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GDC0068

(CAS No:1001264-89-6)

Ipatasertib (GDC-0068) is a highly selective pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 5 nM/18 nM/8 nM in cell-free assays, 620-fold selectivity over PKA. Phase 2.

CAS No:1001264-89-6

Molecular Weight(MW):458

Purity:98%+

Specification:500mg;1g;5g;10g;50g;100g

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QC Documents

COA	MSDS	HPLC	NMR

ChemicalInfomation

CAS No:	1001264-89-6
Molecular formula(MF)	C₂₄H₃₂ClN₅O₂
Molecular Weight(MW):	458
Alias

Solubility

In vitro	DMSO	92 mg/mL (200.87 mM)
	Ethanol	92 mg/mL (200.87 mM)
	Water	<1 mg/mL

Biological Activity

Description

Ipatasertib (GDC-0068) is a highly selective pan-Akt inhibitor targeting Akt1/2/3 with IC50 of 5 nM/18 nM/8 nM in cell-free assays, 620-fold selectivity over PKA. Phase 2.

Targets

Akt1 ^[1] (Cell-free assay)	Akt3 ^[1] (Cell-free assay)	Akt2 ^[1] (Cell-free assay)
5 nM	8 nM	18 nM

In vitro

Testing against a broad panel of 230 kinases, GDC-0068 only inhibits 3 kinases by >70% at 1 μM concentration (PRKG1α, PRKG1β, and p70S6K, with IC50 of 98 nM, 69 nM, and 860 nM, respectively). GDC-0068 displays >100-fold selectivity for Akt over PKA with IC50 of 3.1 μM. In LNCaP, PC3 and BT474M1 cells, GDC-0068 treatment inhibits the phosphorylation of the Akt substrate, PRAS40 with IC50 of 157 nM, 197 nM, and 208 nM, respectively. Furthermore, GDC-0068 selectively inhibits cell cycle progression and viability of cancer cell lines driven by Akt signaling, including those with defects in the tumor suppressor PTEN, oncogenic mutations in PIK3CA, and amplification of HER2, with strongest effects in HER2⁺ and Luminal subtypes. ^[1-4]

Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	Formulation	Activity Description	PMID
HCC70	Function Assay	1 Î¼M	24 h		increases the abundance of HER3 and induces the phosphorylation (activation) of both EGFR and HER3	24667376
MDA-MB-468	Function Assay	1 Î¼M	24 h		increases the abundance of HER3	24667376
HCC70	Growth Inhibition Assay	1 Î¼M	5 d		enhances the antiproliferative response	24667376
MDA-MB-468	Growth Inhibition Assay	1 Î¼M	5 d		enhances the antiproliferative response	24667376
PC-3	Function Assay	0.0038-2.5 Î¼M	1 h	DMSO	induces a dose-dependent increase in Akt phosphorylation at both Thr308Â (T308) and Ser473	23287563
BT474M1	Function Assay	0.0038-2.5 Î¼M	1 h	DMSO	induces a dose-dependent increase in Akt phosphorylation at both Thr308Â (T308) and Ser473	23287563
IGROV-1	Function Assay	0.0038-2.5 Î¼M	1 h	DMSO	induces a dose-dependent increase in Akt phosphorylation at both Thr308Â (T308) and Ser473	23287563
PC-3	Growth Inhibition Assay	1/5/10 Î¼M	24/48/72 h	DMSO	dose-dependently increases the G0âG1Â phase populationÂ	23287563
MCF7-neo/HER2	Growth Inhibition Assay	1/5/10 Î¼M	24/48/72 h	DMSO	dose-dependently increases the G0âG1Â phase populationÂ	23287563
BT474M1	Growth Inhibition Assay	1/5/10 Î¼M	24/48/72 h	DMSO	dose-dependently increases the G0âG1Â phase populationÂ	23287563
PC-3	Apoptosis Assay	1/5/10 Î¼M	15/48/72 h	DMSO	causes a dose- and time-dependent increase in apoptotic and necrotic populations	23287563
MCF7-neo/HER2	Apoptosis Assay	1/5/10 Î¼M	15/48/72 h	DMSO	causes a dose- and time-dependent increase in apoptotic and necrotic populations	23287563
BT474M1	Apoptosis Assay	1/5/10 Î¼M	15/48/72 h	DMSO	causes a dose- and time-dependent increase in apoptotic and necrotic populations	23287563

... Click to View More Cell Line Experimental Data

In vivo

Oral administration of GDC-0068 in PC3 prostate tumor xenografts model induces down-regulation of p-PRAS40. In BT474-Tr xenografts, GDC-0068 treatment reduces pS6 and peIF4G levels, re-localizes FOXO3a to nucleus, and induces feedback upregulation of HER3 and pERK. Administration of GDC-0068 exhibits potent antitumor efficacy in multiple xenograft tumor models, including the PTEN-deficient prostate cancer models LNCaP and PC3, the PIK3CA H1047R mutant breast cancer model KPL-4, and MCF7-neo/HER2 tumor model. ^[1-4]