1207456-01-6 BMN 673 CAS NO.1207456-01-6
- FOB Price: USD: 1,000.00-1,000.00 /Metric Ton Get Latest Price
- Min.Order: 1 Kilogram
- Payment Terms: L/C,T/T
- Available Specifications:
pharma(0-1)Metric Ton
- Product Details
Keywords
- 1207456-01-6
- BMN 673
- BMN 673
Quick Details
- ProName: 1207456-01-6 BMN 673
- CasNo: 1207456-01-6
- Molecular Formula: C19H14F2N6O
- Appearance: white powder
- Application: pharma
- DeliveryTime: prompt
- PackAge: as clients needs
- Port: Shanghai,QingdaoTianjin,Guangzhou
- ProductionCapacity: 1 Metric Ton/Day
- Purity: 99%
- Storage: RT
- Transportation: sea
- LimitNum: 1 Kilogram
- Moisture Content: N/A
- Impurity: N/A
- N/A: N/A
Superiority
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1.Noble Metal Catalysts (Pt.Pd...)
2.Organic Phosphine Ligands (Tert-butyl-phosphine.Cyclohexyl-phosphine...)
3.OLED intermediates (Fluorene,Carbazole,Boric acid...)
4.Customs Synthesis
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Details
BMN 673 Chemical Properties
density 1.63
Safety Information
MSDS Information
BMN 673 Usage And Synthesis
Description Talazoparib (BMN 673) is a novel PARP inhibitor with IC50 of 0.58 nM in a cell-free assay. It is also a potent inhibitor of PARP-2, but does not inhibit PARG and is highly sensitive to PTEN mutation. Phase 3.
Features Most potent and selective PARPi reported thus far.
In vitro BMN-673 selectively binds to PARP and prevents PARP-mediated DNA repair of single strand DNA breaks via the base-excision repair pathway. This enhances the accumulation of DNA strand breaks, promotes genomic instability and eventually leads to apoptosis. BMN 673 selectively kills cancer cells with BRCA-1 or BRCA-2 mutations. BMN 673 demonstrates single-agent cytotoxicityin BRCA-1 mutant (MX-1, IC50 = 0.3 nM) and BRCA-2 mutant cells (Capan-1, IC50 = 5 nM). In contrast, in MRC-5 normal human fibroblastand other tumor cell lines with wild-type BRCA-1 and BRCA-2 genes, IC50 of BMN 673 ranges between 90 nM and 1.9 μM. In cultured human cancer cells, BMN 673 also significantly enhances the cytotoxic efficacy of both Temozolomide and SN-38. Off-target molecular screening did not identify significant non-specific activity for this class of PARP inhibitors.
In vivo In rat pharmacokinetic studies, BMN 673 displays >50% oralbioavailability and pharmacokinetic properties that enable singledaily dosing. In MX-1 xenograft tumor model studies, daily oral dosingof BMN 673 significantly enhances the antitumor effects ofcytotoxic therapies in a dose-dependent manner.