Pamiparib

Alias: BGB-290; BGB 290; BGB290
Cat No.:V3280 Purity: ≥98%
Pamiparib (also known as BGB-290; trade name in China: Baihuize) is a novel, potent and selective inhibitor of PARP1/2 approved in China for cancer treatment.
Pamiparib Chemical Structure CAS No.: 1446261-44-4
Product category: PARP
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description

Pamiparib (also known as BGB-290; trade name in China: Baihuize) is a novel, potent and selective inhibitor of PARP1/2 approved in China for cancer treatment. It uses a mechanism known as "synthetic lethality" to destroy tumor cells. Compared to other PARP enzymes, dapagliparib exhibits a high degree of selectivity. Its DMPK (drug metabolism and pharmacokinetic) profiles are favorable. Using the base-excision repair (BER) pathway, pampiparib binds to PARP specifically and inhibits PARP from repairing single-strand DNA breaks. This process increases the accumulation of DNA strand breaks, causes genomic instability, and ultimately results in apoptosis. Pamiparib has the ability to counteract tumor cells' resistance to chemotherapy and radiation, as well as increase the cytotoxicity of agents that damage DNA.

Biological Activity I Assay Protocols (From Reference)
Targets
PARP2 ( IC50 = 0.11 nM ); PARP1 ( IC50 = 0.83 nM )
ln Vitro

In vitro activity: Pamiparib has a 13 nM IC50 and exhibits strong DNA-trapping activity. With an IC50 of 0.24 nM, Pamiparib prevents intracellular PAR formation in the cellular experiments. Pamiparib has a strong affinity for tumor cell lines that have homologous recombination defects in them. In BRCA mutant tumors, paramiparib exhibits high levels of activity both in vitro and in vivo[3].

ln Vivo
Pamiparib reduces PARP activity in xenografts of small-cell lung cancer and glioblastoma multiforme derived from patients, and enhances the effects of temozolomide. Pamiparib's in vivo properties in patient biopsy-derived small cell lung cancer (SCLC) xenograft models, as well as its combination activity with chemotherapy[4].
Enzyme Assay
BGB-290 showed excellent selectivity over other PARP enzymes and significant potency for PARP1/2 (IC50 = 0.83 and 0.11 nM, respectively) in the biochemical tests. The assay used to measure BGB-290's DNA-trapping activity was the fluorescence polarization (FP) binding method. BGB-290 exhibited a strong ability to trap DNA, with an IC50 of 13 nM. BGB-290 inhibited intracellular PAR formation in the cellular assays, with an IC50 of 0.24 nM. BGB-290 had a strong effect on tumor cell lines with homologous recombination defects. In an MDA-MB-436 (BRCA1 mutant) breast cancer xenograft, oral administration of BGB-290 led to time- and dose-dependent inhibition of PARylation, which correlated well with the tumor drug concentrations. BGB-290 produced PAR inhibition that was more persistent than olaparib. BGB-290 showed remarkable anti-tumor activity in this model, more than ten times more potent than olaparib, which is consistent with this finding.
Cell Assay
Three of the seven SCLC cell lines that were tested showed sensitivity to BGB-290. Using patient biopsy samples from Beijing Cancer Hospital, internal SCLC primary tumor models were created. Eight primary tumor models of SCLC were used to assess the anti-tumor activities of BGB-290, either alone or in conjunction with etoposide/carboplatin (E/C). In these models, BGB-290 exhibited only marginal single agent activity. In line with the clinical response seen in these patients, six of the eight models (or75%) showed sensitivity to E/C treatment. In these chemo-sensitive models, the addition of BGB-290 as maintenance therapy or concurrent treatment greatly extended the duration of the response. BGB-290 and E/C combo had less of an impact in the two chemo-insensitive models. Throughout the trial, BGB-290 was well tolerated as an addition to the chemotherapy regimen.
Animal Protocol

8 SCLC primary tumor models.
References

[1]. Fused tetra or penta-cyclic dihydrodiazepinocarbazolones as parp inhibitors. WO 2013097225 A1.

[2]. 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]. Abstract 1653: BGB-290: A highly potent and specific PARP1/2 inhibitor potentiates anti-tumor activity of chemotherapeutics in patient biopsy derived SCLC models. Cancer Research. August 2015, Volume 75, Issue 15.

[4]. 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.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C16H15FN4O
Molecular Weight
298.31
Exact Mass
298.12
Elemental Analysis
C, 64.42; H, 5.07; F, 6.37; N, 18.78; O, 5.36
CAS #
1446261-44-4
Appearance
Solid powder
SMILES
C[C@]12CCCN1CC3=NNC(=O)C4=C5C3=C2NC5=CC(=C4)F
InChi Key
DENYZIUJOTUUNY-MRXNPFEDSA-N
InChi Code
InChI=1S/C16H15FN4O/c1-16-3-2-4-21(16)7-11-13-12-9(15(22)20-19-11)5-8(17)6-10(12)18-14(13)16/h5-6,18H,2-4,7H2,1H3,(H,20,22)/t16-/m1/s1
Chemical Name
(2R)-14-fluoro-2-methyl-6,9,10,19-tetrazapentacyclo[14.2.1.02,6.08,18.012,17]nonadeca-1(18),8,12(17),13,15-pentaen-11-one
Synonyms
BGB-290; BGB 290; BGB290
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO: 50~60 mg/mL
Water: <1mg/mL
Ethanol: >40 mg/mL
Solubility (In Vivo)
5%DMSO+ 40%PEG300+ 5%Tween 80+ 50%ddH2O: 3.0mg/ml (10.06mM) (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.3522 mL 16.7611 mL 33.5222 mL
5 mM 0.6704 mL 3.3522 mL 6.7044 mL
10 mM 0.3352 mL 1.6761 mL 3.3522 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
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Clinical Trial Information
NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05376722 Recruiting Drug: pamiparib
Drug: abiraterone
Neoadjuvant Therapy Hongqian Guo February 22, 2022 Phase 2
NCT05494580 Recruiting Drug: Pamiparib
Drug: Surufatinib
Ovarian Cancer
Ovarian Carcinoma
Sun Yat-sen University September 22, 2022 Phase 1
Phase 2
NCT04614909 Recruiting Drug: Pamiparib
Drug: Olaparib
Glioblastoma
Glioblastoma Multiforme
Nader Sanai January 11, 2021 Early Phase 1
NCT04985721 Recruiting Drug: Pamiparib
Drug: Tislelizumab
Cancer Peter MacCallum Cancer Centre,
Australia
February 24, 2022 Phase 2
NCT05044871 Not yet recruiting Drug: Pamiparib
Drug: Bevacizumab
Ovarian Cancer Tongji Hospital January 1, 2023 Phase 2
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