BLU-554 free base · Synonyms: Fisogatinib

Fisogatinib is a potent, highly selective and orally active fibroblast growth factor receptor 4 inhibitor.

For research use only. Not for human or veterinary use.

Target FGFR

Research area Cancer

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Data Sheet SDS COA

BLU-554 structure

CAS No.: 1707289-21-1

Download structure (.mol)

Pack sizes & pricing

Size	Price	SKU	Stock
250 mg	USD 420.00	BP-01924-250mg	In stock	Get quote
500 mg	USD 620.00	BP-01924-500mg	In stock	Get quote
1 g	USD 920.00	BP-01924-1g	In stock	Get quote
5 g	Inquire	BP-01924-5g	In stock	Inquire

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Description

Fisogatinib (BLU-554) is a potent, highly selective and orally active fibroblast growth factor receptor 4 (FGFR4) inhibitor with an IC50 of 5 nM. Fisogatinib has significant anti-tumor activity in models of hepatocellular carcinoma (HCC) that are dependent on FGFR4 signalling.

Biological activity

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.

Identifiers

SMILES: COC1=CC(OC)=C(Cl)C(C2=CC3=CN=C(N[C@@H]4COCC[C@@H]4NC(=O)C=C)N=C3C=C2)=C1Cl
InChIKey: MGZKYOAQVGSSGC-DLBZAZTESA-N

Specifications

MW (average): 503.3780
Formula: C₂₄H₂₄Cl₂N₄O₄
CAS No.: 1707289-21-1
Physical state: Solid
Color: White to light yellow
Shipping: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage: Powder -20℃ 2 years; In solvent -20℃ 1 month;

Solubility

Soluble in DMSO

Documents

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.

Same target

Search FGFR

Same research area

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