Lurbinectedin

SKU: orb1308109

Description

Lurbinectedin (PM01183) is a synthetic small molecule that covalently binds to the minor groove of DNA, exhibiting potent antitumor activity. It is widely used in oncology research, demonstrating efficacy in both in vitro cytotoxicity assays and in vivo models of various cancers, including small cell lung cancer.

Research Area

Cell Biology, Molecular Biology, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 497871-47-3
• MW: 784.87
• Purity: 98.11% (May vary between batches)
• Formula: C₄₁H₄₄N₄O₁₀S
• 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
• Target: Others
• Solubility: DMSO:15 mg/mL (19.11 mM)

Bioactivity

• Target IC50:
  RMG2:1.16 nM|RMG1:1.25 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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• 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.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

RMG1, RMG2, Inhibitor, Lurbinectedin, PM-01183, PM 01183, PM01183, inhibit, DNA Alkylator/Crosslinker, DNA/RNA Synthesis

Compound Identifiers

PubChem CID

57327016