BMN 673
Price | $1 |
Package | 1KG |
Min. Order: | 1G |
Supply Ability: | 100KG |
Update Time: | 2019-07-06 |
Product Details
Product Name: BMN 673 | CAS No.: 1207456-01-6 |
Min. Order: 1G | Purity: 98% |
Supply Ability: 100KG | Release date: 2019/07/06 |
AD68
BMN 673 Basic information |
Description Features In vitro In vivo |
Product Name: | BMN 673 |
Synonyms: | BMN 673;LT-673;(8S,9R)-5-Fluoro-8-(4-fluorophenyl)-2,7,8,9-tetrahydro-9-(1-methyl-1H-1,2,4-triazol-5-yl)-3H-pyrido[4,3,2-de]phthalazine-3-one;(8S,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-Methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4,3,2-de]phthalazin-3(7H)-one;Talazoparib;3H-Pyrido[4,3,2-de]phthalazin-3-one, 5-fluoro-8-(4-fluorophenyl)-2,7,8,9-tetrahydro-9-(1-methyl-1H-1,2,4-triazol-5-yl)-, (8S,9R)-;Talazoparib (BMN 673);(8S,9R)-5-Fluoro-8-(4-fluorophenyl)-2,7,8,9-tetrahydro-9-(1-methyl-1H-1,2,4-triazol-5-yl)-3H-pyrido[4,3,2-de]phthalazine-3-one BMN673 |
CAS: | 1207456-01-6 |
MF: | C19H14F2N6O |
MW: | 380.3508664 |
EINECS: | |
Product Categories: | API;Inhibitors |
Mol File: | 1207456-01-6.mol |
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. |
Company Profile Introduction
Established in 2014,Career Henan Chemical Co. is a manufacturerspecializing in the sale of fine chemicals.
Mainly deals in the sales of:
Pharmaceutical intermediates
OLED intermediates:
Pharmaceutical intermediates;
OLED intermediates;
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- Since: 2014-12-17
- Address: No.967,15th Floor,Unit 7, Building 1, No.70 of DianChang Road, High-tech Development Zone, Zhengzho
INQUIRY
楊俊青
sales@coreychem.com
sales@coreychem.com