Lurbinectedin

Research use only, not for human use.

Lurbinectedin is a DNA minor groove covalent binder. Lurbinectedin also shows effective anti-tumor activity.

Lurbinectedin is a DNA minor groove covalent binder. Lurbinectedin also shows effective anti-tumor activity.(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. 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. (In Vivo):Lurbinectedin inhibits tumor growth significantly with no weight loss of treated animals, in four murine xenograft models of human cancer. Mouse CCC cell xenografts show that lurbinectedin significantly inhibits tumor growth. Lurbinectedin plus SN-38 causes a significant synergistic effect.

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PM01183

Others

Other Targets

kynurenine aminotransferase (KAT) II

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497871-47-3

784.88

C41H44N4O10S

>98% (HPLC)

In Vitro:?DMSO : 20 mg/mL (25.48 mM)

[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

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(-20℃)

With Ice Pack

≥ 2 years