FF284
CH5183284
CAS: 1265229-25-1
Molecular Formula: C20H16N6O
FF284 - Names and Identifiers
FF284 - Physico-chemical Properties
| Molecular Formula | C20H16N6O |
| Molar Mass | 356.38 |
| Density | 1.51±0.1 g/cm3(Predicted) |
| Boling Point | 775.5±55.0 °C(Predicted) |
| Solubility | DMSO: ≥ 31mg/mL |
| pKa | 10.51±0.10(Predicted) |
| Storage Condition | -20℃ |
| In vitro study | In cellular level assays, CH5183284 at 100 to 300 nM prevented DMS114 (FGFR1 amplification),SNU-16 (FGFR2 amplification), and KMS11 [t(4;14) translocation and FGFR3 Y373C mutation] autophosphorylation of FGFR1,FGFR2, and FGFR3 in cell lines. CH5183284 thus produces selective anti-proliferative activity against cancer cell lines comprising genetic alterations of FGFR. FGFR2 contains a gating mutation (V564F) that makes it resistant to other FGFR inhibitors, while CH5183284 can inhibit it. |
| In vivo study | CH5183284 (100 mg/kg/day, p.o.) xenografts with genetically altered FGFR, such as KG1 (leukemia, FGFR1OP-FGFR1 fusion),SNU-16 (gastric cancer, FGFR2 amplification),MFE-280 (endometrial cancer, FGFR2 S252W mutant),UM-UC-14 (bladder cancer, FGFR3 S249C mutant), and RT112/84 (bladder cancer, FGFR3-TACC3 fusion) produced significant selective antitumor activity. |
FF284 - Preparation solution concentration reference
| 1mg | 5mg | 10mg | |
|---|---|---|---|
| 1 mM | 2.806 ml | 14.03 ml | 28.06 ml |
| 5 mM | 0.561 ml | 2.806 ml | 5.612 ml |
| 10 mM | 0.281 ml | 1.403 ml | 2.806 ml |
| 5 mM | 0.056 ml | 0.281 ml | 0.561 ml |
Last Update：2024-01-02 23:10:35
FF284 - Reference Information
| biological activity | CH5183284 is a selective, orally effective FGFR inhibitor for FGFR1,FGFR2,FGFR3, and FGFR4 IC50 were 9.3 nM,7.6 nM,22 nM, and 290 nM, respectively. Phase 1. CH5183284 (Debio-1347, FF284) is a selective orally potent FGFR inhibitor with IC50 of 9.3 nM,7.6 nM for FGFR1,FGFR2,FGFR3, and FGFR4, respectively, 22 nM, and 290 nM. Phase 1. |
| Target | Value |
| FGFR2 (Cell-free assay) | 7.6 nM |
| FGFR1 (Cell-free assay) | 9.3 nM |
| FGFR3 (Cell-free assay) | 22 nM |
| FGFR4 (Cell-free assay) | 290 nM |
Last Update：2024-04-09 20:52:54
Supplier List
Spot supply
Product Name: CH5183284 Visit Supplier Webpage Request for quotationCAS: 1265229-25-1
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
Spot supply
Product Name: CH5183284 Visit Supplier Webpage Request for quotationCAS: 1265229-25-1
Tel: 18301782025
Email: 3008007409@qq.com
Mobile: 18021002903
QQ: 3008007409
Wechat: 18301782025
View History