| 包装 | 价格(元) |
| 10mM (in 1mL DMSO) | 电议 |
| 10mg | 电议 |
| 25mg | 电议 |
| 50mg | 电议 |
| 100mg | 电议 |
Cell lines | A549 (adenocarcinoma), NCI-H460 (large cell carcinoma), and SK-MES-1 (squamous cell carcinoma) cells |
Preparation Method | Tumor cells were seeded in 96-well plates at a density of 5×103 per well. After incubation in presence of PF-4708671 (0.1μM, 0.3μM, 1μM, 3μM and 10μM) for 24, 48 and 72 hours, respectively, |
Reaction Conditions | 0.1μM, 0.3μM, 1μM, 3μM and 10μM for 24, 48 and 72 hours |
Applications | Proliferation abilities of the three NSCLC cell lines were significantly inhibited by PF-4708671. After 24 hours of treatment, PF-4708671 inhibited H460 cell proliferation at 10μM, and A549 and SK-MES-1 cell amounts were significantly reduced at 3μM and 0.1μM, respectively. In addition, H460, A549, and SK-MES-1 cell growth rates were significantly inhibited by PF-4708671 at 0.3μM, 0.1μM, and 0.1μM, respectively, 48 hours post treatment. All cell lines showed significantly reduced proliferation at 72 hour after treatment with 0.1μM PF-4708671. |
Animal models | Male C57Bl/6 mice (6 weeks old) |
Preparation Method | Mice were randomly assigned to three groups: (1) control (HF) receiving vehicle (8% EtOH [vol./vol.], 0.2% [wt/vol.] carboxymethylcellulose sterile); (2) treated with PF-4708671 (35 mg kg-1 day-1, i.p.); or (3) treated with rapamycin (2 mg kg-1 day-1, i.p.) for 7 days while being kept on the same high-fat diet. |
Dosage form | Intraperitoneal injection, 35 mg kg-1 day-1 for 7 days. |
Applications | PF-4708671 did not affect body weight or adiposity, 1 week of PF-4708671 treatment was found to improve fasting glucose whereas rapamycin further increased fasting hyperglycaemia in obese mice. |
| 产品描述 | PF-4708671, is a novel cell-permeable inhibitor of S6K1, specifically inhibits the S6K1 isoform with a Ki of 20 nM and IC50 of 160 nM.[1]. PF-4708671 prevents the S6K1-mediated phosphorylation of S6 protein in response to IGF-1 (insulin-like growth factor 1), PF-4708671 was also found to induce phosphorylation of the T-loop and hydrophobic motif of S6K1, an effect that is dependent upon mTORC1 (mTOR complex 1)[1]. RSK1, RSK2 and MSK1 were the other kinases inhibited by PF-4708671 (IC50 = 4.7 μM, 9.2 μM and 0.95 μM, respectively). PF-4708671 decreased phosphorylation of ribosomal protein S6 in HEK-293 cells. PF-4708671 has been used as the standard S6K1 inhibitor for the investigation of the role of S6K1 in several cancers. PF-4708671 in combination with tamoxifen was shown to be highly effective against ER+ MCF7 cells that had overexpression of S6K1[2]and enhanced cell death in glucose-starved MCF7 cells via downregulation of anti-apoptotic proteins Mcl-1 and survivin[3]. PF-4708671 inhibite the AKT/mTOR/S6K1 pathway led to the inhibition of cell migration in triple-negative MDA-MB-231 cells and inhibition of local relapse in mice models[4]. Moreover, PF-4708671 improved glucose tolerance in high-fat -fed obese mice by restoring Akt S473 phosphorylation in metabolic tissues[5]. PF-4708671 has protective effects against NMDA-induced retinal neurotoxicity in rats[6]. References: |
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