Pamiparib (BGB-290) - Moligand™, ≥99% , Poly [ADP-ribose] polymerase 2 inhibitor, CAS No.1446261-44-4, Poly [ADP-ribose] polymerase 2 inhibitor

CAS: 1446261-44-4 Cat. No.: P414075 Molecular Weight: 298.31 PubChem CID: 135565554

GRADE & PURITY Moligand™, ≥99%

Synonyms

(10aR)-2-Fluoro-10a-methyl-5,8,9,10,10a,11-hexahydro-5,6,7a,11-tetraazacyclohepta(1,2,3,4-def)cyclopenta(a)fluoren-4(7H)-one | A884779 | Pamiparib [INN] | BP180190 | DENYZIUJOTUUNY-MRXNPFEDSA-N | Pamiparib (BGB-290) | Q2701649 | Pamiparib free base | SCHE

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

Overview

Information

Pamiparib (BGB-290) is a potent and selective inhibitor ofPARP1andPARP2with IC50 values of 0.83 and 0.11 nM, respectively in biochemical assays. It shows high selectivity over other PARP enzymes.

Targets

PARP2 (Cell-free assay); PARP1 (Cell-free assay) 0.11 nM; 0.83 nM

In vitro

BGB-290 shows potent DNA-trapping activity with IC50 of 13 nM. In the cellular assays, BGB-290 inhibits intracellular PAR formation with an IC50 of 0.24 nM.

In vivo

Oral administration of BGB-290 results in time-dependent and dose-dependent inhibition of PARylation in MDA-MB-436 (BRCA1 mutant) breast cancer xenograft, correlating well with the tumor drug concentrations. BGB-290 has also demonstrated good combination activity with chemotherapeutics in patient biopsy derived SCLC models. BGB-290 has significant brain penetration in C57 mice. The drug exposure in brain vs. that in plasma was close to 20% after oral administration of BGB-290.

Product Application：

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.

Specifications

Synonyms

(10aR)-2-Fluoro-10a-methyl-5, 8, 9, 10, 10a, 11-hexahydro-5, 6, 7a, 11-tetraazacyclohepta(1, 2, 3, 4-def)cyclopenta(a)fluoren-4(7H)-one | A884779 | Pamiparib [INN] | BP180190 | DENYZIUJOTUUNY-MRXNPFEDSA-N | Pamiparib (BGB-290) | Q2701649 | Pamiparib free base | SCHE

Specifications & Purity

Moligand™, ≥99%

Biochemical and Physiological Mechanisms

Pamiparib (BGB-290) is a potent and selective inhibitor of PARP1 and PARP2 with IC50 values of 0.83 and 0.11 nM, respectively in biochemical assays. It shows high selectivity over other PARP enzymes.

Storage

Store at -20°C

Shipped In

Ice chest + Ice pads

This product requires cold chain shipping. Ground and other economy services are not available.

Grade

Moligand™

Action Type

INHIBITOR

Mechanism of action

Poly [ADP-ribose] polymerase 2 inhibitor

Purity

≥99%

Product Properties

• ALogP: 2.078
• HBD Count: 2

Names and Identifiers

• Pubchem Sid: 504773392
• Pubchem Sid Url: https://pubchem.ncbi.nlm.nih.gov/substance/504773392
• Canonical Smiles: CC12CCCN1CC3=NNC(=O)C4=C5C3=C2NC5=CC(=C4)F
• IUPAC 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
• InChIKey: DENYZIUJOTUUNY-MRXNPFEDSA-N
• 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
• Isomeric SMILES: C[C@]12CCCN1CC3=NNC(=O)C4=C5C3=C2NC5=CC(=C4)F
• PubChem CID: 135565554
• Molecular Weight: 298.31

Taxonomic Classification

Taxonomy Tree

• Kingdom Organic compounds
  • Superclass Organoheterocyclic compounds
    • Class Indoles and derivatives
      • Subclass Pyridoindoles

• Kingdom: Organic compounds
• Superclass: Organoheterocyclic compounds
• Class: Indoles and derivatives
• Subclass: Pyridoindoles
• Intermediate Tree Nodes: Not available
• Direct Parent: Beta carbolines
• Alternative Parents: Indoles Aralkylamines N-alkylpyrrolidines Benzenoids Aryl fluorides Pyrroles Heteroaromatic compounds Trialkylamines Lactams Azacyclic compounds Organopnictogen compounds Organooxygen compounds Organofluorides Organic oxides Hydrocarbon derivatives
• Molecular Framework: Aromatic heteropolycyclic compounds
• Substituents: Beta-carboline - Indole - Aralkylamine - Benzenoid - N-alkylpyrrolidine - Aryl halide - Aryl fluoride - Heteroaromatic compound - Pyrrolidine - Pyrrole - Tertiary aliphatic amine - Tertiary amine - Lactam - Azacycle - Organic nitrogen compound - Organic oxygen compound - Organopnictogen compound - Organic oxide - Hydrocarbon derivative - Organooxygen compound - Organonitrogen compound - Organofluoride - Organohalogen compound - Amine - Aromatic heteropolycyclic compound
• Description: This compound belongs to the class of organic compounds known as beta carbolines. These are compounds containing a 9H-pyrido[3,4-b]indole moiety.
• External Descriptors: Not available

Data sources

1. Djoumbou Feunang Y, Eisner R, Knox C, Chepelev L, Hastings J, Owen G, Fahy E, Steinbeck C, Subramanian S, Bolton E, Greiner R, and Wishart DS. ClassyFire: Automated Chemical Classification With A Comprehensive, Computable Taxonomy. Journal of Cheminformatics, 2016, 8:61.

DOI: 10.1186/s13321-016-0174-y

Associated Targets(Human)

TNKS Tchem Tankyrase-1 (1 Activities)

Discover Target: TNKS

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PARP3 Tclin Poly [ADP-ribose] polymerase 3 (2 Activities)

Discover Target: PARP3

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PARP1 Tclin Poly [ADP-ribose] polymerase 1 (4 Activities)

Discover Target: PARP1

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

PARP2 Tclin Poly [ADP-ribose] polymerase 2 (2 Activities)

Discover Target: PARP2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

TNKS2 Tchem Tankyrase-2 (2 Activities)

Discover Target: TNKS2

Activity Type	Activity Value -log(M)	Mechanism of Action	Activity Reference	Publications (PubMed IDs)

KCNH2 Tclin HERG (29587 Activities)

Discover Target: KCNH2

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

CYP2C8 Tchem Cytochrome P450 2C8 (1492 Activities)

Discover Target: CYP2C8

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

CYP2D6 Tclin Cytochrome P450 2D6 (33882 Activities)

Discover Target: CYP2D6

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

PARP1 Tclin Poly [ADP-ribose] polymerase-1 (6206 Activities)

Discover Target: PARP1

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

CYP1A2 Tchem Cytochrome P450 1A2 (26471 Activities)

Discover Target: CYP1A2

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

CYP2C9 Tchem Cytochrome P450 2C9 (32119 Activities)

Discover Target: CYP2C9

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

CYP2C19 Tchem Cytochrome P450 2C19 (29246 Activities)

Discover Target: CYP2C19

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

CYP3A4 Tclin Cytochrome P450 3A4 (53859 Activities)

Discover Target: CYP3A4

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

SK-BR-3 (5175 Activities)

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Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

MDA-MB-231 (73002 Activities)

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Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

PARP2 Tclin Poly [ADP-ribose] polymerase 2 (1185 Activities)

Discover Target: PARP2

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

ABCG2 Tchem ATP-binding cassette sub-family G member 2 (4927 Activities)

Discover Target: ABCG2

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

PARP3 Tclin Poly [ADP-ribose] polymerase 3 (206 Activities)

Discover Target: PARP3

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

TNKS Tchem Tankyrase-1 (1241 Activities)

Discover Target: TNKS

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

TNKS2 Tchem Tankyrase-2 (1531 Activities)

Discover Target: TNKS2

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

HCC1395 (122 Activities)

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Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

SLC22A8 Tclin Solute carrier family 22 member 8 (241 Activities)

Discover Target: SLC22A8

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

SLCO1B1 Tchem Solute carrier organic anion transporter family member 1B1 (2672 Activities)

Discover Target: SLCO1B1

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

SLCO1B3 Tchem Solute carrier organic anion transporter family member 1B3 (2517 Activities)

Discover Target: SLCO1B3

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

NCI-H209 (139 Activities)

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Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

PARP6 Tchem Poly [ADP-ribose] polymerase 6 (23 Activities)

Discover Target: PARP6

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

TIPARP Tbio TCDD-inducible poly [ADP-ribose] polymerase (41 Activities)

Discover Target: TIPARP

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

PARP11 Tbio Poly [ADP-ribose] polymerase 11 (83 Activities)

Discover Target: PARP11

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

PARP10 Tchem Poly [ADP-ribose] polymerase 10 (418 Activities)

Discover Target: PARP10

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

PARP12 Tchem Poly [ADP-ribose] polymerase 12 (63 Activities)

Discover Target: PARP12

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

PARP8 Tbio Poly [ADP-ribose] polymerase 8 (85 Activities)

Discover Target: PARP8

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

POU2F2 Tbio POU domain, class 2, transcription factor 2 (42 Activities)

Discover Target: POU2F2

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

MDA-MB-436 (532 Activities)

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Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Associated Targets(non-human)

rep Replicase polyprotein 1ab (378 Activities)

Discover Target: rep

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Slc22a6 Solute carrier family 22 member 6 (141 Activities)

Discover Target: Slc22a6

Activity Type	Relation	Activity value	Units	Action Type	Journal	PubMed Id	doi	Assay Aladdin ID

Mechanisms of Action

Chemical and Physical Properties

• Solubility: Solubility (25°C) In vitro DMSO: 59 mg/mL (197.78 mM); Ethanol: 45 mg/mL (150.84 mM); Water: Insoluble
• DMSO(mg / mL) Max Solubility: 59
• DMSO(mM) Max Solubility: 197.780832020381
• Water(mg / mL) Max Solubility: ＜1
• Molecular Weight: 298.310 g/mol
• XLogP3: 1.600
• Hydrogen Bond Donor Count: 2
• Hydrogen Bond Acceptor Count: 4
• Rotatable Bond Count: 0
• Exact Mass: 298.123 Da
• Monoisotopic Mass: 298.123 Da
• Topological Polar Surface Area: 60.500 Ų
• Heavy Atom Count: 22
• Formal Charge: 0
• Complexity: 566.000
• Isotope Atom Count: 0
• Defined Atom Stereocenter Count: 1
• Undefined Atom Stereocenter Count: 0
• Defined Bond Stereocenter Count: 0
• Undefined Bond Stereocenter Count: 0
• The total count of all stereochemical bonds: 0
• Covalently-Bonded Unit Count: 1

References

1. Rui Miao, Yanfei Li, Xin Zhang, Haoxue Ran, Yifan Yang, Jinwen Wang, Lei Wang, Xiaorong Meng, Danxi Huang.  (2025)  Exploring the Degradation Mechanism of Bisphenol-A with Low Fe2+&H2O2 Content and the Toxicity Evolution of Oxidation Intermediates.  Water Cycle,      [PMID:] [10.1016/j.watcyc.2025.05.005]

2. Min Chen, Huifang Jiao, Dandan Lu, Wenhuan Chen, Zhen Yang, Xue Liang, Pengcheng Wei, Kunpeng Liu.  (2025)  Broad-spectrum anti-influenza activity of the NMPA-approved drug Pamiparib is uncovered by virtual docking to the evolutionarily conserved domain of IAV-M2 protein.  BIOORGANIC & MEDICINAL CHEMISTRY,      [PMID:41380528] [10.1016/j.bmc.2025.118518]

3. Juying Zhou, Yelong Huang, Haitang Xu, Han Long, Jing Xiang.  (2026)  Fabrication of Polyacrylonitrile-Based Composite Fiber Membranes via Ultraviolet-Curing-Electrospinning Combined Technology and Their Adsorption Performance for Methylene Blue.  ChemistrySelect,  11  (13): (e06769).  [PMID:] [10.1002/slct.202506769]