Pamiparib
Based on 3 publication(s) in Google Scholar
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.
- Purity: 99.96%
- CAS No.: 1446261-44-4
- Formula: C16H15FN4O
- Molecular Weight:298.32
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
Publications Citing Use of MedChemExpress (MCE) Pamiparib
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Biological Activity
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PARP |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| HCC1395 | EC50 |
42.5 nM
Compound: 139; BGB-290
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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] |
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.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1446261-44-4
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Appearance Solid
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Molecular Weight 298.32
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Formula C16H15FN4O
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Color Light yellow to yellow
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SMILES
O=C1NN=C2CN(CCC3)[C@@]3(C)C(N4)=C2C5=C4C=C(F)C=C51
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Synonyms
BGB-290
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (3)
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Journal Impact Factor
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Most Recent
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Nature
2019 Dec;576(7786):274-280. PMID: 31802000 -
Neoplasia
Targeting BARD1 suppresses a Myc-dependent transcriptional program and tumor growth in pancreatic ductal adenocarcinoma. [Abstract]2025 May:63:101152. PMID: 40096771 -
Solvent & Solubility
DMSO : 50 mg/mL (167.60 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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.
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.
Please enter the basic information of animal experiments:
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-
-
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
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).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
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
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Data Sheet (281 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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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 | 3.3521 mL | 16.7605 mL | 33.5209 mL | 83.8023 mL |
| 5 mM | 0.6704 mL | 3.3521 mL | 6.7042 mL | 16.7605 mL | |
| 10 mM | 0.3352 mL | 1.6760 mL | 3.3521 mL | 8.3802 mL | |
| 15 mM | 0.2235 mL | 1.1174 mL | 2.2347 mL | 5.5868 mL | |
| 20 mM | 0.1676 mL | 0.8380 mL | 1.6760 mL | 4.1901 mL | |
| 25 mM | 0.1341 mL | 0.6704 mL | 1.3408 mL | 3.3521 mL | |
| 30 mM | 0.1117 mL | 0.5587 mL | 1.1174 mL | 2.7934 mL | |
| 40 mM | 0.0838 mL | 0.4190 mL | 0.8380 mL | 2.0951 mL | |
| 50 mM | 0.0670 mL | 0.3352 mL | 0.6704 mL | 1.6760 mL | |
| 60 mM | 0.0559 mL | 0.2793 mL | 0.5587 mL | 1.3967 mL | |
| 80 mM | 0.0419 mL | 0.2095 mL | 0.4190 mL | 1.0475 mL | |
| 100 mM | 0.0335 mL | 0.1676 mL | 0.3352 mL | 0.8380 mL |