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.
Cited by 6 Publications
2 Customer Reviews
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.
In vitro evaluation of BAR activity in A549-BAR cell line. (A) Bioluminescence activity was quantified 1 hour after treatment in response to various compounds at two concentrations (n = 6). (B) Western blotting analysis after 1 hour of treatment showing the expression of pAKT (Ser473), AKT, pPRAS40 (Thr246), RAS40, pGSK3β (Ser9), GSK3β, pEGFR (Tyr1068), EGFR, and β-Actin of whole cell lysates.
Neoplasia, 2017, 19(4):310-320. Ipatasertib (GDC-0068) purchased from Selleck.
Purity & Quality Control
Choose Selective Akt Inhibitors
|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)|
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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 31 2013||Phase 2|
|NCT02536391||Completed||Cancer||Genentech Inc.||October 2015||Phase 1|
|NCT01562275||Completed||Neoplasms||Genentech Inc.||April 2012||Phase 1|
|NCT01090960||Completed||Solid Cancers||Genentech Inc.||March 2010||Phase 1|
|NCT02301988||Completed||Breast Cancer||Genentech Inc.|SOLTI Breast Cancer Research Group||February 17 2015||Phase 2|
|NCT01362374||Active not recruiting||Neoplasms||Genentech Inc.||July 11 2011||Phase 1|
Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.
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