1. Cell Cycle/DNA Damage
    Epigenetics
  2. PARP
  3. Pamiparib

Pamiparib (Synonyms: BGB-290)

Cat. No.: HY-104044 Purity: 99.97%
Handling Instructions

Pamiparib (BGB-290) est un inhibiteur de PARP qui est oralement actif, puissant et hautement sélectif, avec des valeurs de IC50 de 0,9 nM et 0,5 nM pour PARP1 et PARP2, respectivement. Pamiparib a un piégeage puissant de PARP et a une capacité à pénétrer dans le cerveau, et peut être utilisé pour la recherche de divers cancers, y compris la tumeur solide.

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. Pamiparib has potent PARP trapping, and capability to penetrate the brain, and can be used for the research of various cancers including the solid tumor.

For research use only. We do not sell to patients.

Pamiparib Chemical Structure

Pamiparib Chemical Structure

CAS No. : 1446261-44-4

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10 mM * 1 mL in DMSO USD 99 In-stock
Estimated Time of Arrival: December 31
5 mg USD 90 In-stock
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10 mg USD 150 In-stock
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25 mg USD 250 In-stock
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50 mg USD 450 In-stock
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100 mg USD 750 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

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. Pamiparib has potent PARP trapping, and capability to penetrate the brain, and can be used for the research of various cancers including the solid tumor[1][2].

IC50 & Target

PARP

 

In Vitro

Pamiparib shows potent DNA-trapping activity with an IC50 of 13 nM. In the cellular assays, Pamiparib inhibits intracellular PAR formation with an IC50 of 0.24 nM. Tumor cell lines with homologous recombination defects are profoundly sensitive to Pamiparib. Pamiparib is highly active both in vitro and in vivo in BRCA mutant tumors[3].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Pamiparib suppresses PARP activity in patient-derived glioblastoma multiforme and small-cell-lung cancer xenografts, and potentiates the effects of Temozolamide. In vivo activities of Pamiparib, and its combination activity with chemotherapies in patient biopsy derived small cell lung cancer (SCLC) xenograft models[4].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Clinical Trial
Molecular Weight

298.31

Formula

C₁₆H₁₅FN₄O

CAS No.

1446261-44-4

SMILES

O=C1NN=C2CN(CCC3)[[email protected]@]3(C)C(N4)=C2C5=C4C=C(F)C=C51

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 62.5 mg/mL (209.51 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 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
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.25 mg/mL (7.54 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.25 mg/mL (7.54 mM); Clear solution

*All of the co-solvents are provided by MCE.
References

Purity: 99.97%

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Keywords:

PamiparibBGB-290BGB290BGB 290PARPpoly ADP ribose polymeraseInhibitorinhibitorinhibit

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Pamiparib
Cat. No.:
HY-104044
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