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Ipatasertib (GDC-0068)

Ipatasertib (GDC-0068)

Item no.	S2808-10
Manufacturer	Selleckchem
CASRN	1001264-89-6
Amount	10 mg
Quantity options	10 mg 100 mg 1 g 10 g 10 mM/1 mL 25 mg 5 mg 50 mg 5 g
Category	Oncology Neuroscience Metabolism Diabetes Aging & Neurological Disorders Inhibitors & Compound Libraries Small Molecules By Organ Breast Cancer Testicular & Prostate Cancer
Type	Inhibitors
Specific against	other
Smiles	CC1CC(C2=C1C(=NC=N2)N3CCN(CC3)C(=O)C(CNC(C)C)C4=CC=C(C=C4)Cl)O
ECLASS 10.1	32160490
ECLASS 11.0	32160490
UNSPSC	12000000
Alias	RG7440
Similar products	GDC-0068
Available
Manufacturer - Targets	AKT3, AKT2, AKT1
Storage Conditions	2 years -80 in solvent
Molecular Weight	458
Administration	Orally
Animal Models	Female nude mice bearing LNCaP, PC3, KPL-4, or MCF7 tumor xenografts
Clinical Trials	A Phase I study of GDC-0068 in patients with refractory solid tumors is ongoing.
Dosages	ca.100 mg/kg/day
Formulation	Formulated in 0.5% methylcellulose/0.2% Tween-80
IC50	5 nM, 5 nM, 5 nM, 5 nM, 5 nM, 5 nM
In vitro	Testing against a broad panel of 230 kinases, GDC-0068 only inhibits 3 kinases by >70% at 1 uM concentration (PRKG1alpha, PRKG1beta, 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 uM. 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]
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]
Solubility (25C)	DMSO 92 mg/mL, Water <1 mg/mL, Ethanol 92 mg/mL
Information	Ipatasertib (GDC-0068, RG7440) 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.
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

Note: The presented information and documents (Manual, Product Datasheet, Safety Datasheet and Certificate of Analysis) correspond to our latest update and should serve for orientational purpose only. We do not guarantee the topicality. We would kindly ask you to make a request for specific requirements, if necessary.

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S2808-10-datasheet.pdf

S2808-10-safety-datasheet.pdf