China (Mainland)
Olaparib(AZD2281) CAS NO.763113-22-0
- Min.Order: 10 Metric Ton
- Payment Terms:
- Product Details
Keywords
- Olaparib
- AZD2281
- Ku-0059436
Quick Details
- ProName: Olaparib(AZD2281)
- CasNo: 763113-22-0
- Molecular Formula: C24H23FN4O3
- ProductionCapacity: Metric Ton/Day
- Purity: 99.09%
- LimitNum: 10 Metric Ton
Superiority
Biological Activity
| Description | Olaparib (AZD2281, KU0059436) is a selective inhibitor of PARP1/2 with IC50 of 5 nM/1 nM in cell-free assays, 300-times less effective against tankyrase-1. Olaparib induces significant autophagy that is associated with mitophagy in cells with BRCA mutations. | ||||||||||||||||||||||||||||||
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| Features | A potent PARP inhibitor (currently in late stage clinical trials). | ||||||||||||||||||||||||||||||
| Targets |
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| In vitro |
Olaparib would act against BRCA1 or BRCA2 mutations. Olaparib is not sensitive to tankyrase-1 (IC50 >1 μM). Olaparib could ablate the PARP-1 activity at concentrations of 30-100 nM in SW620 cells. Olaparib is hypersensitive to BRCA1-deficient cell lines (MDA-MB-463 and HCC1937), compared with BRCA1- and BRCA2-proficient cell lines (Hs578T, MDA-MB-231, and T47D). [1] Olaparib is strongly sensitive to KB2P cells due to suppression of base excision repair by PARP inhibition, which may result in the conversion of single-strand breaks to double-strand breaks during DNA replication, thus activating BRCA2-dependent recombination pathways. [2] |
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| Cell Data |
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| Assay |
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| In vivo | Combining with temozolomide, Olaparib (10 mg/kg, p.o.) significantly suppresses tumor growth in SW620 xenografts. [1] Olaparib shows great response to Brca1-/-;p53-/- mammary tumors (50 mg/kg i.p. per day), while no responses to HR-deficient Ecad-/-;p53-/- mammary tumors. Olaparib even does not show dose-limiting toxicity in tumor-bearing mice. [3] Olaparib has been used to treat with BRCA mutated tumors, such as ovarian, breast and prostate cancers. Moreover, Olaparib shows selectively inhibition to ATM (Ataxia Telangiectasia Mutated)-deficient tumor cells, which indicates to be a potential agent for treating ATM mutant lymphoid tumors. [4] |