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Pamiparib

Catalog No. T5058 CAS 1446261-44-4

Synonyms: BGB-290

Pamiparib (BGB-290) is an orally active, potent, highly selective PARP inhibitor(IC50 of 0.9 nM and 0.5 nM for PARP1 and PARP2, respectively). It has potent PARP trapping, and capability to penetrate the brain, and can be used for the research of various cancers including the solid tumor

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Pamiparib, CAS 1446261-44-4

Pack Size	Availability	Price/USD
1 mg	In stock	$ 30.00
2 mg	In stock	$ 40.00
5 mg	In stock	$ 50.00
25 mg	In stock	Inquiry
50 mg	In stock	Inquiry
1 mL * 10 mM (in DMSO)	In stock	$ 58.00

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Purity: 99.53%

Biological Description

Chemical Properties

Storage & Solubility Information

Description	Pamiparib (BGB-290) is an orally active, potent, highly selective PARP inhibitor(IC50 of 0.9 nM and 0.5 nM for PARP1 and PARP2, respectively). It has potent PARP trapping, and capability to penetrate the brain, and can be used for the research of various cancers including the solid tumor
Targets&IC50	PARP2:0.5 nM, PARP1:0.9 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[1].

Synonyms	BGB-290
Molecular Weight	298.31
Formula	C16H15FN4O
CAS No.	1446261-44-4

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 62.5 mg/mL (209.51 mM), Sonication is recommended.

References and Literature

1. Xiong Y , Guo Y , Liu Y , et al. Pamiparib is a potent and selective PARP inhibitor with unique potential for the treatment of brain tumor[J]. Neoplasia (New York, N.Y.), 2020, 22(9):431-440. 2. Friedlander M, et al. Pamiparib in combination with tislelizumab in patients with advanced solid tumours: results from the dose-escalation stage of a multicentre, open-label, phase 1a/b trial. Lancet Oncol. 2019 Sep;20(9):1306-1315. 3. Shiv K. Gupta, et al. Abstract 3505: Inhibition of PARP activity by BGB-290 potentiates efficacy of NSC 362856 in patient derived xenografts of glioblastoma multiforme. Cancer Research. August 2015, Volume 75, Issue 15

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Highly Selective Inhibitor Library Anti-Cancer Active Compound Library Inhibitor Library Drug Repurposing Compound Library Anti-Cancer Drug Library Anti-Cancer Approved Drug Library Bioactive Compounds Library Max Anti-Cancer Compound Library Orally Active Compound Library

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Keywords

Pamiparib 1446261-44-4 Chromatin/Epigenetic DNA Damage/DNA Repair PARP inhibit Inhibitor BGB-290 poly ADP ribose polymerase BGB 290 BGB290 inhibitor

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