Talazoparib-tosylate-BMN-673ts-DataSheet-生命科学试剂-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemETalazoparib tosylateCat. No.: HY-108413CAS No.: 1373431-65-2Synonyms: BMN 673ts分式: CHFNOS分量: 552.55作靶点: PARP作通路: Cell Cycle/DNA Damage; Epigenetics储存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性数据体外实验 D

2、MSO : 108 mg/mL (195.46 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 1.8098 mL 9.0490 mL 18.0979 mL5 mM 0.3620 mL 1.8098 mL 3.6196 mL10 mM 0.1810 mL 0.9049 mL 1.8098 mL请根据产品在不同溶剂中的溶解度，选择合适的溶剂配制储备液，并请注意储备液的保存式和期限。体内实验 请根据您的实验动物和给药式选择适当的溶解案，配制前请先配制澄的储备液

3、，再依次添加助溶剂(为保证实验结果的可靠性，体内实验的作液，建议您现现配，当天使；澄的储备液可以根据储存条件，适当保存；以下溶剂前的百分指该溶剂在您配制终溶液中的体积占)：1. 请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (4.52 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (4.52 mM); Clear solution1/3 Master of Small Molecules

4、 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 Talazoparib tosylate (BMN 673ts)种新型，效，有可服活性的 PARP1/2 抑制剂，抑制PARP1的IC50值为 0.57 nM。IC50 & Target IC50: 0.57 nM (PARP1) 1体外研究 Talazoparib is a potent PARP1/2 inhibitor (PARP1 IC50=0.57 nM), it has no effect on PARG activity atconcentrations up to 1 M. Talazopar

5、ib binds to PARP1 with a dissociation constant (KD) of 0.29 nM.Talazoparib inhibits PARP1 and -2 to a similar extent, with Kis of 1.20 and 0.85 nM, respectively. Talazoparibselectively targets tumor cells with BRCA1, BRCA2, or PTEN gene defects with 20- to more than 200-foldgreater potency than exis

6、ting PARP1/2 inhibitors. Talazoparib targets tumor cells with homologousrecombination gene defects. Tumor models that are either BRCA1-deficient (MX-1 and SUM149) or BRCA2-deficient (Capan-1) are profoundly sensitive to Talazoparib. Talazoparib induces nuclear -H2AX foci atconcentrations as low as 1

7、00 pM 1.体内研究 Talazoparib is readily orally bioavailable, with more than 40% absolute oral bioavailability in rats when dosedin carboxylmethyl cellulose. Oral administration of Talazoparib elicits remarkable antitumor activity;xenografted tumors that carry defects in DNA repair due to BRCA mutations

8、or PTEN deficiency areprofoundly sensitive to oral Talazoparib treatment at well-tolerated doses in mice. Synergistic or additiveantitumor effects are also found when Talazoparib is combined with temozolomide, SN38, or platinum drugs1.PROTOCOLCell Assay 1 LoVo cells are treated with Talazoparib (10,

9、 40 nM) and temozolomide (TMZ) either alone or in combinationfor 5 days. Surviving fraction is determined using CellTiter-Glo assay. 1MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Mice 1Administration 1 In single-agent studies, olaparib (100 mg

10、/kg), Talazoparib (0.33 or 0.1 mg/kg/d), or vehicle (10% DMAc, 6%Solutol, and 84% PBS) is administered by oral gavage (per os), once daily or Talazoparib (0.165 mg/kg)twice daily for 28 consecutive days. Mice are continuously monitored for 10 more days after last day ofdosing 1.MCE has not independe

11、ntly confirmed the accuracy of these methods. They are for reference only. Cancer Discov. 2017 Sep;7(9):984-998. Mol Cell. 2017 May 18;66(4):503-516.e5. Nat Commun. 2019 Jun 11;10(1):2556. Clin Cancer Res. 2017 Feb 15;23(4):1001-1011.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemE ACS Appl Mater I

12、nterfaces. 2019 Apr 3;11(13):12342-12356.See more customer validations on HYPERLINK / www.MedChemEREFERENCES1. Shen 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 Sep 15;19(18):5003-15.McePdfHeightCaution: Pr