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Purity: ≥98%
BLU-554 is a novel potent, highly-selective, and orally bioavailable inhibitor of FGFR4 (fibroblast growth factor receptor 4) with an IC50 value of 5 nM in cell free assays. BLU-554 has the potential to be used for the treatment of hepatocellular carcinoma and cholangiocarcinoma. BLU-554 shows promise as a treatment for cholangiocarcinoma and hepatocellular carcinoma. These tumor models demonstrate good tolerance to BLU-554. In models of liver cancer, BLU-554 administration results in tumor regression. When taken orally, BLU-554 selectively attaches to FGFR4 and prevents the ligand FGF19 from binding to it. This stops FGFR4 from activating, suppresses FGFR4-mediated signaling, and stops tumor cell growth in FGFR4-overexpressing cells. The receptor tyrosine kinase FGFR4 is implicated in the survival, angiogenesis, proliferation, and differentiation of tumor cells. Some types of tumor cells overexpress FGF19. See if there are any ongoing clinical trials with this medication. (Thesaurus NCI).
| Targets |
FGFR4 (IC50 = 5 nM)
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| ln Vitro |
BLU-554 confers potency and selectivity by taking advantage of a special interaction with FGFR4.
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| ln Vivo |
BLU-554 is well tolerated in these tumor models. In models of liver cancer, BLU-554 administration results in tumor regression[1].
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| Enzyme Assay |
BLU-554 is a novel potent, highly-selective, and orally bioavailable inhibitor of FGFR4 (fibroblast growth factor receptor 4) with an IC50 value of 5 nM in cell free assays.
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| Cell Assay |
For four hours, either DMSO or BLU-554 at a concentration of one microgram per cell were applied to ST8814 resistant cells.
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| Animal Protocol |
Male FVB/NRj mice
10 mg/kg p.o. |
| References | |
| Additional Infomation |
Fisogatinib is under investigation in clinical trial NCT04194801 (A Phase Ib/ii Study of Fisogatinib(blu-554) in Subjects With Hepatocellular Carcinoma).
Fisogatinib is an orally bioavailable inhibitor of human fibroblast growth factor receptor 4 (FGFR4), with potential antineoplastic activity. Upon oral administration, fisogatinib specifically binds to and blocks the binding of the ligand FGF19 to FGFR4. This prevents the activation of FGFR4, inhibits FGFR4-mediated signaling and leads to an inhibition of tumor cell proliferation in FGFR4-overexpressing cells. FGFR4 is a receptor tyrosine kinase and is involved in tumor cell proliferation, differentiation, angiogenesis, and survival. FGF19 is overexpressed by certain tumor cell types. |
| Molecular Formula |
C24H24CL2N4O4
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|---|---|---|
| Molecular Weight |
503.38
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| Exact Mass |
502.117
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| Elemental Analysis |
C, 57.27; H, 4.81; Cl, 14.08; N, 11.13; O, 12.71
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| CAS # |
1707289-21-1
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| Related CAS # |
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| PubChem CID |
91885617
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| Appearance |
White to light yellow solid powder
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| Density |
1.4±0.1 g/cm3
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| Index of Refraction |
1.647
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| LogP |
3.14
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
7
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
34
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| Complexity |
688
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| Defined Atom Stereocenter Count |
2
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| SMILES |
ClC1C(=C([H])C(=C(C=1C1C([H])=C([H])C2C(C=1[H])=C([H])N=C(N=2)N([H])[C@]1([H])C([H])([H])OC([H])([H])C([H])([H])[C@]1([H])N([H])C(C([H])=C([H])[H])=O)Cl)OC([H])([H])[H])OC([H])([H])[H]
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| InChi Key |
MGZKYOAQVGSSGC-DLBZAZTESA-N
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| 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
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| Chemical Name |
N-[(3S,4S)-3-[[6-(2,6-dichloro-3,5-dimethoxyphenyl)quinazolin-2-yl]amino]oxan-4-yl]prop-2-enamide
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| Synonyms |
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
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| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (4.97 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.5 mg/mL (4.97 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 2.5 mg/mL (4.97 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
| Preparing Stock Solutions | 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 |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Recruitment | interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT00651365 | Active Recruiting |
Drug: Fisogatinib (BLU-554) |
Hepatocellular Carcinoma (HCC) |
Blueprint Medicines Corporation | July 31, 2015 | Phase 1 |
| NCT04194801 | Completed | Drug: Phase Ib: Fisogatinib (BLU-554) 400mg in combination with Sugemalimab (CS1001) 1200mg Drug: Phase Ib: Fisogatinib (BLU-554) 600mg in combination with Sugemalimab (CS1001) 1200mg |
Hepatocellular Carcinoma | CStone Pharmaceuticals | December 16, 2019 | Phase 1 Phase 2 |
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