貨號:A124368
同義名:
RG7388; Ro 5503781
Idasanutlin (RG7388) 是一種強效且選擇性的 MDM2 拮抗劑,IC50 為 6 nM,能抑制 p53-MDM2 結合。


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| 產品名稱 | p53 ↓ ↑ | 其他靶點 | 純度 | ||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| Pifithrin-μ | ? | 99%+ | |||||||||||||||||
| Pifithrin-α HBr | ? | 98% | |||||||||||||||||
| 1. 鼠標懸停在“+”上可以顯示相關IC50的具體數值。"+"越多,抑制作用越強。2. "?"表示該化合物對相應的亞型有抑制作用,但抑制強度暫時沒有相關數據。 | |||||||||||||||||||
| 描述 | Tumor suppressor p53 is a powerful growth suppressive and pro-apoptotic protein that plays a central role in protectionfrom tumor development. The overproduction of MDM2, the primary negative regulator of p53, effectively disables p53 function. RG7388, a potent and selective MDM2 antagonist, inhibits p53-MDM2 interaction with an IC50 value of 6 nM. RG7388 induced dose-dependent p53 stabilization, cell cycle arrest, and apoptosis in cancer cells expressing wild-type p53, consistent with a nongenotoxic p53 activation mechanism[2]. In the MDM2-amplified SJSA1 osteosarcoma cell line, a significant apoptotic response over the control was induced with both the single 300 nmol/L and 1.8 μmol/L concentrations of RG7388 for 16 hours (P < 0.005), with the 1.8 μmol/L concentration providing optimal response. In SJSA osteosarcoma xenograft-bearing mice, the once-daily dose of 30 mg/kg of RG7388 (total 210 mg/kg/wk) seemed to be the most effective dose at inhibiting tumor growth (>100% TGI with 9 partial regressions), the 50 mg/kg of RG7388 given twice a week (total 100 mg/kg/wk) was equivalent by statistical analysis (96% TGI with 3 partial regressions; P > 0.05) [1]. It also achieved 88% tumor growth inhibition against established human SJSA1 osterosarcoma xenografts in nude mice at a dose of 12.5 mg/kg[2]. |
| 細胞系 | 濃度 | 檢測類型 | 檢測時間 | 活性說明 | 數據源 |
| HCT116 cells | Cytotoxic?assay | Cytotoxicity against human HCT116 cells expressing wild type p53 assessed as growth inhibition by MTT assay, IC50=0.01 μM | 23808545 | ||
| MDA-MB-435 cells | Cytotoxic?assay | Cytotoxicity against human MDA-MB-435 cells expressing p53 mutant assessed as growth inhibition by MTT assay, IC50=9.1 μM | 23808545 | ||
| RKO cells | Cytotoxic?assay | Cytotoxicity against human RKO cells expressing wild type p53 assessed as growth inhibition by MTT assay, IC50=0.07 μM | 23808545 | ||
| SJSA1 cells | Cytotoxic?assay | Cytotoxicity against human SJSA1 cells expressing wild type p53 assessed as growth inhibition by MTT assay, IC50=0.01 μM | 23808545 | ||
| 計算器 | ||||
| 存儲液制備 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
1.62mL 0.32mL 0.16mL |
8.11mL 1.62mL 0.81mL |
16.22mL 3.24mL 1.62mL |
|
| CAS號 | 1229705-06-9 |
| 分子式 | C31H29Cl2F2N3O4 |
| 分子量 | 616.48 |
| SMILES Code | O=C(O)C1=CC(OC)=C(NC([C@H]2[C@H](C3=C(F)C(Cl)=CC=C3)[C@](C4=CC=C(Cl)C=C4F)(C#N)[C@H](CC(C)(C)C)N2)=O)C=C1 |
| MDL No. | MFCD26142931 |
| 別名 | RG7388; Ro 5503781 |
| 運輸 | 藍冰 |
| InChI Key | TVTXCJFHQKSQQM-LJQIRTBHSA-N |
| Pubchem ID | 53358942 |
| 存儲條件 |
In solvent -20°C: 3-6個月 -80°C: 12個月 Pure form Keep in dark place, sealed in dry, 2-8°C |
| 溶解方案 |
DMSO 中的溶解度 : ≥ 45 mg/mL (73.00 mM; 吸濕的 DMSO 對產品的溶解度有顯著影響,請使用新開封的 DMSO) * "≥" means soluble, but saturation unknown. 以下溶解方案都請先按照體外實驗的方式配制澄清的儲備液,再依次添加助溶劑: ——為保證實驗結果的可靠性,澄清的儲備液可以根據儲存條件,適當保存;體內實驗的工作液,建議現用現配,當天使用; 以下溶劑前顯示的百分比是指該溶劑在終溶液中的體積占比;如在配制過程中出現沉淀、析出現象,可以通過加熱和/或超聲的方式助溶
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