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| 品牌 | absin | CAS | 1303607-60-4 |
|---|---|---|---|
| 分子式 | C29H34Cl2FN3O3 | 纯度 | 98% |
| 分子量 | 562.5 | 货号 | abs47028298 |
| 规格 | 10mg | 供货周期 | 现货 |
| 主要用途 | is an orally available MDM2 antagonist | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
SAR405838 1303607-60-4
| 产品描述 | |
| 描述 | MI-77301 (SAR405838))is an orally available MDM2 antagonist with Ki of 0.88 nM. Phase 1. |
| 纯度 | 98% |
| 储存/保存方法 | Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 别名 | SAR405838 |
| 可溶性/溶解性 | DMSO : 100 mg/mL (177.78 mM; Need ultrasonic) |
| 生物活性 | |
| 靶点 | p53,MDM2 |
| In vitro(体外研究) | MI-77301 (SAR405838) binds to MDM2 with Ki of 0.88 nM. MI-77301 (SAR405838) potently inhibits cell growth in cancer cell lines, including SJSA-1 (IC50, 0.092 μM), RS4;11 (IC50, 0.089 μM), LNCaP (IC50, 0.27 μM), and HCT-116 (IC50, 0.20 μM) cells, and displays high selectivity over cancer cell lines with mutated or deleted p53, including SAOS-2 (IC50, >10 μM), PC-3 (IC50, >10 μM), SW620 (IC50, >10 μM), and HCT-116 (p53-/-) (IC50, >20 μM) cells. |
| In vivo(体内研究) | In the SJSA-1 osteosarcoma, acute lymphoblastic leukemia RS4;11, LNCaP prostate cancer, and HCT-116 colon cancer xenograft model, MI-77301 (SAR405838) (p.o.) effectively inhibits tumor growth in a dose-dependent manner (10 mg/kg, 30 mg/kg, 50 mg/kg, 100 mg/kg, and 200 mg/kg,). |
| 参考文献 | |
| 参考文献 |
| 研究领域 | |
| 研究领域 | CancerCell cycleCell cycle inhibitorsp53 pathway CancerOncoproteins/suppressorsTumor suppressorsp53 pathway ApoptosisIntracellularp53 Pathway Cell CycleCell Cycle Inhibitorsp53 EpigeneticsCell cycleCell Cycle Inhibitorsp53 EpigeneticsDNA / RNADNA Damage & RepairDNA Damage Responsep53 EpigeneticsTranscriptionCancer susceptibilityTumor Suppressors NeuroscienceDevelopment NeuroscienceProcesses Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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