For research use only, not for therapeutic use.
Ripretinib（Cat No.:I020229）is a broad-spectrum tyrosine kinase inhibitor used for treating advanced gastrointestinal stromal tumors (GIST) that are resistant to other therapies. It works by inhibiting multiple mutant forms of KIT and PDGFRA kinases, which drive the proliferation of cancer cells in GIST. Ripretinib uniquely switches off these oncogenic kinases, preventing tumor growth and overcoming resistance mechanisms. Its efficacy in patients with previously treated GIST makes it a valuable option for managing this aggressive cancer, offering improved progression-free survival and enhanced clinical outcomes in difficult-to-treat cases.
| Catalog Number | I020229 |
| CAS Number | 1442472-39-0 |
| Molecular Formula | C₂₄H₂₁BrFN₅O₂ |
| Purity | 98% |
| Target | PDGFRA KIT |
| Target Protein | |
| Appearance | Solid |
| Storage | Dry, dark and at 2 - 8 °C for six months or -20°C for two years. |
| IC50 | ROSAKIT K509I cells:34 ± 10 nM(IC50) |
| IUPAC Name | 1-[4-bromo-5-[1-ethyl-7-(methylamino)-2-oxo-1,6-naphthyridin-3-yl]-2-fluorophenyl]-3-phenylurea |
| InChI | InChI=1S/C24H21BrFN5O2/c1-3-31-21-12-22(27-2)28-13-14(21)9-17(23(31)32)16-10-20(19(26)11-18(16)25)30-24(33)29-15-7-5-4-6-8-15/h4-13H,3H2,1-2H3,(H,27,28)(H2,29,30,33) |
| InChIKey | CEFJVGZHQAGLHS-UHFFFAOYSA-N |
| SMILES | CCN1C2=CC(=NC=C2C=C(C1=O)C3=CC(=C(C=C3Br)F)NC(=O)NC4=CC=CC=C4)NC |
| Reference | [1]. Schneeweiss M, et al. The KIT and PDGFRA switch-control inhibitor DCC-2618 blocks growth and survival of multiple neoplastic cell types in advanced mastocytosis. Haematologica. 2018 May;103(5):799-809.<br>[2]. KIT/PDGFR Inhibitor DCC-2618.<br>[3]. Schneeweiss M, et al. The KIT and PDGFRA switch-control inhibitor DCC-2618 blocks growth and survival of multiple neoplastic cell types in advanced mastocytosis. Haematologica. 2018 May;103(5):799-809.<br>[4]. BLU-285, DCC-2618 Show Activity against GIST. Cancer Discov. 2017 Feb;7(2):121-122. |
