WARNING: This product is for research use only, not for human or veterinary use.
Hodoodo CAT#: H527807
CAS#: 1707289-21-1
Description: Fisogatinib, also known as 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.
Hodoodo Cat#: H527807
Name: Fisogatinib
CAS#: 1707289-21-1
Chemical Formula: C24H24Cl2N4O4
Exact Mass: 502.12
Molecular Weight: 503.380
Elemental Analysis: C, 57.27; H, 4.81; Cl, 14.08; N, 11.13; O, 12.71
Synonym: BLU-554; BLU 554; BLU554, Fisogatinib
IUPAC/Chemical Name: N-((3S,4S)-3-((6-(2,6-dichloro-3,5-dimethoxyphenyl)quinazolin-2-yl)amino)tetrahydro-2H-pyran-4-yl)acrylamide
InChi Key: MGZKYOAQVGSSGC-DLBZAZTESA-N
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
SMILES Code: 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
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
More Info: Aberration in FGFR4 signaling drives carcinogenesis and progression in a subset of hepatocellular carcinoma (HCC) patients, thereby making FGFR4 an attractive molecular target for this disease. Selective FGFR4 inhibition can be achieved through covalently targeting a poorly conserved cysteine residue in the FGFR4 kinase domain.
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The following data is based on the product molecular weight 503.38 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 1 mM | 1.15 mL | 5.76 mL | 11.51 mL |
| 5 mM | 0.23 mL | 1.15 mL | 2.3 mL |
| 10 mM | 0.12 mL | 0.58 mL | 1.15 mL |
| 50 mM | 0.02 mL | 0.12 mL | 0.23 mL |
| Formulation protocol: | |
| In vitro protocol: | |
| In vivo protocol: |
1: 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.
2: 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.
3: 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.
4: 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.
5: 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.
