| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 询价 |
| 5mg | 询价 |
| 10mg | 询价 |
| 50mg | 询价 |
| 100mg | 询价 |
GDC-0068 (RG7440, Ipatasertib) is a novel highly selective ATP-competitive pan-Akt inhibitor that inhibits all three isoforms of Akt1, Akt2, and Akt3 at an IC50 of 5,18,8 nM, respectively.
Preparation Method | Inhibitor(GDC-0068 (RG7440)), enzyme (9 nM Akt1 or 100 pM PKA), and substrate (100 nM Crosstide) were incubated with 5 μM ATP in assay buffe, final DMSO 2% (v/v)) for 60 min at ambient temperature in a 5 μL reaction volume. Reactions were initiated by addition of enzyme + peptide substrate to ATP solutions. IMAP binding reagent (15 μL) was added to terminate the reaction, and the stopped reactions were incubated for a minimum of 30 min at room temperature (rt). |
Applications | GDC-0068 (RG7440) is a selective, ATP-competitive pan-Akt inhibitor that inhibits Akt1, Akt2, and Akt3 at an IC50 of 5,18,8 nM, respectively. |
Cell lines | HCT116 cell |
Preparation Method | To study how GDC-0068 (RG7440) influences tumor progression, cell viability was detected by CCK-8 in HCT116 at indicated time points after 1–20 μmol/L GDC-0068 (RG7440)treatment. |
Reaction Conditions | 1–20 μmol/L GDC-0068 (RG7440) for 0, 3, 6, 12, and 24 h |
Applications | Cell viability decreased markedly with increasing dose or time, cell proliferation was inhibited by GDC-0068 (RG7440) in a dose- and time-dependent manner. |
Animal models | Nude mice |
Preparation Method | Nude mice were injected s.c. with HCT116 WT or PUMA–/–. Once the tumor was measurable, mice were treated daily with 30 mg/kg GDC-0068 (RG7440) by oral gavage, for 15 consecutive days. |
Dosage form | 30 mg/kg GDC-0068 (RG7440) by oral gavage, for 15 consecutive days |
Applications | GDC-0068 (RG7440) therapy significantly inhibited the growth of WT tumors, however, for the PUMA / tumors, GDC-0068 (RG7440) therapy caused some suppression, but not so markedly compared with that of WT tumors |
| 产品描述 | GDC-0068 (RG7440, Ipatasertib) is a novel highly selective ATP-competitive pan-Akt inhibitor that inhibits all three isoforms of Akt1, Akt2, and Akt3 at an IC50 of 5,18,8 nM, respectively[1,5]. GDC-0068 decreased cell viability, induced apoptosis, and inhibited phosphorylation of proline rich Akt substrate 40 kDa and p70 S6 kinase in a dose-dependent manner in PIK3CA-mutant breast cancer brain metastatic cell lines compared with PIK3CA-wildtype cell lines[6]. The combined treatment of GDC-0068 (RG7440) plus anti-microtubule chemotherapy, including vinorelbine, paclitaxel, eribulin, is contributed to anti-proliferative, pro-apoptotic, and anti-metastatic effect on human breast cancer cells[7]. GDC-0068 (RG7440) blocked Akt signaling both in cultured human cancer cell lines and in tumor xenograft models as evidenced by dose-dependent decrease in phosphorylation of downstream targets. Inhibition of Akt activity by GDC-0068 (RG7440) resulted in blockade of cell-cycle progression and reduced viability of cancer cell lines[2]. Preclinical Pharmacology demonstrates GDC-0068 (RG7440) exposure resulting in a dose-dependently pharmacodynamic effect and robust anti-tumor activity in a broad spectrum of human cancer cells in vitro and in vivo[5]. GDC-0068 (RG7440) therapy significantly inhibited the growth of WT tumors, however, for the PUMA / tumors, GDC-0068 (RG7440) therapy caused some suppression, but not so markedly compared with that of WT tumors. Immunohistochemistry staining shows that the expression of P-Akt reduced in both WT and PUMA / tumors after GDC-0068 (RG7440) therapy. PUMA-dependent antitumor effects of GDC-0068 (RG7440) in colon cancer[4]. As an ATP-competitive Akt inhibitor, GDC-0068 (RG7440) is a strong and safe target for Akt, which has been proved in a first-in-human phase I study[3]. References: |
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