| 名称 | Supinoxin |
| 描述 | Supinoxin (RX-5902) is an orally active inhibitor of phosphorylated-p68 RNA helicase and a potent first-in-class anti-cancer agent, inducing cell apoptosis and inhibiting the growth of TNBC cancer cell lines (IC50s: 10 nM - 20 nM). |
| 体外活性 | Supinoxin inhibits cell growth, MDA-MB-231, Caki-1, UMRC2, PANC-1, A549, MKN-45, HepG2, HCT116, HT29, PC-3, U251, HeLa, SK-MEL-28 and OVCAR-3 (IC50: range from 0.01 μM to 0.021 μM in the growth inhibition of cancer cells). Supinoxin (0-10 μM; 72 hours) is active against cell lines of all TNBC molecular subtypes and is active against cell lines with mutations in p53, RB1, CDKN2A, and loss of PTEN. Supinoxin (20-100 nM; 24 hours) treatment causes a dose-dependent increase in tetraploid cells, consistent with induction of G2–M cell-cycle arrest. Supinoxin (0-100 nM; 24 or 48 hours) reduces MCL-1 expression in a dose-dependent manner in TNBC cell lines sensitive to Supinoxin. Supinoxin (0-100 nM; 72 hours) exhibits no significant induction of apoptosis in cell lines resistant to the antiproliferative effects of Supinoxin. But in sensitive cells, the observed activation of apoptosis begins at 24–48 hours and reaches a peak at 72 hours. The induced apoptosis is treated with a dose of 100 nM [1][2]. |
| 体内活性 | Supinoxin (p.o.; 160/320/600 mg/kg; once weekly for 3 weeks) obviously dose-dependent tumor growth inhibition in the MDA-MB-231 model, exhibits TGI of 55.7%, 80.29% and 94.58% at 160 mg/kg, 320 mg/kg and 600 mg/kg, respectively [1]. |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. |
| 溶解度 | DMSO : 100 mg/mL (226.52 mM), Sonication is recommended.
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| 关键字 | breast | inhibit | PANC-1 | Inhibitor | HCT116 | UMRC2 | PC-3 | MKN-45 | RX5902 | TNBC | HepG2 | DNA/RNA Synthesis | RNA helicase | HT29 | cancer | Apoptosis | A549 | Supinoxin | Caki-1 | RX 5902 |
| 相关产品 | Stavudine | 5-Fluorouracil | Acetylcysteine | Myricetin | Sodium 4-phenylbutyrate | L-Ascorbic acid | Dextran sulfate sodium salt (MW 4500-5500) | Guanidine hydrochloride | Metronidazole | Sorafenib | Tributyrin | Thymidine |
| 相关库 | 细胞凋亡化合物库 | 经典已知活性库 | 抗癌临床化合物库 | 药物功能重定位化合物库 | 抑制剂库 | 口服活性化合物库 | 抗衰老化合物库 | 已知活性化合物库 | 抗癌药物库 | 抗癌活性化合物库 |
United States
