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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. 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.
| Molecular Weight | 530.92 |
| Formula | C24H34Cl3N5O2 |
| CAS Number | 1396257-94-5 |
| Solubility (25°C) | DMSO 10 mM |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
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| GSK690693
GSK690693 is a potent Akt inhibitor (Akt1 IC50 = 2 nM, Akt2 IC50 = 13 nM, Akt3 IC50 = 9 nM) which also inhibited the phosphorylation of the downstream target GSK3b in cells. |
| Perifosine
Perifosine is an orally active Akt inhibitor, the antiproliferative properties of Perifosine with an IC50 of 0.6–8.9 µM. |
| MK-2206 2HCl
MK-2206 is a novel allosteric inhibitor of Akt with IC50 values of 8 nM, 12 nM and 65 nM for Akt1, Akt2 and Akt3, respectively. |
| Ipatasertib
Ipatasertib (GDC-0068, RG7440) is a potent and selective, ATP-competitive Akt inhibitor with IC50 values of 5 to 18 nM. |
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