[CAS NO. 1707289-21-1] Fisogatinib
PRODUCTS SPECIFICATIONS [1707289-21-1]
DESCRIPTION [1707289-21-1]
Overview
| MDL | MFCD30496704 |
|---|---|
| Molecular Weight | 503.38 |
| Molecular Formula | C24H24Cl2N4O4 |
| SMILES | C=CC(N[C@@H]1[C@H](NC2=NC=C3C=C(C4=C(Cl)C(OC)=CC(OC)=C4Cl)C=CC3=N2)COCC1)=O |
1 Publications Citing Use of MCE
Summary
Fisogatinib (BLU-554) is a potent, highly selective and orally active fibroblast growth factor receptor 4 (FGFR4) inhibitor with an IC 50 of 5 nM. Fisogatinib has significant anti-tumor activity in models of hepatocellular carcinoma (HCC) that are dependent on FGFR4 signalling [1] [2] .
IC50 & Target
|
FGFR4 5 nM (IC 50 ) |
In Vivo
Tissue distribution of Fisogatinib (10 mg/kg; oral gavage; for 4 hours; FVB/NRj mice) in wild-type mice is as follows; tissue concentrations decreases in the order liver > kidney > small intestine > spleen > brain. The high Fisogatinib liver-to-plasma ratio suggests there is a relatively high amount of the drug being transported into the liver [1] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
| Animal Model: | Wild type male mice(FVB/NRj, 11-14 weeks of age) [1] |
| Dosage: | 10 mg/kg |
| Administration: | Oral gavage; for 4 hours (Pharmacokinetic study) |
| Result: | Tissue concentrations decreased in the order liver > kidney > small intestine > spleen > brain. |
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT04194801 | CStone Pharmaceuticals|Blueprint Medicines Corporation |
Hepatocellular Carcinoma
|
December 16, 2019 | Phase 1|Phase 2 |
| NCT02508467 | Blueprint Medicines Corporation |
Hepatocellular Carcinoma (HCC)
|
July 31, 2015 | Phase 1 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : 100 mg/mL ( 198.66 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.9866 mL | 9.9329 mL | 19.8657 mL |
| 5 mM | 0.3973 mL | 1.9866 mL | 3.9731 mL |
| 10 mM | 0.1987 mL | 0.9933 mL | 1.9866 mL |
References
- [1] Dogan-Topal B, et al. Quantification of FGFR4 inhibitor BLU-554 in mouse plasma and tissue homogenates using liquid chromatography-tandem mass spectrometry. J Chromatogr B Analyt Technol Biomed Life Sci. 2019 Mar 15;1110-1111:116-123.
- [2] Richard Kim, et al. First-in-human study of BLU-554, a potent, highly selective FGFR4 inhibitor designed for hepatocellular carcinoma (HCC) with FGFR4 pathway activation. EJC. December 2016, Volume 69, Supplement 1, Page S41.