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MedKoo Cat#: 561124 | Name: Pamiparib free base
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

Pamiparib, also known as BGB-290, is a highly potent and selective PARP inhibitor with favorable drug metabolism and pharmacokinetic properties. BGB-290 selectively binds to PARP and prevents PARP-mediated repair of single-strand DNA breaks via the base-excision repair (BER) pathway. This enhances the accumulation of DNA strand breaks, promotes genomic instability, and eventually leads to apoptosis. BGB-290 may both potentiate the cytotoxicity of DNA-damaging agents and reverse tumor cell chemo- and radioresistance.

Chemical Structure

Pamiparib free base
Pamiparib free base
CAS#1446261-44-4 (free base)

Theoretical Analysis

MedKoo Cat#: 561124

Name: Pamiparib free base

CAS#: 1446261-44-4 (free base)

Chemical Formula: C16H15FN4O

Exact Mass: 298.1230

Molecular Weight: 298.32

Elemental Analysis: C, 64.42; H, 5.07; F, 6.37; N, 18.78; O, 5.36

Price and Availability

Size Price Availability Quantity
10mg USD 150.00 Ready to ship
25mg USD 250.00 Ready to ship
50mg USD 450.00 Ready to ship
100mg USD 750.00 Ready to ship
200mg USD 1,250.00 Ready to ship
500mg USD 2,650.00 Ready to ship
1g USD 3,850.00 Ready to ship
2g USD 6,450.00 Ready to ship
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Related CAS #
1858211-28-5 (hydrate) 1446261-44-4 (free base) 2243699-99-0 (maleate) 2243700-03-8 (fumarate)
Synonym
Pamiparib; BGB-290; BGB 290; BGB290.
IUPAC/Chemical Name
(10aR)-2-fluoro-10a-methyl-5,8,9,10,10a,11-hexahydro-5,6,7a,11-tetraazacyclohepta[def]cyclopenta[a]fluoren-4(7H)-one
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
SMILES Code
O=C1NN=C2CN(CCC3)[C@@]3(C)C(N4)=C2C5=C4C=C(F)C=C51
Appearance
Solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
Biological target:
Pamiparib (BGB-290) is an orally active, potent, highly selective PARP inhibitor, with IC50 values of 0.9 nM and 0.5 nM for PARP1 and PARP2, respectively.
In vitro activity:
Further detection of cell cycle distribution by flow cytometry revealed that SW1990 cells were significantly blocked in G2/M phase upon pamiparib treatment in a time-dependent manner (all P values less than 0.01; Figure 1B). This suggests that pamiparib can significantly induce apoptosis and block cell cycle progression of pancreatic cancer cells in vitro. Reference: Front Immunol. 2021 Dec 17;12:762989. https://pubmed.ncbi.nlm.nih.gov/34975854/
In vivo activity:
Then, the PD effect of pamiparib was evaluated in vivo by directly measurement of PAR level in tumor site. MDA-MB-436 xenograft mice were treated once orally with the vehicle or pamiparib, at a dose ranging from 0.17 to 10.9 mg/kg. A single dose of pamiparib at 1.5 mg/kg induced 89% PARylation inhibition at 0.5 h post treatment which remained at ∼81% throughout the first 12 h. Meanwhile a single dose of olaparib at 25 mg/kg induced ∼100% PARylation inhibition but dropped to 72% by 12 h post treatment. These results suggest that pamiparib exhibits approximately 16-fold higher efficacy than olaparib in this model, likely due to higher drug exposure in body. Reference: Neoplasia. 2020 Sep;22(9):431-440. https://pubmed.ncbi.nlm.nih.gov/32652442/
Solvent mg/mL mM
Solubility
DMF 20.0 67.04
DMF:PBS (pH 7.2) (1:10) 0.1 0.30
DMSO 40.8 136.88
Ethanol 45.0 150.84
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 298.32 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Wang Y, Zheng K, Xiong H, Huang Y, Chen X, Zhou Y, Qin W, Su J, Chen R, Qiu H, Yuan X, Wang Y, Zou Y. PARP Inhibitor Upregulates PD-L1 Expression and Provides a New Combination Therapy in Pancreatic Cancer. Front Immunol. 2021 Dec 17;12:762989. doi: 10.3389/fimmu.2021.762989. PMID: 34975854; PMCID: PMC8718453. 2. Xiong Y, Guo Y, Liu Y, Wang H, Gong W, Liu Y, Wang X, Gao Y, Yu F, Su D, Wang F, Zhu Y, Zhao Y, Wu Y, Qin Z, Sun X, Ren B, Jiang B, Jin W, Shen Z, Tang Z, Song X, Wang L, Liu X, Zhou C, Jiang B. Pamiparib is a potent and selective PARP inhibitor with unique potential for the treatment of brain tumor. Neoplasia. 2020 Sep;22(9):431-440. doi: 10.1016/j.neo.2020.06.009. Epub 2020 Jul 8. PMID: 32652442; PMCID: PMC7350150.
In vitro protocol:
1. Wang Y, Zheng K, Xiong H, Huang Y, Chen X, Zhou Y, Qin W, Su J, Chen R, Qiu H, Yuan X, Wang Y, Zou Y. PARP Inhibitor Upregulates PD-L1 Expression and Provides a New Combination Therapy in Pancreatic Cancer. Front Immunol. 2021 Dec 17;12:762989. doi: 10.3389/fimmu.2021.762989. PMID: 34975854; PMCID: PMC8718453. 2. Xiong Y, Guo Y, Liu Y, Wang H, Gong W, Liu Y, Wang X, Gao Y, Yu F, Su D, Wang F, Zhu Y, Zhao Y, Wu Y, Qin Z, Sun X, Ren B, Jiang B, Jin W, Shen Z, Tang Z, Song X, Wang L, Liu X, Zhou C, Jiang B. Pamiparib is a potent and selective PARP inhibitor with unique potential for the treatment of brain tumor. Neoplasia. 2020 Sep;22(9):431-440. doi: 10.1016/j.neo.2020.06.009. Epub 2020 Jul 8. PMID: 32652442; PMCID: PMC7350150.
In vivo protocol:
1. Wang Y, Zheng K, Xiong H, Huang Y, Chen X, Zhou Y, Qin W, Su J, Chen R, Qiu H, Yuan X, Wang Y, Zou Y. PARP Inhibitor Upregulates PD-L1 Expression and Provides a New Combination Therapy in Pancreatic Cancer. Front Immunol. 2021 Dec 17;12:762989. doi: 10.3389/fimmu.2021.762989. PMID: 34975854; PMCID: PMC8718453. 2. Xiong Y, Guo Y, Liu Y, Wang H, Gong W, Liu Y, Wang X, Gao Y, Yu F, Su D, Wang F, Zhu Y, Zhao Y, Wu Y, Qin Z, Sun X, Ren B, Jiang B, Jin W, Shen Z, Tang Z, Song X, Wang L, Liu X, Zhou C, Jiang B. Pamiparib is a potent and selective PARP inhibitor with unique potential for the treatment of brain tumor. Neoplasia. 2020 Sep;22(9):431-440. doi: 10.1016/j.neo.2020.06.009. Epub 2020 Jul 8. PMID: 32652442; PMCID: PMC7350150.
1: Li N, Yan Y, Li Y, Yang Y, Dai C, Li N. ATM, BLM, and CDH1 gene co-mutations in a high-grade endometrial stromal sarcoma patient with multiple abdominal cavity metastases: a case report and literature review. BMC Geriatr. 2024 Jul 15;24(1):603. doi: 10.1186/s12877-024-05201-z. PMID: 39009979; PMCID: PMC11247777. 2: Stradella A, Johnson M, Goel S, Park H, Lakhani N, Arkenau HT, Galsky MD, Calvo E, Baz V, Moreno V, Saavedra O, Luen SJ, Mu S, Wan Q, Chang V, Zhang W, Barve M. Phase 1b study to assess the safety, tolerability, and clinical activity of pamiparib in combination with temozolomide in patients with locally advanced or metastatic solid tumors. Cancer Med. 2024 Jul;13(13):e7385. doi: 10.1002/cam4.7385. PMID: 38970256; PMCID: PMC11226541. 3: Duaa SU, Fatima E, Qureshi Z. Pamiparib, A Novel Intervention with Anti- neoplastic Activity for the Treatment of Glioblastoma. Am J Med Sci. 2024 Jul 3:S0002-9629(24)01341-7. doi: 10.1016/j.amjms.2024.07.007. Epub ahead of print. PMID: 38969284. 4: Xu Y, Xiong F, Li H, Zheng H, Jiang J, Li Q, Li G, Zhao W, Li R, Li J, Xie R, An R, Zhang H, Gao Q. Biomarker-driven targeted therapy in patients with recurrent platinum-resistant epithelial ovarian cancer (BRIGHT): protocol for an open-label, multicenter, umbrella study. Int J Gynecol Cancer. 2024 Apr 23:ijgc-2024-005351. doi: 10.1136/ijgc-2024-005351. Epub ahead of print. PMID: 38658024. 5: Mao J, Ni J, Chu L, Chu X, Xu D, Yang X, Zhu Z. Pamiparib as consolidation treatment after concurrent chemoradiotherapy of limited-stage small cell lung cancer: a single-arm, open-label phase 2 trial. Radiat Oncol. 2024 Apr 12;19(1):47. doi: 10.1186/s13014-024-02437-2. PMID: 38610031; PMCID: PMC11010395. 6: Liu F, Chen J, Li X, Liu R, Zhang Y, Gao C, Shi D. Advances in Development of Selective Antitumor Inhibitors That Target PARP-1. J Med Chem. 2023 Dec 28;66(24):16464-16483. doi: 10.1021/acs.jmedchem.3c00865. Epub 2023 Dec 13. PMID: 38088333. 7: Zeng Y, Arisa O, Peer CJ, Fojo A, Figg WD. PARP inhibitors: A review of the pharmacology, pharmacokinetics, and pharmacogenetics. Semin Oncol. 2024 Feb- Apr;51(1-2):19-24. doi: 10.1053/j.seminoncol.2023.09.005. Epub 2023 Oct 14. PMID: 37880048; PMCID: PMC11016131. 8: Wei Y, Liang H, Liu S, Guan S, Ma K, Guan Y, Chen Y, Huang M, Wang X, Lan C. Development and validation of a sensitive LC-MS/MS method for the assay of four PARP inhibitors in human plasma and its application in ovarian cancer patients. J Pharm Biomed Anal. 2024 Jan 5;237:115758. doi: 10.1016/j.jpba.2023.115758. Epub 2023 Oct 2. PMID: 37832476. 9: Vollmer J, Ecker J, Hielscher T, Valinciute G, Ridinger J, Jamaladdin N, Peterziel H, van Tilburg CM, Oehme I, Witt O, Milde T. Class I HDAC inhibition reduces DNA damage repair capacity of MYC-amplified medulloblastoma cells. J Neurooncol. 2023 Sep;164(3):617-632. doi: 10.1007/s11060-023-04445-w. Epub 2023 Oct 3. PMID: 37783879; PMCID: PMC10589189. 10: Friedlander M, Mileshkin L, Lombard J, Frentzas S, Gao B, Wilson M, Meniawy T, Baron-Hay S, Briscoe K, McCarthy N, Fountzilas C, Cervantes A, Ge R, Wu J, Spira A. Pamiparib in combination with tislelizumab in patients with advanced solid tumours: results from the dose-expansion stage of a multicentre, open- label, phase I trial. Br J Cancer. 2023 Sep;129(5):797-810. doi: 10.1038/s41416-023-02349-0. Epub 2023 Jul 20. PMID: 37474720; PMCID: PMC10449784. 11: Ciardiello F, Bang YJ, Cervantes A, Dvorkin M, Lopez CD, Metges JP, Sánchez Ruiz A, Calvo M, Strickland AH, Kannourakis G, Muro K, Kawakami H, Wei J, Borg C, Zhu Z, Gupta N, Pelham RJ, Shen L. Efficacy and safety of maintenance therapy with pamiparib versus placebo for advanced gastric cancer responding to first- line platinum-based chemotherapy: Phase 2 study results. Cancer Med. 2023 Jun;12(12):13145-13154. doi: 10.1002/cam4.5997. Epub 2023 Jun 1. PMID: 37260158; PMCID: PMC10315793. 12: Murai J, Pommier Y. BRCAness, Homologous Recombination Deficiencies, and Synthetic Lethality. Cancer Res. 2023 Apr 14;83(8):1173-1174. doi: 10.1158/0008-5472.CAN-23-0628. PMID: 37057596. 13: Huang X, He X, Li D, Chen X, Chen X. Advanced ovarian clear cell carcinoma with RAD50 mutation treated by PARP inhibitor pamiparib combined with anti- angiogenesis therapy: a case report. Anticancer Drugs. 2023 Feb 1;34(2):290-293. doi: 10.1097/CAD.0000000000001412. Epub 2022 Nov 15. PMID: 36729997; PMCID: PMC9815817. 14: Xu B, Sun T, Shi Y, Cui J, Yin Y, Ouyang Q, Liu Q, Zhang Q, Chen Y, Wang S, Wang X, Tong Z, Zhong Y, Wang J, Yan M, Yan X, Wang C, Feng J, Wang X, Hu G, Cheng Y, Ge R, Zhu Z, Zhang W, Shao Z. Pamiparib in patients with locally advanced or metastatic HER2-negative breast cancer with germline BRCA mutations: a phase II study. Breast Cancer Res Treat. 2023 Feb;197(3):489-501. doi: 10.1007/s10549-022-06785-z. Epub 2022 Dec 2. PMID: 36459284; PMCID: PMC9883365. 15: Smith HL, Willmore E, Mukhopadhyay A, Drew Y, Curtin NJ. Differences in Durability of PARP Inhibition by Clinically Approved PARP Inhibitors: Implications for Combinations and Scheduling. Cancers (Basel). 2022 Nov 12;14(22):5559. doi: 10.3390/cancers14225559. PMID: 36428653; PMCID: PMC9688250. 16: Haase S, Banerjee K, Mujeeb AA, Hartlage CS, Núñez FM, Núñez FJ, Alghamri MS, Kadiyala P, Carney S, Barissi MN, Taher AW, Brumley EK, Thompson S, Dreyer JT, Alindogan CT, Garcia-Fabiani MB, Comba A, Venneti S, Ravikumar V, Koschmann C, Carcaboso ÁM, Vinci M, Rao A, Yu JS, Lowenstein PR, Castro MG. H3.3-G34 mutations impair DNA repair and promote cGAS/STING-mediated immune responses in pediatric high-grade glioma models. J Clin Invest. 2022 Nov 15;132(22):e154229. doi: 10.1172/JCI154229. PMID: 36125896; PMCID: PMC9663161. 17: Yang D, Liu F, Wan M, Liu J, Huang L, Chen C, Li X, Zhang L, Ding X, Liao X, Xiong G, Lu H, Xiao J, Cao Z. Pamiparib Induces Neurodevelopmental Defects and Cerebral Haemorrhage in Zebrafish Embryos via Inhibiting Notch Signalling. Mol Neurobiol. 2022 Nov;59(11):6652-6665. doi: 10.1007/s12035-022-02988-z. Epub 2022 Aug 19. PMID: 35982279. 18: Jiang J, Bao X, Yue Y, Schiff D, Bindra R, Li J. Development and validation of a liquid chromatography coupled with tandem mass spectrometry method for determining total and unbound pamiparib in human plasma and brain tumors. Biomed Chromatogr. 2022 Dec;36(12):e5478. doi: 10.1002/bmc.5478. Epub 2022 Aug 19. PMID: 35938683; PMCID: PMC10316684. 19: Skrzypczyk-Ostaszewicz A. Pamiparib for germline BRCA mutation-associated recurrent advanced ovarian, fallopian tube or primary peritoneal cancer. Drugs Today (Barc). 2022 Jun;58(6):299-309. doi: 10.1358/dot.2022.58.6.3389001. PMID: 35670707. 20: Luo L, Keyomarsi K. PARP inhibitors as single agents and in combination therapy: the most promising treatment strategies in clinical trials for BRCA- mutant ovarian and triple-negative breast cancers. Expert Opin Investig Drugs. 2022 Jun;31(6):607-631. doi: 10.1080/13543784.2022.2067527. Epub 2022 May 3. PMID: 35435784; PMCID: PMC9296104.

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