Pamiparib

SKU: orb1226263

Description

Pamiparib (BGB-290, BGB290) is a highly potent, selective and brain penetrant PARP1/2 inhibitor with potent anti-tumor activity.Ovarian Cancer Phase 2 Clinical(In Vitro):Pamiparib shows potent DNA-trapping activity with an IC50 of 13 nM. In the cellular assays, Pamiparib inhibits intracellular PAR formation with an IC50 of 0.24 nM. Tumor cell lines with homologous recombination defects are profoundly sensitive to Pamiparib. Pamiparib is highly active both in vitro and in vivo in BRCA mutant tumors.(In Vivo):Pamiparib suppresses PARP activity in patient-derived glioblastoma multiforme and small-cell-lung cancer xenografts, and potentiates the effects of Temozolamide. In vivo activities of Pamiparib, and its combination activity with chemotherapies in patient biopsy derived small cell lung cancer (SCLC) xenograft models.

Key Properties

• CAS Number: 1446261-44-4
• MW: 298.32
• Purity: >98% (HPLC)
• Formula: C₁₆H₁₅FN₄O
• SMILES: CC12CCCN1CC3=NNC(=O)C4=C5C3=C2NC5=CC(=C4)F
• Target: PARP
• Solubility: DMSO : 83.3 mg/mL 279.24 mM

Bioactivity

• In Vivo:
  Pamiparib suppresses PARP activity in patient-derived glioblastoma multiforme and small-cell-lung cancer xenografts, and potentiates the effects of Temozolamide. In vivo activities of Pamiparib, and its combination activity with chemotherapies in patient biopsy derived small cell lung cancer (SCLC) xenograft models.
• In Vitro:
  Pamiparib shows potent DNA-trapping activity with an IC50 of 13 nM. In the cellular assays, Pamiparib inhibits intracellular PAR formation with an IC50 of 0.24 nM. Tumor cell lines with homologous recombination defects are profoundly sensitive to Pamiparib. Pamiparib is highly active both in vitro and in vivo in BRCA mutant tumors.

Storage & Handling

• Storage: Storage temperature: -20°C. Stability: ≥ 2 years
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BGB-290 | BGB 290

Quick Database Links

Gene Symbol

PARP