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Lurbinectedin (PM01183) 是一种 DNA 小沟共价粘合剂,可抑制 RMG1和 RMG2,IC50值分别为1.25和1.16 nM。它具有高效的抗肿瘤活性。
Lurbinectedin (PM01183) 是一种 DNA 小沟共价粘合剂,可抑制 RMG1和 RMG2,IC50值分别为1.25和1.16 nM。它具有高效的抗肿瘤活性。
规格 | 价格 | 库存 | 数量 |
---|---|---|---|
1 mg | ¥ 3,950 | 现货 | |
5 mg | ¥ 8,150 | 现货 | |
10 mg | ¥ 11,700 | 现货 | |
25 mg | ¥ 17,200 | 现货 |
产品描述 | Lurbinectedin (PM01183) is a DNA minor groove covalent binder. Lurbinectedin also shows effective anti-tumor activity. |
靶点活性 | RMG2:1.16 nM, RMG1:1.25 nM |
体外活性 | Lurbinectedin inhibits RMG1 and RMG2 cell growth (IC50: 1.25 and 1.16 nM, respectively). Lurbinectedin exhibits significant antitumor activity toward chemosensitive and chemoresistant human ovarian clear cell carcinoma (CCC) cells in vitro[1]. Lurbinectedin-DNA adducts in living cells give rise to double-strand breaks, triggering S-phase accumulation, and apoptosis. Lurbinectedin is a new synthetic tetrahydroisoquinoline alkaloid that is currently in phase I clinical development for the treatment of solid tumors. The potent cytotoxic activity of Lurbinectedin is ascertained in a 23-cell line panel with a mean GI50 value of 2.7 nM[2]. |
体内活性 | Lurbinectedin inhibits tumor growth significantly with no weight loss of treated animals, in four murine xenograft models of human cancer[2]. Mouse CCC cell xenografts show that lurbinectedin significantly inhibits tumor growth. Lurbinectedin plus SN-38 causes a significant synergistic effect[1]. |
别名 | 卢比克替定, PM01183 |
分子量 | 784.87 |
分子式 | C41H44N4O10S |
CAS No. | 497871-47-3 |
Smiles | [H][C@@]12Cc3cc(C)c(OC)c(O)c3[C@@]([H])(N1C)[C@@]1([H])N([C@H]2O)[C@@]2([H])COC(=O)[C@]3(CS[C@]1([H])c1c(OC(C)=O)c(C)c4OCOc4c21)NCCc1c3[nH]c2ccc(OC)cc12 |
密度 | 1.55 g/cm3 (Predicted) |
存储 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
溶解度信息 | DMSO: 15 mg/mL (19.11 mM) | ||||||||||||||||||||
溶液配制表 | |||||||||||||||||||||
DMSO
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