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

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

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 109 In-stock
Solution
10 mM * 1 mL in DMSO USD 109 In-stock
Solid
5 mg USD 99 In-stock
10 mg USD 165 In-stock
25 mg USD 275 In-stock
50 mg USD 495 In-stock
100 mg USD 825 In-stock
200 mg   Get quote  
500 mg   Get quote  

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Customer Review

Based on 2 publication(s) in Google Scholar

Other Forms of Pamiparib:

Pamiparib Related Antibodies

Top Publications Citing Use of Products

View All PARP Isoform Specific Products:

View All Isoforms
PARP PARP1 PARP2 PARP3 PARP4 TNKS1/PARP5A TNKS2/PARP5B PARP7 PARP10 PARP14 PARP15 PARP12 PARP16

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

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[1]

PARP

 

Cellular Effect
Cell Line Type Value Description References
HCC1395 EC50
42.5 nM
Compound: 139; BGB-290
Antiproliferation activity against human HCC1395 cells expressing BRCA1 mutant incubated for 7 days by CellTiter-Glo luminescent cell viability assay
Antiproliferation activity against human HCC1395 cells expressing BRCA1 mutant incubated for 7 days by CellTiter-Glo luminescent cell viability assay
[PMID: 33264017]
MDA-MB-231 EC50
> 10000 nM
Compound: 139; BGB-290
Antiproliferation activity against human MDA-MB-231 cells incubated for 7 days by CellTiter-Glo luminescent cell viability assay
Antiproliferation activity against human MDA-MB-231 cells incubated for 7 days by CellTiter-Glo luminescent cell viability assay
[PMID: 33264017]
MDA-MB-436 EC50
10.6 nM
Compound: 139; BGB-290
Antiproliferation activity against human MDA-MB-436 cells expressing BRCA1 mutant incubated for 7 days by CellTiter-Glo luminescent cell viability assay
Antiproliferation activity against human MDA-MB-436 cells expressing BRCA1 mutant incubated for 7 days by CellTiter-Glo luminescent cell viability assay
[PMID: 33264017]
SK-BR-3 EC50
> 10000 nM
Compound: 139; BGB-290
Antiproliferation activity against human SK-BR-3 cells incubated for 7 days by CellTiter-Glo luminescent cell viability assay
Antiproliferation activity against human SK-BR-3 cells incubated for 7 days by CellTiter-Glo luminescent cell viability assay
[PMID: 33264017]
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].

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

Pamiparib Related Antibodies
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].

MedChemExpress (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.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C1NN=C2CN(CCC3)[C@@]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 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : 50 mg/mL (167.61 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

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
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

×
Volume (start)

V1

=
Concentration (final)

C2

×
Volume (final)

V2

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

  • Protocol 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

    This protocol yields a clear solution of ≥ 2.25 mg/mL (saturation unknown).

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (22.5 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

    Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation

Purity: 99.97%

SDS (393 KB)

COA (257 KB) HNMR (209 KB) LCMS (338 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.3522 mL 16.7611 mL 33.5222 mL 83.8054 mL
5 mM 0.6704 mL 3.3522 mL 6.7044 mL 16.7611 mL
10 mM 0.3352 mL 1.6761 mL 3.3522 mL 8.3805 mL
15 mM 0.2235 mL 1.1174 mL 2.2348 mL 5.5870 mL
20 mM 0.1676 mL 0.8381 mL 1.6761 mL 4.1903 mL
25 mM 0.1341 mL 0.6704 mL 1.3409 mL 3.3522 mL
30 mM 0.1117 mL 0.5587 mL 1.1174 mL 2.7935 mL
40 mM 0.0838 mL 0.4190 mL 0.8381 mL 2.0951 mL
50 mM 0.0670 mL 0.3352 mL 0.6704 mL 1.6761 mL
60 mM 0.0559 mL 0.2794 mL 0.5587 mL 1.3968 mL
80 mM 0.0419 mL 0.2095 mL 0.4190 mL 1.0476 mL
100 mM 0.0335 mL 0.1676 mL 0.3352 mL 0.8381 mL
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Pamiparib Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Pamiparib1446261-44-4BGB-290BGB290BGB 290PARPpoly ADP ribose polymeraseInhibitorinhibitorinhibit

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