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Lurbinectedin (Synonyms: PM01183)

Cat. No.: HY-16293 Purity: 96.81%
Handling Instructions

Lurbinectedin (PM01183) is a new 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

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 14504 In-stock
Stock in the United States
Estimated Time of Arrival: December 31
1 mg USD 1800 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
2 mg USD 3360 In-stock
Stock in Sweden
Estimated Time of Arrival: December 31
5 mg   Get quote  
10 mg   Get quote  

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Customer Review

  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

Lurbinectedin (PM01183) is a new 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 cisplatin-combined therapies are effective in treating cisplatin-sensitive and cisplatin-resistant preclinical ovarian tumor models. The strongest synergistic effect is observed for combined treatments, especially in cisplatin-resistant tumors. Lurbinectedin tumor growth inhibition is associated with reduced proliferation, increased rate of aberrant mitosis, and subsequent induced apoptosis[3].

Clinical Trial
References
Preparing Stock Solutions
Concentration Volume Mass 1 mg 5 mg 10 mg
1 mM 1.2741 mL 6.3705 mL 12.7410 mL
5 mM 0.2548 mL 1.2741 mL 2.5482 mL
10 mM 0.1274 mL 0.6370 mL 1.2741 mL
Please refer to the solubility information to select the appropriate solvent.
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) Cisplatin (3.5 mg/kg); and iv) Lurbinectedin plus cisplatin (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
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

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO: 10 mM

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

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Product Name:
Lurbinectedin
Cat. No.:
HY-16293
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