Pamiparib

SKU: orb1302131

Description

Pamiparib (BGB-290) is a potent, brain-penetrant, and selective PARP1/2 inhibitor with strong PARP-trapping activity. It is widely used in preclinical cancer research, demonstrating efficacy in both in vitro assays and in vivo models for solid tumors, including those with central nervous system involvement.

Research Area

Epigenetics & Chromatin, Molecular Biology

Key Properties

• CAS Number: 1446261-44-4
• MW: 298.31
• Purity: 99.53% (May vary between batches)
• Formula: C₁₆H₁₅FN₄O
• SMILES: C[C@]12CCCN1Cc1n[nH]c(=O)c3cc(F)cc4[nH]c2c1c34
• Target: PARP
• Solubility: DMSO:62.5 mg/mL (209.51 mM);10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (6.7 mM)

Bioactivity

• Target IC50:
  PARP1:0.9 nM|PARP2:0.5 nM
• In Vivo:
  Pamiparib, an investigational Poly (ADP-ribose) polymerase (PARP) inhibitor in clinical development, demonstrates excellent selectivity for both PARP1 and PARP2, and superb anti-proliferation activities in tumor cell lines with BRCA1/2 mutations or HR pathway deficiency (HRD). Pamiparib has good bioavailability and is 16-fold more potent than olaparib in an efficacy study using BRCA1 mutated MDA-MB-436 breast cancer xenograft model. Pamiparib also shows strong anti-tumor synergy with temozolomide (TMZ), a DNA alkylating agent used to treat brain tumors. Compared to other PARP inhibitors, pamiparib demonstrated improved penetration across the blood brain barrier (BBB) in mice. Oral administration of pamiparib at a dose as low as 3 mg/kg is sufficient to abrogate PARylation in brain tumor tissues. In SCLC-derived, TMZ-resistant H209 intracranial xenograft model, combination of pamiparib with TMZ overcomes its resistance and shows significant tumor inhibitory effects and prolonged life span.
  Read more...

Storage & Handling

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

Alternative Names

BGB290, BGB-290, BGB 290, Inhibitor, inhibit, Pamiparib, PARP, PARP1, PARP2, poly ADP ribose polymerase

Compound Identifiers

PubChem CID

135565554