BLU-554 is a fibroblast growth factor receptor 4 (FGFR4) inhibitor potentially for the treatment of hepatocellular carcinoma and cholangiocarcinoma. Fisogatinib demonstrates clinical benefit and tumor regression in patients with HCC with aberrant FGF19 expression.
Chemical Formula: C24H24Cl2N4O4
Exact Mass: 502.1175
Molecular Weight: 503.38
Elemental Analysis: C, 57.27; H, 4.81; Cl, 14.08; N, 11.13; O, 12.71
Chemical Name: N-((3S,4S)-3-((6-(2,6-dichloro-3,5-dimethoxyphenyl)quinazolin-2-yl)amino)tetrahydro-2H-pyran-4-yl)acrylamide
InChi Code: InChI=1S/C24H24Cl2N4O4/c1-4-20(31)28-16-7-8-34-12-17(16)30-24-27-11-14-9-13(5-6-15(14)29-24)21-22(25)18(32-2)10-19(33-3)23(21)26/h4-6,9-11,16-17H,1,7-8,12H2,2-3H3,(H,28,31)(H,27,29,30)/t16-,17+/m0/s1
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: 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 Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
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.
Subbiah V, Pal SK. Precision Oncology for Hepatocellular Cancer: Slivering the Liver by FGF19-FGF4-KLB Pathway Inhibition. Cancer Discov. 2019 Dec;9(12):1646-1649. doi: 10.1158/2159-8290.CD-19-1156. Erratum in: Cancer Discov. 2020 Feb;10(2):326. PMID: 31792121.
Roskoski R Jr. The role of fibroblast growth factor receptor (FGFR) protein- tyrosine kinase inhibitors in the treatment of cancers including those of the urinary bladder. Pharmacol Res. 2020 Jan;151:104567. doi: 10.1016/j.phrs.2019.104567. Epub 2019 Nov 23. PMID: 31770593.
Li W, Sparidans R, El-Lari M, Wang Y, Lebre MC, Beijnen JH, Schinkel AH. P-glycoprotein (ABCB1/MDR1) limits brain accumulation and Cytochrome P450-3A (CYP3A) restricts oral availability of the novel FGFR4 inhibitor fisogatinib (BLU-554). Int J Pharm. 2020 Jan 5;573:118842. doi: 10.1016/j.ijpharm.2019.118842. Epub 2019 Nov 20. PMID: 31759109.
Kim RD, Sarker D, Meyer T, Yau T, Macarulla T, Park JW, Choo SP, Hollebecque A, Sung MW, Lim HY, Mazzaferro V, Trojan J, Zhu AX, Yoon JH, Sharma S, Lin ZZ, Chan SL, Faivre S, Feun LG, Yen CJ, Dufour JF, Palmer DH, Llovet JM, Manoogian M, Tugnait M, Stransky N, Hagel M, Kohl NE, Lengauer C, Sherwin CA, Schmidt- Kittler O, Hoeflich KP, Shi H, Wolf BB, Kang YK. First-in-Human Phase I Study of Fisogatinib (BLU-554) Validates Aberrant FGF19 Signaling as a Driver Event in Hepatocellular Carcinoma. Cancer Discov. 2019 Dec;9(12):1696-1707. doi: 10.1158/2159-8290.CD-19-0555. Epub 2019 Oct 1. PMID: 31575541.
Hatlen MA, Schmidt-Kittler O, Sherwin CA, Rozsahegyi E, Rubin N, Sheets MP, Kim JL, Miduturu C, Bifulco N, Brooijmans N, Shi H, Guzi T, Boral A, Lengauer C, Dorsch M, Kim RD, Kang YK, Wolf BB, Hoeflich KP. Acquired On-Target Clinical Resistance Validates FGFR4 as a Driver of Hepatocellular Carcinoma. Cancer Discov. 2019 Dec;9(12):1686-1695. doi: 10.1158/2159-8290.CD-19-0367. Epub 2019 Oct 1. PMID: 31575540.
Products are for research use only. Not for human use.
Payment & Security
Your payment information is processed securely. We do not store credit card details nor have access to your credit card information.