Catalog No.S2808 Synonyms: RG7440
Molecular Weight(MW): 458
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.
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Inhibition of AKT signaling abolishes MKK4 phosphorylation on Ser78 in injured axons. Cultures of sensory neurons were treated with 5 µM MK-2206 or 5 µM GDC-0068 for 1 hr prior to axotomy. Axonal proteins harvested at indicated time points after axotomy were subjected to immunoblot analysis.
Cell, 2015, 160(1-2): 161-76 . Ipatasertib (GDC-0068) purchased from Selleck.
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|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.|
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]
|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]|
-  Lin K. Cancer Res, 2011, 71(8 Supplement), abstract DDT02-01.
-  James F. Blake. 2011.
-  Tabernero J, et al. Ann Oncol, 2011, 22(suppl 3), abstract IL33.
|In vitro||DMSO||92 mg/mL (200.87 mM)|
|Ethanol||92 mg/mL (200.87 mM)|
* 1 mg/ml means slightly soluble or insoluble.
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Clinical Trial Information
|NCT Number||Recruitment||Conditions||Sponsor/Collaborators||Start Date||Phases|
|NCT01896531||Active, not recruiting||Gastric Cancer||Genentech, Inc.||August 2013||Phase 2|
|NCT01485861||Active, not recruiting||Prostate Cancer||Genentech, Inc.||December 2011||Phase 1|Phase 2|
|NCT01362374||Active, not recruiting||Solid Cancers||Genentech, Inc.||July 2011||Phase 1|
|NCT01090960||Completed||Solid Cancers||Genentech, Inc.||March 2010||Phase 1|
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