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Lurbinectedin (PM01183) is a DNA minor groove covalent binder that demonstrates effective anti-tumor activity.
Pack Size | Price | Availability | Quantity |
---|---|---|---|
1 mg | $1,480 | In Stock | |
2 mg | $1,990 | In Stock | |
5 mg | $2,960 | In Stock |
Description | Lurbinectedin (PM01183) is a DNA minor groove covalent binder that demonstrates effective anti-tumor activity. |
Targets&IC50 | RMG2:1.16 nM, RMG1:1.25 nM |
In vitro | 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]. |
In vivo | 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]. |
Alias | PM01183 |
Molecular Weight | 784.87 |
Formula | 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 |
Relative Density. | 1.55 g/cm3 (Predicted) |
Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | ||||||||||||||||||||
Solubility Information | DMSO: 15 mg/mL (19.11 mM) | ||||||||||||||||||||
Solution Preparation Table | |||||||||||||||||||||
DMSO
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