 mg/kg dose groups, respectively, within 1 hour of GDC0068 administration. With the 50 mg/kg po dose, plasma concentrations are approximately 7.4 µM at 1 hour postdose and 0.5 µM at 9 hours postdose. The concentration of GDC0068 is above 200 nM for approximately 9 hours. GDC0068 is efficacious against human PC3 prostate cancer xenografts in vivo when dosed orally either qd or bid. ^[1] GDC0068 induces pharmacodynamic knockdown of key Akt signaling outputs that correlates with drug exposure. Antitumor efficacy of GDC0068 is observed in multiple xenograft tumor models, including those of human prostate, breast, ovarian, colon, glioma and melanoma origins.^[2]

References

[1] 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, 55(18): 8110-8127. [2] Lin K. GDC-0068: A novel, selective, ATP-competitive inhibitor of Akt. AACR 102nd Annual Meeting 2011, Apr 2-6, No. DDT02-01.

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