Pamiparib free base
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MedKoo CAT#: 561124

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

Description: 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

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Pamiparib free base
CAS# 1446261-44-4 (free base)
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 561124
Name: Pamiparib free base
CAS#: 1446261-44-4 (free base)
Chemical Formula: C16H15FN4O
Exact Mass: 298.12
Molecular Weight: 298.321
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 Ready to ship
25mg USD 250 Ready to ship
50mg USD 450 Ready to ship
100mg USD 750 Ready to ship
200mg USD 1250 Ready to ship
500mg USD 2650 Ready to ship
1g USD 3850 Ready to ship
2g USD 6450 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/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. 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

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.

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