GDC 0068 (Hydrochloride)
GDC 0068 (Hydrochloride) Basic information
- Product Name:
- GDC 0068 (Hydrochloride)
- Synonyms:
-
- Ipatasertib 2HCl
- GDC 0068 (Hydrochloride)
- GDC-0068 dihydrochloride
- (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 dihydrochloride
- Ipatasertib dihydrochloride
- RG-7440 dihydrochloride
- GDC0068 2HCl
- Ipatasertib (GDC-0068) 2HCl
- CAS:
- 1396257-94-5
- MF:
- C24H33Cl2N5O2
- MW:
- 494.46
- Mol File:
- 1396257-94-5.mol
GDC 0068 (Hydrochloride) Chemical Properties
- storage temp.
- Store at -20°C, sealed storage, away from moisture
- solubility
- DMSO : 125 mg/mL (235.44 mM);Water : ≥ 41 mg/mL (77.22 mM)
- form
- Solid
- color
- Light yellow to yellow
GDC 0068 (Hydrochloride) Usage And Synthesis
Uses
Ipatasertib dihydrochloride (GDC-0068 dihydrochloride) is a highly selective and ATP-competitive pan-Akt inhibitor with IC50s of 5, 18 and 8 nM for Akt1, Akt2 and Akt3, respectively.
in vivo
Ipatasertib is typically efficacious in xenograft models in which Akt is activated because of genetic alterations including PTEN loss, PIK3CA mutations/amplifications, or HER2 overexpression. In these models, tumor growth delay, stasis, or regression is achieved at or below 100 mg/kg daily oral dose, which is the maximum dose tested in immunocompromised mice that is well tolerated. When tested in vivo, daily dosing of Ipatasertib in combination with RP-56976 induces tumor regression and stasis in the PC-3 and MCF7-neo/HER2 xenograft models, at doses where each single agent is ineffective or only causes modest tumor growth delay. Similarly, increased TGI is observed in the OVCAR3 ovarian cancer xenograft model when Ipatasertib is combined with NSC 241240. The combination of Ipatasertib with RP-56976 or NSC 241240 is tolerated with less than 5% body weight loss when compared with treatment with each chemotherapeutic agent alone[2].
IC 50
Akt1: 5 nM (IC50); Akt3: 8 nM (IC50); Akt2: 18 nM (IC50); PKA: 3100 nM (IC50)
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 Sep 27;55(18):8110-27. DOI:10.1021/jm301024w
[2] Lin J, et al. Targeting activated Akt with GDC-0068, a novel selective Akt inhibitor that is efficacious in multiple tumor models. Clin Cancer Res. 2013 Apr 1;19(7):1760-72. DOI:10.1158/1078-0432.CCR-12-3072
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