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MedKoo Cat#: 527807 | Name: Fisogatinib
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

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.

Chemical Structure

Fisogatinib
Fisogatinib
CAS#1707289-21-1

Theoretical Analysis

MedKoo Cat#: 527807

Name: Fisogatinib

CAS#: 1707289-21-1

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

Price and Availability

Size Price Availability Quantity
10mg USD 250.00 2 Weeks
25mg USD 450.00 2 Weeks
50mg USD 750.00 2 Weeks
100mg USD 1,250.00 2 Weeks
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Related CAS #
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Synonym
BLU-554; BLU 554; BLU554, NSC795718; NSC 795718; NSC-795718; 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.

Preparing Stock Solutions

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.

Recalculate based on batch purity %
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
1: 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. 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: Damoiseaux D, Li W, Martínez-Chávez A, Beijnen JH, Schinkel AH, Huitema ADR, Dorlo TPC. Predictiveness of the Human-CYP3A4-Transgenic Mouse Model (Cyp3aXAV) for Human Drug Exposure of CYP3A4-Metabolized Drugs. Pharmaceuticals (Basel). 2022 Jul 13;15(7):860. doi: 10.3390/ph15070860. PMID: 35890158; PMCID: PMC9322370. 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. 6: Li C, Chen T, Liu J, Wang Y, Zhang C, Guo L, Shi D, Zhang T, Wang X, Li J. FGF19-Induced Inflammatory CAF Promoted Neutrophil Extracellular Trap Formation in the Liver Metastasis of Colorectal Cancer. Adv Sci (Weinh). 2023 Aug;10(24):e2302613. doi: 10.1002/advs.202302613. Epub 2023 Jun 22. PMID: 37345586; PMCID: PMC10460854. 7: 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. 8: Zhang X, Zhang X, Han R, Wang Z, Yang Q, Huang Y, Yan Y. BLU-554, A selective inhibitor of FGFR4, exhibits anti-tumour activity against gastric cancer in vitro. Biochem Biophys Res Commun. 2022 Mar 5;595:22-27. doi: 10.1016/j.bbrc.2022.01.067. Epub 2022 Jan 21. PMID: 35093636. 9: Ardizzone A, Scuderi SA, Giuffrida D, Colarossi C, Puglisi C, Campolo M, Cuzzocrea S, Esposito E, Paterniti I. Role of Fibroblast Growth Factors Receptors (FGFRs) in Brain Tumors, Focus on Astrocytoma and Glioblastoma. Cancers (Basel). 2020 Dec 18;12(12):3825. doi: 10.3390/cancers12123825. PMID: 33352931; PMCID: PMC7766440. 10: Xie H, Alem Glison DM, Kim RD. FGFR4 inhibitors for the treatment of hepatocellular carcinoma: a synopsis of therapeutic potential. Expert Opin Investig Drugs. 2022 Apr;31(4):393-400. doi: 10.1080/13543784.2022.2017879. Epub 2021 Dec 20. PMID: 34913780. 11: Zhou M, Zhu S, Xu C, Liu B, Shen J. A phase Ib/II study of BLU-554, a fibroblast growth factor receptor 4 inhibitor in combination with CS1001, an anti-PD-L1, in patients with locally advanced or metastatic hepatocellular carcinoma. Invest New Drugs. 2023 Feb;41(1):162-167. doi: 10.1007/s10637-023-01335-w. Epub 2023 Feb 10. PMID: 36763233.