BMN 673

Description Features In vitro In vivo

Product Name: BMN 673
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
Formula Weight: 380.35
MOL File: 1207456-01-6.mol

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BMN 673 Property

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

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Danger

Hazard statements

H341Suspected of causing genetic defects

H360May damage fertility or the unborn child

H372Causes damage to organs through prolonged or repeated exposure

Precautionary statements

P201Obtain special instructions before use.

P202Do not handle until all safety precautions have been read and understood.

P260Do not breathe dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P270Do not eat, drink or smoke when using this product.

P281Use personal protective equipment as required.

P308+P313IF exposed or concerned: Get medical advice/attention.

P314Get medical advice/attention if you feel unwell.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 19782
Product name: BMN-673
Purity: ≥98%
Packaging: 1mg
Price: $72
Updated: 2024/03/01

Cayman Chemical

Product number: 19782
Product name: BMN-673
Purity: ≥98%
Packaging: 5mg
Price: $301
Updated: 2024/03/01

Cayman Chemical

Product number: 19782
Product name: BMN-673
Purity: ≥98%
Packaging: 10mg
Price: $530
Updated: 2024/03/01

Cayman Chemical

Product number: 19782
Product name: BMN-673
Purity: ≥98%
Packaging: 25mg
Price: $968
Updated: 2024/03/01

TRC

Product number: B595885
Product name: (8S,9R)-BMN673
Packaging: 50mg
Price: $870
Updated: 2021/12/16

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BMN 673 Chemical Properties,Usage,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 Preparation Products And Raw materials

Raw materials

Preparation Products

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BMN 673 Suppliers

China 165 India 3 The Netherlands 1 United Kingdom 1 United States 16 Global 186

MedChemexpress LLC

Tel: 021-58955995
Fax: 609-228-5909
Email: sales@medchemexpress.cn
Country: United States
ProdList: 4861
Advantage: 58

AdooQ BioScience, LLC

Tel: +1 (866) 930-6790
Fax: +1 (866) 333-9607
Email: info@adooq.com
Country: United States
ProdList: 2782
Advantage: 58

Target molecule Corp.

Tel: 857-239-0968
Fax: 857-239-8801
Email: service1@targetmol.com
Country: United States
ProdList: 2559
Advantage: 60

Musechem

Tel: +1-800-259-7612
Fax: +1-800-259-7612
Email: info@musechem.com
Country: United States
ProdList: 4660
Advantage: 60

TargetMol Chemicals Inc.

Tel: +1-781-999-5354 +1-00000000000
Email: marketing@targetmol.com
Country: United States
ProdList: 32165
Advantage: 58

InvivoChem

Tel: +1-708-310-1919 +1-13798911105
Fax: 708-557-7486
Email: sales@invivochem.cn
Country: United States
ProdList: 6391
Advantage: 58

Cckinase, Inc.

Tel: +1 (732)236-3202
Email: sales@cckinase.com
Country: United States
ProdList: 2738
Advantage: 58

BOC Sciences

Tel: +1-631-485-4226
Fax: 1-631-614-7828
Email: inquiry@bocsci.com
Country: United States
ProdList: 19553
Advantage: 58

Aladdin Scientific

Tel: +1-+1(833)-552-7181
Email: sales@aladdinsci.com
Country: United States
ProdList: 57505
Advantage: 58

TargetMol Chemicals Inc.

Tel
Email: support@targetmol.com
Country: United States
ProdList: 38632
Advantage: 58

ApexBio Technology

Tel: --
Fax: --
Email: sales@apexbt.com
Country: United States
ProdList: 6251
Advantage: 58

Cayman Chemical Company

Tel: --
Fax: --
Email: cayman@caymanchem.com
Country: United States
ProdList: 6213
Advantage: 81

Creative Enzymes

Tel: --
Fax: --
Email: info@creative-enzymes.com
Country: United States
ProdList: 6057
Advantage: 58

ChemShuttle. Inc.

Tel: --
Fax: --
Email: Sales@ChemShuttle.com
Country: United States
ProdList: 6695
Advantage: 58

Axon Medchem LLC

Tel: --
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Email: info@axonmedchem.com
Country: United States
ProdList: 763
Advantage: 58

Matrix Scientific

Tel: --
Fax: --
Email: sales@matrixscientific.com
Country: United States
ProdList: 6632
Advantage: 80

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View Lastest Price from BMN 673 manufacturers

Nanjing Fred Technology Co., Ltd

Product: BMN673/Talazoparib 1207456-01-6
Price: US $0.00-0.00/kg
Min. Order: 1kg
Purity: 99%, Single impurity＜0.1
Supply Ability: 1 ton
Release date: 2023-12-22

Zhuozhou Wenxi import and Export Co., Ltd

Product: Talazoparib 1207456-01-6
Price: US $15.00-10.00/KG
Min. Order: 1KG
Purity: 99%+ HPLC
Supply Ability: Monthly supply of 1 ton
Release date: 2021-07-11

Zhuozhou Wenxi import and Export Co., Ltd

Product: Talazoparib 1207456-01-6
Price: US $15.00-10.00/KG
Min. Order: 1KG
Purity: 99%+ HPLC
Supply Ability: Monthly supply of 1 ton
Release date: 2021-07-09

1207456-01-6, BMN 673Related Search:

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

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

BMN-673, TALAZOPARIB

(8S,9R)-BMN 673

LT-673;BMN673;LT673;BMN-673;BMN 673

CS-750

Talazoparib - BMN 673 | LT 00673

LT-673;BMN673;LT673;TALAZOPARIB; BMN 673

BMN 673 USP/EP/BP

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

BMN-673 (TALAZOPARIB) (MDV-3800) (LT 00673)

Brotizolam Impurity 4

1207456-01-6

C19H14F2N6O

Inhibitors

API