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BMN 673

Description Features In vitro In vivo
BMN 673
BMN 673 structure
CAS No.
1207456-01-6
Chemical Name:
BMN 673
Synonyms
LT-673;BMN 673;Talazoparib;BMN 673, >=98%;(8S,9R)-BMN 673;Talazoparib (BMN 673);Talazoparib - BMN 673 | LT 00673;(8S,9R)-5-Fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4;(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;(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
CBNumber:
CB22615112
Molecular Formula:
C19H14F2N6O
Formula Weight:
380.3508664
MOL File:
1207456-01-6.mol

BMN 673 Properties

Density 
1.63

BMN 673 price More Price(4)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 19782 BMN-673 ≥98% 1207456-01-6 1mg $55 2018-11-13 Buy
Cayman Chemical 19782 BMN-673 ≥98% 1207456-01-6 5mg $234 2018-11-13 Buy
Cayman Chemical 19782 BMN-673 ≥98% 1207456-01-6 10mg $413 2018-11-13 Buy
Cayman Chemical 19782 BMN-673 ≥98% 1207456-01-6 25mg $756 2018-11-13 Buy

BMN 673 Chemical Properties,Uses,Production

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.

Enzyme inhibitor

This novel, orally bioavailable poly(ADP-ribose) polymerase, or PARP, inhibitor (FW = 380.35 g/mol; CAS 1207456-01-6), also known as (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, targets PARP-mediated DNA repair (IC50 = 0.58 nM) of single-strand DNA breaks by the base-excision repair pathway. By enhancing the accumulation of DNA strand breaks, BMN 673 promotes genomic instability, eventually leading to apoptosis. BMN 673 exhibits selective anti-tumor cytotoxicity and elicits DNA repair biomarkers at much lower concentrations than earlier generation PARP1/2 inhibitors, including olaparib, rucaparib and veliparib. BMN 673 shows remarkable anti-tumor activity in vivo, with strong action against xenografted tumors carrying defects in DNA repair due to BRCA mutations or PTEN deficiency. Synergistic or additive anti-tumor effects are observed, when BMN 673 was combined with temozolomide, SN38 or platinum drugs.

BMN 673 Preparation Products And Raw materials

Raw materials

Preparation Products


BMN 673 Suppliers

Global( 88)Suppliers
Supplier Tel Fax Email Country ProdList Advantage
ATK CHEMICAL COMPANY LIMITED
+86 21 5161 9050/ 5187 7795
+86 21 5161 9052/ 5187 7796 ivan@atkchemical.com CHINA 24191 60
Henan DaKen Chemical CO.,LTD.
+86-371-55531817
info@dakenchem.com CHINA 21701 58
Henan Tianfu Chemical Co.,Ltd.
0371-55170693
0371-55170693 info@tianfuchem.com CHINA 20672 55
career henan chemical co
+86-371-86658258
sales@coreychem.com CHINA 29979 58
Biochempartner
0086-13720134139
candy@biochempartner.com CHINA 969 58
Hubei Jusheng Technology Co.,Ltd.
86-18871470254
027-59599243 sales@jushengtech.com CHINA 28236 58
Shochem(Shanghai) Co.,Ltd
86-21-50800795
info@shochem.com CHINA 212 58
BOC Sciences
1-631-619-7922
1-631-614-7828 inquiry@bocsci.com United States 20115 58
Chongqing Chemdad Co., Ltd
+86-13650506873
sales@chemdad.com CHINA 30864 58
MedChemexpress LLC 609-228-6898
609-228-5909 sales@medchemexpress.com United States 4609 58

View Lastest Price from BMN 673 manufacturers

Image Release date Product Price Min. Order Purity Supply Ability Manufacturer
2018-08-21 BMN 673
1207456-01-6
US $1.00 / KG 1G 98% 100KG career henan chemical co

1207456-01-6(BMN 673)Related Search:


  • Talazoparib - BMN 673 | LT 00673
  • (8S,9R)-BMN 673
  • 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
  • BMN 673, >=98%
  • (8S,9R)-5-Fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)-8,9-dihydro-2H-pyrido[4
  • (8S,9R)-5-fluoro-8-(4-fluorophenyl)-9-(1-methyl-1H-1,2,4-triazol-5-yl)- 2,7,8,9-tetrahydro-3H-pyrido[4,3,2-de]phthalazin-3-one
  • 1207456-01-6
  • C19H14F2N6O
  • API
  • Inhibitors
  • -
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