S82947 |
AMG 232 |
| 源叶(MedMol) | 99% |
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- 产品描述： Navtemadlin (AMG 232) is a potent, selective and orally available inhibitor of p53-MDM2 interaction, with an IC50 of 0.6 nM. Navtemadlin binds to MDM2 with a Kd of 0.045 nM
- 靶点： IC50: 0.6 nM (p53-MDM2 interaction) Kd: 0.045 nM (MDM2)
- 体外研究：
Navtemadlin (AMG 232) (10 μM) induces p53 signaling and inhibits tumor cell proliferation in three p53 wild-type tumor cell lines. Navtemadlin potently inhibits proliferation of non-MDM2-amplified HCT116 colorectal cells (IC50=10 nM). Cell Viability Assay Cell Line: SJSA-1, HCT116, ACHN, NCI-H460, MOLM-13, RKO, MCF7, 22RV1, HT-29, PC-3, NCI-H82, NCI-SNU1, MG-63, NCI-H2452, SW982, C32, SK-HEP-1, A375, RT4, RPMI2650, MDA-MB-134-VI, NCI-H2347 and A427 cells.Concentration: 0-10 μM. Incubation Time: 72 hours. Result: Induced p53 signaling and inhibits tumor cell proliferation in three p53 wild-type tumor cell lines (SJSA-1, HCT116, and ACHN).Caused robust p21 mRNA induction between 9.76 and 34.9 fold with IC50 values ranging from 12.8 to 46.8 nM.
- 体内研究：
Navtemadlin (AMG 232) (10, 25, 75 mg/kg, once daily, p.o.) activates p53 pathway activity in vivo. Navtemadlin (10, 25, 75 mg/kg, once daily, p.o.) potently inhibits growth of tumor xenografts in mice. Navtemadlin (10, 25, 75 mg/kg, once daily, p.o.) blocks DNA synthesis and induces apoptosis in vivo. Navtemadlin causes a dose-dependent tumor growth inhibition with an ED50 of 16 mg/kg. Animal Model: Female athymic nude mice (n=10/group) based cancer models. Dosage: 10, 25, 75 mg/kg. Administration: Once daily by oral gavage. Result: Resulted in significant tumor growth inhibition across all models. SJSA-1, an MDM2 amplified osteosarcoma model, was the most sensitive to AMG 232 treatment with an ED50 of 9.1 mg/kg. In the highest dose group of 75 mg/kg, 10/10 tumors completely regressed and were undetectable after 10 days of treatment.
- 参考文献：
1. Canon J, et al. The MDM2 Inhibitor AMG 232 Demonstrates Robust Antitumor Efficacy and Potentiates the Activity of p53-Inducing Cytotoxic Agents. Mol Cancer Ther. 2015 Mar;14(3):649-58. 2. Rew Y, et al. Discovery of a small molecule MDM2 inhibitor (AMG 232) for treating cancer. J Med Chem. 2014 Aug 14;57(15):6332-41.
- 溶解性： Soluble in DMSO、H2O
- 保存条件： -20℃
- 配置溶液浓度参考：
1mg 5mg 10mg 1 mM 1.759 ml 8.794 ml 17.589 ml 5 mM 0.352 ml 1.759 ml 3.518 ml 10 mM 0.176 ml 0.879 ml 1.759 ml 50 mM 0.035 ml 0.176 ml 0.352 ml
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