1. Cell Cycle/DNA Damage
  2. DNA Alkylator/Crosslinker
    DNA/RNA Synthesis
  3. Lurbinectedin

Lurbinectedin (Synonyms: PM01183)

Cat. No.: HY-16293 Purity: 99.73%
Handling Instructions

Lurbinectedin (PM01183) is a DNA minor groove covalent binder with potent anti-tumour activity; inhibits RMG1 and RMG2 cell growth with IC50 values of 1.25 and 1.16 nM, respectively.

For research use only. We do not sell to patients.

Lurbinectedin Chemical Structure

Lurbinectedin Chemical Structure

CAS No. : 497871-47-3

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100 μg USD 550 In-stock
Estimated Time of Arrival: December 31
1 mg USD 1800 In-stock
Estimated Time of Arrival: December 31
2 mg USD 3360 In-stock
Estimated Time of Arrival: December 31
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Based on 1 publication(s) in Google Scholar

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Description

Lurbinectedin (PM01183) is a DNA minor groove covalent binder with potent anti-tumour activity; inhibits RMG1 and RMG2 cell growth with IC50 values of 1.25 and 1.16 nM, respectively.

IC50 & Target

IC50: 1.25 nM (RMG1), 1.16 nM (RMG2)[1]

In Vitro

PM01183 is a new synthetic tetrahydroisoquinoline alkaloid that is currently in phase I clinical development for the treatment of solid tumours. PM01183–DNA adducts in living cells give rise to double-strand breaks, triggering S-phase accumulation and apoptosis. The potent cytotoxic activity of PM01183 is ascertained in a 23-cell line panel with a mean GI50 value of 2.7 nM[2]. Lurbinectedin exhibits significant antitumor activity toward chemosensitive and chemoresistant human ovarian clear cell carcinoma (CCC) cells in vitro[1].

In Vivo

Mouse CCC cell xenografts reveals that lurbinectedin significantly inhibits tumor growth. Lurbinectedin plus SN-38 results in a significant synergistic effect[1]. In four murine xenograft models of human cancer, PM01183 inhibits tumour growth significantly with no weight loss of treated animals[2]. Single lurbinectedin or NSC 119875-combined therapies are effective in treating NSC 119875-sensitive and NSC 119875-resistant preclinical ovarian tumor models. The strongest synergistic effect is observed for combined treatments, especially in NSC 119875-resistant tumors. Lurbinectedin tumor growth inhibition is associated with reduced proliferation, increased rate of aberrant mitosis, and subsequent induced apoptosis[3].

Clinical Trial
Molecular Weight

784.87

Formula

C₄₁H₄₄N₄O₁₀S

CAS No.

497871-47-3

SMILES

O[[email protected]@H]([[email protected]@](CC1=CC(C)=C2OC)([H])N(C)[[email protected]]3([H])C1=C2O)N([[email protected]](COC4=O)([H])C5=C(OCO6)C6=C7C)[[email protected]@]3([H])[[email protected]@](SC[[email protected]@]4(NCC8)C9=C8C%10=CC(OC)=CC=C%10N9)([H])C5=C7OC(C)=O

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
References
Cell Assay
[1]

The MTS assay is used to analyze the effects of each drug. Cells are plated in 96-well plates and treated with PM01183 (0, 0.1, 0.3, 1, 3 nM) . After 48 hours’ incubation, the number of surviving cells is assessed by determining the A490nm of the dissolved formazan product after the addition of MTS for 1 hour. Cell viability is calculated as follows: Aexp group / Acontrol×100[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[3]

Mice: Mice are transplanted with fragments of OVAX1 and OVAX1R tumors, and when tumors reaches a homogeneous palpable size are randomly allocated into the treatment groups: i) Placebo; ii) Lurbinectedin (0.18 mg/kg); iii) NSC 119875 (3.5 mg/kg); and iv) Lurbinectedin plus NSC 119875 (0.18 + 3.5 mg/kg). Drugs are i.v. administered once per week for 3 consecutive weeks (days 0, 7, and 14). Seven days after the final dose (day 21), animals are sacrificed, their ovaries dissected out, and weighed. Representative fragments are either frozen in nitrogen or fixed and then processed for paraffin embedding[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References

Purity: 99.73%

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Keywords:

LurbinectedinPM01183PM 01183PM-01183DNA Alkylator/CrosslinkerDNA/RNA SynthesisInhibitorinhibitorinhibit

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Lurbinectedin
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