RK-287107 _PARP 抑制剂 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemERK-287107Cat. No.: HY-123892CAS No.: 2171386-10-8分式: CHFNO分量: 416.46作靶点: PARP作通路: Cell Cycle/DNA Damage; Epigenetics储存式: 4C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect fromlight)溶解性数据体外实验 DMSO : 125

2、mg/mL (300.15 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制备储备液1 mM 2.4012 mL 12.0060 mL 24.0119 mL5 mM 0.4802 mL 2.4012 mL 4.8024 mL10 mM 0.2401 mL 1.2006 mL 2.4012 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，配制前请先配制澄清的储备液，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

3、议您现现配，当天使；澄清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: 2.08 mg/mL (4.99 mM); Clear solution2. 请依序添加每种溶剂： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (4.99 mM); Clear solution3. 请依序添加每种溶剂： 10% DMSO 90% corn oilSolubil

4、ity: 2.08 mg/mL (4.99 mM); Clear solution1/3 Master of Small Molecules 您边的抑制剂师www.MedChemEBIOLOGICAL ACTIVITY物活性 RK-287107种有效的特异性 tankyrase 抑制剂，抑制 tankyrase-1 和 tankyrase-2，IC50 分别为 14.3 和10.6 nM。RK-287107 可阻断结直肠癌细胞长 1。IC50 & Target tankyrase-1 tankyrase-214.3 nM (IC50) 10.6 nM (IC50)体外研究 RK-87107 (

5、0.01-10 M; 12 hours) shows an antiproliferative effect on colorectal cancer cells harboring shortadenomatous polyposis coli (APC) mutations. The 50% growth inhibition (GI50) value of RK-287107 onCOLO-320DM cells is 0.449 M 1.RK-287107 (0.03-10 M; 16 hours) causes accumulation of tankyrase and Axin1/

6、2 1.RK-287107 (0.03-10 M; 16 hours) also downregulates -catenin signaling in cultured cells 1.Cell Proliferation Assay 1Cell Line: Colorectal cancer COLO-320DM, SW403, RKO, HCC2998, HCT-116, and DLD-1 cellsConcentration: 0.01, 0.1, 1, 10 MIncubation Time: 12 hoursResult: Inhibited the growth of APC-

7、mutated (-catenin-dependent) colorectal cancer COLO-320DM and SW403 cells. The GI50 value of RK-287107 on COLO-320DM is 0.449 M.Did not inhibit the growth of APC-wild (-catenin-independent) colorectal cancer celllines, including RKO, HCT-116, HCC2998 and DLD-1.Western Blot Analysis 1Cell Line: COLO-

8、320DM cellsConcentration: 0.03, 0.1, 0.33, 1, 3, and 10 MIncubation Time: 16 hoursResult: Downregulation of active -catenin was observed体内研究 RK-287107 (100 and 300 mg/kg; i.p. administration; once per day; 5-days on/ 2-days off schedule for 2weeks) inhibits tumor growth in a mouse xenograft model 1.

9、Animal Model: 6-week-old female NOD.CB17-Prkdcscid/J mice with colorectal cancer COLO-320DM 1Dosage: 100 and 300 mg/kgAdministration: Administration i.p.; once per day; 5-days on/ 2-days off schedule for 2 weeksResult: 100 and 300 mg/kg resulted in 32.9% and 44.2% TGI, respectively.2/3 Master of Small Molecules 您边的抑制剂师www.MedChemEREFERENCES1. Mizutani A, et al. RK-287107, a potent and specific tankyrase inhibitor, blocks colorectal cancer cell growth in a preclinical model.Cancer Sci. 2018 Dec;109(12):4003-4014.McePdfHeightCaution: Product has not been fully validate