Product Name :
GDC-0068 — Akt Inhibitor
Description:
GDC-0068 is a highly potent, selective, and orally available pan-Akt inhibitor, targeting Akt1, Akt2 and Akt3 with IC50 of 5 nM, 18 nM and 8 nM, respectively. It has >100-fold selectivity over a broad panel of 230 kinases, except PRKG1α and PRKG1β with IC50 of 98 nM and 69 nM. GDC-0068 can effectively block Akt signaling and induce cell cycle arrest in human cancer cell lines in vitro, and exhibit significant efficacy in PTEN- and PI3K mutant xenograft models, including PTEN-deficient prostate cancer models LNCaP and PC3, the PIK3CA H1047R mutant breast cancer model KPL-4, and MCF7-neo/HER2 tumor model. A Phase I study of GDC-0068 in patients with refractory solid tumors is ongoing.
CAS:
1001264-89-6
Molecular Weight:
458.00
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 :
CC(C)NC[C@H](C1=CC=C(Cl)C=C1)C(=O)N1CCN(CC1)C1=NC=NC2[C@H](O)C[C@@H](C)C=21
InChiKey:
GRZXWCHAXNAUHY-NSISKUIASA-N
InChi :
InChI=1S/C24H32ClN5O2/c1-15(2)26-13-19(17-4-6-18(25)7-5-17)24(32)30-10-8-29(9-11-30)23-21-16(3)12-20(31)22(21)27-14-28-23/h4-7,14-16,19-20,26,31H,8-13H2,1-3H3/t16-,19-,20-/m1/s1
Purity:
≥98% (or refer to the Certificate of Analysis)
Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition :
Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.{{Hydrochlorothiazide} web|{Hydrochlorothiazide} TGF-beta/Smad|{Hydrochlorothiazide} Protocol|{Hydrochlorothiazide} Formula|{Hydrochlorothiazide} supplier|{Hydrochlorothiazide} Cancer}
Shelf Life:
≥12 months if stored properly.{{Theaflavin} MedChemExpress|{Theaflavin} Influenza Virus|{Theaflavin} Technical Information|{Theaflavin} In stock|{Theaflavin} manufacturer|{Theaflavin} Cancer}
Stock Solution Storage:
0 – 4 oC for 1 month or refer to the Certificate of Analysis.
Additional information:
GDC-0068 is a highly potent, selective, and orally available pan-Akt inhibitor, targeting Akt1, Akt2 and Akt3 with IC50 of 5 nM, 18 nM and 8 nM, respectively. It has >100-fold selectivity over a broad panel of 230 kinases, except PRKG1α and PRKG1β with IC50 of 98 nM and 69 nM. GDC-0068 can effectively block Akt signaling and induce cell cycle arrest in human cancer cell lines in vitro, and exhibit significant efficacy in PTEN- and PI3K mutant xenograft models, including PTEN-deficient prostate cancer models LNCaP and PC3, the PIK3CA H1047R mutant breast cancer model KPL-4, and MCF7-neo/HER2 tumor model. A Phase I study of GDC-0068 in patients with refractory solid tumors is ongoing.|Product information|CAS Number: 1001264-89-6|Molecular Weight: 458.00|Formula: C24H32ClN5O2|Synonym:|Ipatasertib|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: CC(C)NC[C@H](C1=CC=C(Cl)C=C1)C(=O)N1CCN(CC1)C1=NC=NC2[C@H](O)C[C@@H](C)C=21|InChiKey: GRZXWCHAXNAUHY-NSISKUIASA-N|InChi: InChI=1S/C24H32ClN5O2/c1-15(2)26-13-19(17-4-6-18(25)7-5-17)24(32)30-10-8-29(9-11-30)23-21-16(3)12-20(31)22(21)27-14-28-23/h4-7,14-16,19-20,26,31H,8-13H2,1-3H3/t16-,19-,20-/m1/s1|Technical Data|Appearance: Solid Power.|Purity: ≥98% (or refer to the Certificate of Analysis)|Solubility: DMSO up to 100 mM|Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis|Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.PMID:23671446 |Shelf Life: ≥12 months if stored properly.|Stock Solution Storage: 0 – 4 oC for 1 month or refer to the Certificate of Analysis.|Drug Formulation: To be determined.|HS Tariff Code: 382200|How to use|In Vitro:|GDC-0068 was used at 5-10 µM final concentration in vitro and in cellular assays.|In Vivo:|GDC-0068 was orally dosed to mice at 50-100 mg/kg once per day, or in combination with MEK inhibitors or chemotherapy agents to significantly reduce the tumor volume. Formulation: 0.5% methylcellulose/0.2% Tween-80.|References:|Blake JF, et al. Discovery and Preclinical Pharmacology of a Selective ATP-Competitive Akt Inhibitor (GDC-0068) for the Treatment of Human Tumors. (2012) J Med Chem. 55(18):8110-27.Heidi M, et al. Abstract 966: Predictive biomarkers of the AKT inhibitor, GDC-0068, in single agent and combination studies. (2012) Cancer Research. Volume 72, Issue 8, Supplement 1Kui Lin. Abstract DDT02-01: GDC-0068: A novel, selective, ATP-competitive inhibitor of Akt. (2011) Cancer Research. Volume 71, Issue 8, Supplement 1Products are for research use only. Not for human use.|Documents||