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5mg |
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10mg |
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25mg |
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50mg |
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100mg |
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250mg |
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Other Sizes |
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Purity: ≥98%
Pamiparib maleate, the maleate salt of pamiparib (formerly BGB-290), is a selective inhibitor of PARP1 and PARP2 with IC50 values of 0.83 and 0.11 nM, respectively. Pamiparib is being studied in clinical settings and may be used to treat a number of cancers, including solid tumors. In China, it was accepted in 2021.
ln Vitro |
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ln Vivo |
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Enzyme Assay |
BGB-290 exhibited strong potency for PARP1/2 (IC50 = 0.83 and 0.11 nM, respectively) and high selectivity over other PARP in the biochemical assays. BGB-290 exhibited strong potency for PARP1/2 (IC50 = 0.83 and 0.11 nM, respectively) and excellent selectivity against other PARP enzymes in the biochemical assays. Using a fluorescence polarization (FP) binding assay, the DNA-trapping activity of BGB-290 was determined. With an IC50 of 13 nM, BGB-290 demonstrated strong DNA-trapping activity. With an IC50 of 0.24 nM, BGB-290 suppressed intracellular PAR formation in the cellular experiments. BGB-290 showed significant sensitivity to tumor cell lines with homologous recombination defects. When BGB-290 was administered orally, it was observed that the MDA-MB-436 (BRCA1 mutant) breast cancer xenograft showed time- and dose-dependent inhibition of PARylation, which correlated well with the concentrations of tumor drug. BGB-290 produced PAR inhibition that was more persistent than olaparib. BGB-290 showed remarkable anti-tumor activity in this model, more than ten times more potent than olaparib, which is consistent with this finding.
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Cell Assay |
Three of the seven SCLC cell lines examined in the panel were BGB-290 sensitive. Using patient biopsy samples from Beijing Cancer Hospital, in-house primary tumor models for SCLC were created. Using eight SCLC primary tumor models, the anti-tumor properties of BGB-290 alone or in combination with etoposide/carboplatin (E/C) were assessed. In these models, BGB-290 displayed only marginal single agent activity. The clinical response seen in these patients was consistent with the sensitivity of six out of the eight models (75%) to E/C treatment.In these chemosensitive models, the addition of BGB-290 as maintenance therapy or concurrent treatment greatly extended the duration of the response. The combined effects of BGB-290 and E/C were less successful in the two chemo-insensitive models. Throughout the trial, adding BGB-290 to the chemotherapy regimen was well tolerated.
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Animal Protocol |
8 SCLC primary tumor models.
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References |
Molecular Formula |
C16H15FN4O
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Molecular Weight |
414.39
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Exact Mass |
298.12
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Elemental Analysis |
C, 64.42; H, 5.07; F, 6.37; N, 18.78; O, 5.36
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CAS # |
2086689-94-1
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Related CAS # |
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Appearance |
Solid powder
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SMILES |
C[C@]12N(CC3=NNC(=O)C4=C5C3=C1NC5=CC(=C4)F)CCC2.C[C@]12N(CC3=NNC(=O)C4=C5C3=C1NC5=CC(=C4)F)CCC2.C(=C\C(=O)O)\C(=O)O.C(=C\C(=O)O)\C(=O)O.C(=C\C(=O)O)\C(=O)O
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InChi Key |
CQDVXYMHPXRRCS-YIIKDHGFSA-N
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InChi Code |
InChI=1S/2C16H15FN4O.3C4H4O4/c2*1-16-3-2-4-21(16)7-11-13-12-9(15(22)20-19-11)5-8(17)6-10(12)18-14(13)16;3*5-3(6)1-2-4(7)8/h2*5-6,18H,2-4,7H2,1H3,(H,20,22);3*1-2H,(H,5,6)(H,7,8)/b;;3*2-1-/t2*16-;;;/m11.../s1
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Chemical Name |
(Z)-but-2-enedioic acid;(2R)-14-fluoro-2-methyl-6,9,10,19-tetrazapentacyclo[14.2.1.02,6.08,18.012,17]nonadeca-1(18),8,12(17),13,15-pentaen-11-one
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Synonyms |
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HS Tariff Code |
2934.99.9001
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Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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Solubility (In Vitro) |
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Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.4132 mL | 12.0659 mL | 24.1319 mL | |
5 mM | 0.4826 mL | 2.4132 mL | 4.8264 mL | |
10 mM | 0.2413 mL | 1.2066 mL | 2.4132 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.