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Talazoparib

(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

CAS: 1207456-01-6

Molecular Formula: C19H14F2N6O

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Talazoparib - Names and Identifiers

Name (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
Synonyms BMN673
LT-673
BMN-673
BMN 673
Talazoparib
NDI-010976, ND-630
Talazoparib (BMN 673)
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]phthalazin-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
(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
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)-
(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

Talazoparib - Physico-chemical Properties

Molecular FormulaC19H14F2N6O
Molar Mass380.35
Density1.63
Melting Point247 - 249°C
Solubility DMSO (Slightly), Methanol (Slightly)
AppearanceSolid
ColorWhite to Off-White
pKa10.14±0.60(Predicted)
Storage ConditionHygroscopic, -20°C Freezer, Under inert atmosphere
In vitro studyBMN-673 selectively binds to PARP and inhibits PARP-mediated repair of single-stranded DNA breaks through the base excision repair pathway. It enhances the accumulation of DNA strand breaks, promotes genomic instability, and ultimately leads to apoptosis. BMN 673 selectively kills cancer cells with BRCA-1 or BRCA-2 mutations. BMN 673 acts on cells with BRCA-1 mutation (MX-1,IC50=0.3 nM) and BRCA-2 mutation (Capan-1,IC50=5 nM), and has single-agent cytotoxicity. In contrast, BMN-673 acted on MRC-5 normal human fibroblasts and other tumor cell lines containing wild-type BRCA-1 and BRCA-2 genes, with an IC50 of 90 nM to 1.9 μm. BMN 673 also significantly enhanced the cytotoxic effects of Temozolomide and SN-38 on cultured human cancer cells.
In vivo studyIn pharmacokinetic studies in rats, BMN673 was dosed alone daily with> 50% oral bioavailability and pharmacokinetic properties. In a MX-1 xenograft tumor model study, daily oral administration of BMN 673 significantly enhanced the antitumor effect of cytotoxic therapy in a dose-dependent manner.

Talazoparib - Introduction

BMN 673 is a new type of PARP inhibitor. IC50 is 0.58 nM. It also effectively inhibits PARP-2, but does not inhibit PARG. It is highly sensitive to PTEN mutation.
Last Update:2022-10-16 17:12:43

Talazoparib - Reference Information

biological activity Talazoparib (BMN 673) is a new type of PARP inhibitor with IC50 of 0.58 nM, which also effectively inhibits PARP-2, but does not inhibit PARG and is highly sensitive to PTEN mutation. Phase 3.
Talazoparib (BMN 673, LT-673) is a new type of PARP inhibitor. the IC50 of PARP1 in cell-free test is 0.57 nM. It is also a potent PARP-2 inhibitor but does not inhibit PARG and is highly sensitive to PTEN mutants. Phase 3.
features the most effective selective PARP inhibitor reported so far.
TargetValue
PARP1 (Cell-free assay) 0.57 nM
Last Update:2024-04-09 20:49:11
Talazoparib
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Shanghai Macklin Biochemical Co., Ltd
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CAS: 1207456-01-6
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
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Shanghai Macklin Biochemical Co., Ltd
Featured ProductsSpot supply
Product Name: BMN 673 Visit Supplier Webpage Request for quotation
CAS: 1207456-01-6
Tel: +86-18821248368
Email: Int06@meryer.com
Mobile: +86-18821248368
QQ: 495145328 Click to send a QQ message
WhatsApp: +86-18821248368
Hubei Rhema Reference Materials Technology Co., Ltd.
Spot supply
Product Name: Talazoparib Request for quotation
CAS: 1207456-01-6
Tel: 0712-8899838
Email: jy6101@rmastandards.com
Mobile: 86-15787876101
QQ: 2518299249 Click to send a QQ message
Wechat: 15787876101
Shanghai Amole Biotechnology Co., Ltd.
Multiple SpecificationsSpot supply
Product Name: BMN 673 Request for quotation
CAS: 1207456-01-6
Tel: 400-968-2212
Email: 3623107365@qq.com
Mobile: 18916960931
QQ: 3623107365 Click to send a QQ message
Wechat: 18916960931
SHANGHAI ACMEC BIOCHEMICAL TECHNOLOGY CO., LTD.
Spot supply
Product Name: BMN 673 Visit Supplier Webpage Request for quotation
CAS: 1207456-01-6
Tel: +86-400-900-4166
Email: product@acmec-e.com
Mobile: +86-18621343501
QQ: 2881950922 Click to send a QQ message
Wechat: 18621343501
WhatsApp: +86-18621343501
MedChemExpress (MCE)
Spot supply
Product Name: BMN-673; LT-673 Visit Supplier Webpage Request for quotation
CAS: 1207456-01-6
Tel: 609-228-6898
Email: sales@medchemexpress.com
     tech@medchemexpress.com
Mobile: 609-228-6898
SKYRUN INDUSTRIAL CO.,LTD
Spot supply
Product Name: BMN 673 Visit Supplier Webpage Request for quotation
CAS: 1207456-01-6
Tel: +86 0571-86722205
Email: sales@chinaskyrun.com
Mobile: +8618958170122
QQ: 2531159185 Click to send a QQ messageSend QQ message
Wechat: chinaskyrun
Shanghai Yuanye Bio-Technology Co., Ltd.
Spot supply
Product Name: (8S,9R)-BMN 673 Visit Supplier Webpage Request for quotation
CAS: 1207456-01-6
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409 Click to send a QQ message
View History
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