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Pamiparib

Cat. No. M9525
Pamiparib Structure
Synonym:

BGB-290

Size Price Availability Quantity
5mg USD 95  USD95 In stock
10mg USD 155  USD155 In stock
25mg USD 255  USD255 In stock
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Quality Control & Documentation
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.

Chemical Information
Molecular Weight 298.31
Formula C16H15FN4O
CAS Number 1446261-44-4
Solubility (25°C) DMSO ≥ 30 mg/mL
Storage Powder          -20°C   3 years ;  4°C   2 years
In solvent       -80°C   6 months ;  -20°C   1 month
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Zhiyu Tang, et al. Cancer Research. BGB-290: A highly potent and specific PARP1/2 inhibitor potentiates anti-tumor activity of chemotherapeutics in patient biopsy derived SCLC models.

[2] Shiv K. Gupta, et al. Cancer Research. Inhibition of PARP activity by BGB-290 potentiates efficacy of NSC 362856 in patient derived xenografts of glioblastoma multiforme.

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


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