|
Toll Free: (877) 796-6397 -- USA and Canada only -- |
Fax: +1-832-582-8590 Orders: +1-832-582-8158 |
Tech Support: +1-832-582-8158 Ext:3 Please provide your Order Number in the email. |
Technical Data
| Formula | C16H15FN4O |
|||
| Molecular Weight | 298.31 | CAS No. | 1446261-44-4 | |
| Solubility (25°C)* | In vitro | DMSO | 60 mg/mL (201.13 mM) | |
| Ethanol | 15 mg/mL (50.28 mM) | |||
| Water | Insoluble | |||
|
* <1 mg/ml means slightly soluble or insoluble. * Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. * Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.) |
||||
Preparing Stock Solutions
Biological Activity
| Description | Pamiparib is a potent and selective inhibitor of PARP1 and PARP2 with IC50 values of 0.83 and 0.11 nM, respectively in biochemical assays. It shows high selectivity over other PARP enzymes. | ||||
|---|---|---|---|---|---|
| Targets |
|
||||
| In vitro | BGB-290 shows potent DNA-trapping activity with IC50 of 13 nM. In the cellular assays, BGB-290 inhibits intracellular PAR formation with an IC50 of 0.24 nM[1]. |
||||
| 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, correlating well with the tumor drug concentrations. BGB-290 has also demonstrated good combination activity with chemotherapeutics in patient biopsy derived SCLC models[1]. 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[2]. |
Protocol (from reference)
References
Selleck's Pamiparib has been cited by 10 publications
| Aggregability of the SQSTM1/p62-based aggresome-like induced structures determines the sensitivity to parthanatos [ Cell Death Discov, 2024, 10(1):74] | PubMed: 38346947 |
| Zinc Finger MYND-Type Containing 8 (ZMYND8) Is Epigenetically Regulated in Mutant Isocitrate Dehydrogenase 1 (IDH1) Glioma to Promote Radioresistance [ Clin Cancer Res, 2023, 29(9):1763-1782] | PubMed: 36692427 |
| Class I HDAC inhibition reduces DNA damage repair capacity of MYC-amplified medulloblastoma cells [ J Neurooncol, 2023, 164(3):617-632] | PubMed: 37783879 |
| Class I HDAC inhibition reduces DNA damage repair capacity of MYC-amplified medulloblastoma cells [ J Neurooncol, 2023, 164(3):617-632] | PubMed: 37783879 |
| PARP-mediated PARylation of MGMT is critical to promote repair of temozolomide-induced O6-methylguanine DNA damage in glioblastoma [ Neuro Oncol, 2021, 23(6):920-931] | PubMed: 33433610 |
| A pan-cancer organoid platform for precision medicine [ Cell Rep, 2021, 36(4):109429] | PubMed: 34320344 |
| Pharmacological Poly (ADP-Ribose) Polymerase Inhibitors Decrease Mycobacterium tuberculosis Survival in Human Macrophages [ Front Immunol, 2021, 12:712021] | PubMed: 34899683 |
| Pharmacological Poly (ADP-Ribose) Polymerase Inhibitors Decrease Mycobacterium tuberculosis Survival in Human Macrophages [ Front Immunol, 2021, 12:712021] | PubMed: 34899683 |
| EGFR Amplification Induces Increased DNA Damage Response and Renders Selective Sensitivity to Talazoparib (PARP Inhibitor) in Glioblastoma [ Clin Cancer Res, 2020, 26(6):1395-1407] | PubMed: 31852834 |
| EGFR amplification induces increased DNA damage response and renders selective sensitivity to Talazoparib (PARP inhibitor) in glioblastoma. [ Clin Cancer Res, 2019, 10.1158/1078-0432.CCR-19-2549] | PubMed: 31852834 |
RETURN POLICY
Selleck Chemical’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.
NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.