Rociletinib-hydrobromide-CO-1686-hydrobromide-DataSheet-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemERociletinib hydrobromideCat. No.: HY-15729ACAS No.: 1446700-26-0Synonyms: CO-1686 (hydrobromide); AVL-301 hydrobromide; CNX-419hydrobromide分式: CHBrFNO分量: 636.46作靶點: EGFR作通路: JAK/STAT Signaling; Protein Tyrosine Kinase/RTK儲存式: Po

2、wder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 59 mg/mL (92.70 mM)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 1.5712 mL 7.8560 mL 15.7119 mL5 mM 0.3142 mL 1.5712 mL 3.1424 mL10 mM 0.1571 mL 0.7856 mL 1.5712 mL請根據(jù)產(chǎn)品在不同溶劑中

3、的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 Rociletinib hydrobromide (CO-1686 hydrobromide)種可服的 EGFR 突變型抑制劑，對EGFRL858R/T790M 和 EGFRWT 的 Ki 值分別為 21.5 nM 和 303.3 nM。IC50 & Target EGFRL858R/T790M EGFRT790M1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE21.5 nM (Ki) 303.3 nM (Ki)體外研究 Rocile

4、tinib (0.1 M) inhibits EGFR potently and irreversibly, and inhibits more than 50% of 23 targets.Rociletinib potently and selectively inhibits growth of NSCLC cells expressing mutant EGFR and inducesapoptosis. Rociletinib resistant NSCLC cell lines are sensitive to AKT inhibition 1.體內(nèi)研究 Rociletinib (

5、100 mg/kg/day, p.o.) demonstrates anti-tumor activity in NSCLC EGFR mutant xenograft models.Rociletinib (50 mg/kg bid, p.o.) demonstrates anti-tumor activity in human EGFR-L858R and EGFR-L858R-T790M expressing transgenic mice 1.PROTOCOLCell Assay 1 Cells are seeded at 3,000 cells/well in growth medi

6、a supplemented with 5% FBS, 2 mM L-glutamine, and 1% P/S, allowed to adhere overnight, and treated with a dilution series of test compound (Rociletinib) for 72 hr.Cell viability is determined by CellTiter Glo and results are represented as background-subtracted relativelight units normalized to a DM

7、SO-treated control. Growth inhibition (GI50) values are determined byGraphPad Prism 5.04. Combination index (CI) data is generated using CalcuSyn.MCE has not independently confirmed the accuracy of these methods. They are for reference only.Animal Briefly, NCr nu/nu mice are sub-cutaneously implante

8、d with 1107 tumor cells in 50% Matrigel (injectionAdministration 1 volume of 0.2 mL/mouse). Once tumors reached 100-200 mm3, Animals are dosed with compounds(Rociletinib) as outlined (N=10 animals/gp). The LUM1686 PDX xenograft study is performed by CrownBio.Briefly, LUM1686 PDX tumor fragments, har

9、vested from donor mice, are inoculated into BALB/c nude mice.Administration of test compounds (Rociletinib) is initiated at a mean tumor size of approximately 160 mm3.Tumor growth is monitored over time to determine tumor growth inhibition of the experimental agent vs.vehicle. The endpoint of the ex

10、periment is a mean tumor volume (MTV) in control group of 2000 mm3.Percent TGI is defined as the difference between the MTV of the designated control group and the MTV ofthe drug-treated group, expressed as a percentage of the MTV of the designated control group. Data ispresented as meanstandard err

11、or of the mean (SEM).MCE has not independently confirmed the accuracy of these methods. They are for reference only.戶使本產(chǎn)品發(fā)表的科研獻 Science. 2017 Dec 1;358(6367). J Med Chem. 2017 Apr 13;60(7):2944-2962. Mol Cancer Ther. 2018 Mar;17(3):603-613. ChemMedChem. 2017 Nov 22;12(22):1857-1865. Patent. US201900

12、10159A1.See more customer validations on HYPERLINK / www.MedChemEREFERENCES2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemE1. Walter AO, et al. Discovery of a mutant-selective covalent inhibitor of EGFR that overcomes T790M-mediated resistance in NSCLC.Cancer Discov. 2013 Sep 25.McePdfHeightCaution: Pr