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Pamiparib

Cat. No. M9525
Pamiparib Structure
Synonym:

BGB-290

Size Price Availability Quantity
5mg USD 139.5  USD155 In stock
10mg USD 229.5  USD255 In stock
25mg USD 450  USD500 In stock
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Biological Activity

Pamiparib (BGB-290) is an orally active, potent, highly selective inhibitor of PARP1 and PARP2 with IC50 values of 0.9 nM and 0.5 nM, respectively. Pamiparib shows potent DNA-trapping activity with an IC50 of 13 nM. Pamiparib 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. 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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

Chemical Information
Molecular Weight 298.31
Formula C16H15FN4O
CAS Number 1446261-44-4
Purity 100.0%
Solubility DMSO ≥ 30 mg/mL
Storage at -20°C
References

BGB-290: A highly potent and specific PARP1/2 inhibitor potentiates anti-tumor activity of chemotherapeutics in patient biopsy derived SCLC models.
Zhiyu Tang, et al. Cancer Research. 2015 Aug;Volume 75, Issue 15.

Inhibition of PARP activity by BGB-290 potentiates efficacy of NSC 362856 in patient derived xenografts of glioblastoma multiforme.
Shiv K. Gupta, et al. Cancer Research. 2015 Aug;Volume 75, Issue 15.

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  Catalog
Abmole Inhibitor Catalog 2017




Keywords: Pamiparib, BGB-290 supplier, PARP, inhibitors

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