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| 品牌 | absin | CAS | 1265229-25-1 |
|---|---|---|---|
| 分子式 | C20H16N6O | 纯度 | 98% |
| 分子量 | 356.38 | 货号 | abs47028249 |
| 规格 | 2mg | 供货周期 | 现货 |
| 主要用途 | is a selective and orally available FGFR | 应用领域 | 化工,生物产业,农林牧渔,制药/生物制药,综合 |
CH5183284 (Debio-1347) 1265229-25-1
| 产品描述 | |
| 描述 | CH5183284 is a selective and orally available FGFR inhibitor with IC50 of 9.3 nM, 7.6 nM, 22 nM, and 290 nM for FGFR1, FGFR2, FGFR3, and FGFR4, respectively. Phase 1. |
| 纯度 | 98% |
| 储存/保存方法 | Store at -20℃ for one year（Powder）；Store at 2-4℃ for two weeks；Store at -20℃ for six months after dissolution. |
| 基本信息 | |
| 可溶性/溶解性 | DMSO:71 mg/mL (199.22 mM) |
| 生物活性 | |
| 靶点 | FGFR2 ,FGFR1 ,FGFR3 ,FGFR4 |
| In vitro(体外研究) | In cell-based assay, CH5183284 prevents autophosphorylation of FGFR1, FGFR2, and FGFR3 at 100 to 300 nM in the DMS114 (FGFR1 amplification), SNU-16 (FGFR2 amplification), and KMS11 cell lines. CH5183284 thus produces selective antiproliferative activity against cancer cell lines harboring genetic alterations in FGFR. CH5183284 also inhibit FGFR2 harboring one type of the gatekeeper mutation (V564F) that causes resistance to other FGFR inhibitors. |
| In vivo(体内研究) | CH5183284 (100 mg/kg/day, p.o.) shows selective and significant antitumor activity against xenografts with FGFR genetic alterations such as KG1 (leukemia, FGFR1OP-FGFR1 fusion), SNU-16 (gastric cancer, FGFR2 amplification), MFE-280 (endometrial cancer, FGFR2 S252W mutation), UM-UC-14 (bladder cancer, FGFR3 S249C mutation), and RT112/84 (bladder cancer, FGFR3-TACC3 fusion). |
| 参考文献 | |
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| 研究领域 | |
| 研究领域 | CancerGrowth factorsFGF CancerSignal transductionProtein phosphorylationTyrosine kinasesReceptor tyrosine kinases CardiovascularAngiogenesisGrowth FactorsFGFFGF Receptors Developmental BiologyLineage specificationEctoderm NeuroscienceDevelopment NeuroscienceNeurology processNeurogenesis Signal TransductionGrowth Factors/HormonesFGF Signal TransductionProtein PhosphorylationTyrosine KinasesReceptor Tyrosine Kinases Stem CellsLineage MarkersEctoderm Drug DiscoverySmall Molecule DrugLead Compound Discovery |
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