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BMN 673

BMN 673 Structure
BMN 673 structure
CAS No.
1207456-01-6
Chemical Name:
BMN 673
Synonyms
LT-673;CS-750;BMN 673;MDV3800);Talazoparib;BMN 673, >=98%;(8S,9R)-BMN 673;BMN 673 USP/EP/BP;BMN-673, TALAZOPARIB;Talazoparib (BMN 673)
CBNumber:
CB22615112
Molecular Formula:
C19H14F2N6O
Molecular Weight:
380.35
MDL Number:
MFCD22666357
MOL File:
1207456-01-6.mol
Last updated:2024-01-03 15:56:48
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BMN 673 Properties

Melting point 247 - 249°C
Density 1.63
storage temp. Hygroscopic, -20°C Freezer, Under inert atmosphere
solubility DMSO (Slightly), Methanol (Slightly)
form Solid
pka 10.14±0.60(Predicted)
color White to Off-White
FDA UNII 9QHX048FRV
ATC code L01XK04

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS08
Signal word  Danger
Hazard statements  H360-H372-H341
Precautionary statements  P260-P264-P270-P314-P501-P201-P202-P281-P308+P313-P405-P501

BMN 673 price More Price(31)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 19782 BMN-673 ≥98% 1207456-01-6 1mg $72 2024-03-01 Buy
Cayman Chemical 19782 BMN-673 ≥98% 1207456-01-6 5mg $301 2024-03-01 Buy
Cayman Chemical 19782 BMN-673 ≥98% 1207456-01-6 10mg $530 2024-03-01 Buy
Cayman Chemical 19782 BMN-673 ≥98% 1207456-01-6 25mg $968 2024-03-01 Buy
TRC B595885 (8S,9R)-BMN673 1207456-01-6 50mg $870 2021-12-16 Buy
Product number Packaging Price Buy
19782 1mg $72 Buy
19782 5mg $301 Buy
19782 10mg $530 Buy
19782 25mg $968 Buy
B595885 50mg $870 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.

Uses

BMN 673 is a pyrrolopyrazine derivative and anpoly (ADP-ribose) polymerase (PARP) inhibitor for patients with advanced or recurrent solid tumors such as ovarian and breast cancer.

Biological Activity

bmn673 is a potent and selective parp1/2 inhibitor with ki of 1.2 and 0.9 nm, respectively 1. it had no effect on panels of 72 receptors, ion channels, and enzymes 1. bmn673 showed ic50 value of 0.57 nm in enzymatic assay of parp1 1. in in vitro assay, it exhibited greater potency than other existing parp inhibitors, such as veliparib, rucaparib, and olaparib 2. it is also much more potent at trapping parp-dna complexes than other parp inhibitors 3.bmn673 has shown anti-tumor activity both in vitro and in vivo. it inhibited proliferation of tumor cells and xenografts with defects in homologous recombination 1. the combination of bmn673 and dna-damaging agents demonstrated synergistic anti-tumor effects 1. in addition, study showed that the expression levels of dna repair proteins and status of pi3k pathway predict response to bmn673 in small cell lung cancer 4.bmn673 is currently under investigation in multiple

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.

target

PARP

References

1. shen y, rehman fl, feng y et al. bmn 673, a novel and highly potent parp1/2 inhibitor for the treatment of human cancers with dna repair deficiency. clin cancer res 2013; 19: 5003-5015.2. cardnell rj, byers la. proteomic markers of dna repair and pi3k pathway activation predict response to the parp inhibitor bmn 673 in small cell lung cancer--response. clin cancer res 2014; 20: 2237.3. murai j, huang sy, renaud a et al. stereospecific parp trapping by bmn 673 and comparison with olaparib and rucaparib. mol cancer ther 2014; 13: 433-443.4. cardnell rj, feng y, diao l et al. proteomic markers of dna repair and pi3k pathway activation predict response to the parp inhibitor bmn 673 in small cell lung cancer. clin cancer res 2013; 19: 6322-6328.

BMN 673 synthesis

1207454-56-5
1207456-01-6
1207456-00-5
Synthesis of BMN 673 from LT-673

BMN 673 Preparation Products And Raw materials

Raw materials

LT-673 Benzoic acid, 5-fluoro-2-[2-(1-Methyl-1H-1,2,4-triazol-5-yl)acetyl]-3-nitro-, Methyl ester 1(2H)-Phthalazinone, 7-fluoro-5-[(E)-[(4-fluorophenyl)methylene]amino]-4-[(1-methyl-1H-1,2,4-triazol-5-yl)methyl]- 5-Quinolinecarboxylic acid, 7-fluoro-2-(4-fluorophenyl)-1,2,3,4-tetrahydro-1-hydroxy-3-(1-methyl-1H-1,2,4-triazol-5-yl)-4-oxo-, methyl ester 5-Quinolinecarboxylic acid,7-fluoro-2-(4-fluorophenyl)-1,2,3,4-tetrahydro-3-(1-Methyl-1H-1,2,4-triazol-5-yl)-4-oxo-,Methyl ester,(2S,3S)-
1(3H)-Isobenzofuranone,6-fluoro-3-[(1-Methyl-1H-1,2,4-triazol-5-yl)Methylene]-4-nitro-,(3Z)- BMN 673 (8R,9S) 6-Fluoro-4-nitro-3H-isobenzofuran-1-one 5-Quinolinecarboxylic acid, 7-fluoro-2-(4-fluorophenyl)-1,2,3,4-tetrahydro-3-(1-Methyl-1H-1,2,4-triazol-5-yl)-4-oxo-, Methyl ester

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Preparation Products

BMN 673 Suppliers

Global( 176)Suppliers
Supplier Tel Email Country ProdList Advantage
Capot Chemical Co.,Ltd. 		571-85586718 +8613336195806 sales@capotchem.com China 29797 60
ATK CHEMICAL COMPANY LIMITED 		+undefined-21-51877795 ivan@atkchemical.com China 32480 60
career henan chemical co 		+86-0371-86658258 sales@coreychem.com China 29914 58
Biochempartner 		0086-13720134139 candy@biochempartner.com CHINA 967 58
Hubei Jusheng Technology Co.,Ltd. 		18871490254 linda@hubeijusheng.com CHINA 28180 58
Shochem(Shanghai) Co.,Ltd 		86-21-50800795 info@shochem.com CHINA 288 58
BOC Sciences 		+1-631-485-4226 inquiry@bocsci.com United States 19553 58
Chongqing Chemdad Co., Ltd 		+86-023-61398051 +8613650506873 sales@chemdad.com China 39916 58
Antai Fine Chemical Technology Co.,Limited 		18503026267 info@antaichem.com CHINA 9641 58
HANGZHOU CLAP TECHNOLOGY CO.,LTD 		86-571-88216897,88216896 13588875226 sales@hzclap.com CHINA 6313 58
Supplier Advantage
Capot Chemical Co.,Ltd. 		60
ATK CHEMICAL COMPANY LIMITED 		60
career henan chemical co 		58
Biochempartner 		58
Hubei Jusheng Technology Co.,Ltd. 		58
Shochem(Shanghai) Co.,Ltd 		58
BOC Sciences 		58
Chongqing Chemdad Co., Ltd 		58
Antai Fine Chemical Technology Co.,Limited 		58
HANGZHOU CLAP TECHNOLOGY CO.,LTD 		58

Related articles

View Lastest Price from BMN 673 manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
BMN673/Talazoparib pictures 2023-12-23 BMN673/Talazoparib
1207456-01-6
 US $0.00-0.00 / kg 1kg 99%, Single impurity＜0.1 1 ton Nanjing Fred Technology Co., Ltd
Talazoparib pictures 2021-07-13 Talazoparib
1207456-01-6
 US $15.00-10.00 / KG 1KG 99%+ HPLC Monthly supply of 1 ton Zhuozhou Wenxi import and Export Co., Ltd
Talazoparib pictures 2021-07-10 Talazoparib
1207456-01-6
 US $15.00-10.00 / KG 1KG 99%+ HPLC Monthly supply of 1 ton Zhuozhou Wenxi import and Export Co., Ltd
  • BMN673/Talazoparib pictures
  • BMN673/Talazoparib
    1207456-01-6
  • US $0.00-0.00 / kg
  • 99%, Single impurity＜0.1
  • Nanjing Fred Technology Co., Ltd
  • Talazoparib pictures
  • Talazoparib
    1207456-01-6
  • US $15.00-10.00 / KG
  • 99%+ HPLC
  • Zhuozhou Wenxi import and Export Co., Ltd
  • Talazoparib pictures
  • Talazoparib
    1207456-01-6
  • US $15.00-10.00 / KG
  • 99%+ HPLC
  • Zhuozhou Wenxi import and Export Co., Ltd

BMN 673 Spectrum

BMN 673(1207456-01-6)MS

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

LOXO-101 (sulfate) LOXO-101 Bortezomib PF-01367338 Selumetinib
MG-132 Veliparib Olaparib

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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 BMN 673 USP/EP/BP LT-673;BMN673;LT673;TALAZOPARIB; BMN 673 Talazoparib - BMN 673 | LT 00673 CS-750 LT-673;BMN673;LT673;BMN-673;BMN 673 (8S,9R)-BMN 673 BMN-673, TALAZOPARIB (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 MDV3800) (8S,9R)-5-Fluoro-8-(4-fluorophenyl)-2,7,8,9-tetrahydro-9-(1-... inhibit,LT673,BRCA1/2,MX-1,PARP-mediated,Talazoparib,poly ADP ribose polymerase,BMN 673,breast cancer,BMN673,Inhibitor,PARylation,anticancer,LT 673,PARP Brotizolam Impurity 4 BMN-673 (TALAZOPARIB) (MDV-3800) (LT 00673) 1207456-01-6 C19H14F2N6O Inhibitors API