Ripretinib-DCC-2618-DataSheet-生命科學試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemERipretinibCat. No.: HY-112306CAS No.: 1442472-39-0Synonyms: DCC-2618分式: CHBrFNO分量: 510.36作靶點: c-Kit; PDGFR作通路: Protein Tyrosine Kinase/RTK儲存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實驗 DMSO : 45

2、mg/mL (88.17 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 1.9594 mL 9.7970 mL 19.5940 mL5 mM 0.3919 mL 1.9594 mL 3.9188 mL10 mM 0.1959 mL 0.9797 mL 1.9594 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，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。體內(nèi)實驗 請根據(jù)您的實驗動物和給藥式選擇適當?shù)娜芙獍?，配制前請先配制澄清的儲備液，再依次添加助溶?為保證實驗結(jié)果的可靠性，體內(nèi)實驗的作液，建議您

3、現(xiàn)現(xiàn)配，當天使；澄清的儲備液可以根據(jù)儲存條件，適當保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.08 mg/mL (4.08 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.08 mg/mL (4.08 mM); Clear solution1/2 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIV

4、ITY物活性 Ripretinib (DCC-2618)種譜的 KIT 和 PDGFRA 的抑制劑，具有抗腫瘤活性。IC50 & Target PDGFRA KIT體外研究 Ripretinib is a pan-KIT and PDGFRA inhibitor, shows cytotoxic activity against gastrointestinal stromaltumors 1. Ripretinib suppresses phosphorylation of KIT and decreases the expression ofphosphosphorylated (p)ST

5、AT5, pAKT and pERK1/2 in neoplastic mast cells. Ripretinib inhibits the growth ofROSAKIT K509I cells with an IC50 of 34 10 nM, and also induces apoptosis in these cells. Ripretinib (0.1-1.0 M) inhibits IgE-dependent histamine release from basophils and spontaneous tryptase release fromneoplastic mas

6、t cells, and also counteracts growth and survival of leukemic monocytes and blast cells at0.01-5 M 2.REFERENCES1. BLU-285, DCC-2618 Show Activity against GIST. Cancer Discov. 2017 Feb;7(2):121-122.2. Schneeweiss M, et al. The KIT and PDGFRA switch-control inhibitor DCC-2618 blocks growth and survival of multiple neoplastic celltypes in advanced mastocytosis. Haematologica. 2018 May;103(5):799-809.McePdfHeightCaution: Product has not been fully validated for medical applications.For research use only.Te