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| Size | Price | Stock |
|---|---|---|
| 5mg | $150 | 3-6 Days |
| 10mg | $235 | 3-6 Days |
| 25mg | $410 | 3-6 Days |
| 50mg | $650 | 3-6 Days |
| 100mg | $1000 | 3-6 Days |
| 250mg | $1800 | 3-6 Days |
: Cat #: V2693 CAS #: 1707289-21-1 Purity ≥ 98%
Description: 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 is well tolerated in these tumor models. Administration of BLU-554 induces tumor regression in liver cancer models. Upon oral administration, BLU-554 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. Check for active clinical trials using this agent. (NCI Thesaurus).
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| Molecular Weight (MW) | 503.38 |
|---|---|
| Molecular Formula | C24H24Cl2N4O4 |
| CAS No. | 1707289-21-1 |
| Storage | -20℃ for 3 years in powder form |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 100 mg/mL (198.7 mM) |
| Water: <1 mg/mL | |
| Ethanol: 2 mg/mL (4 mM) | |
| Synonyms | BLU-554; BLU 554; BLU554 |
| Protocol | In Vitro | In vitro activity: 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 is well tolerated in these tumor models. Administration of BLU-554 induces tumor regression in liver cancer models. Upon oral administration, BLU-554 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. Check for active clinical trials using this agent. (NCI Thesaurus). Kinase 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. Cell Assay: Fibroblast growth factor receptor 4 (FGFR-4) is a protein that in humans is encoded by the FGFR-4 gene. This protein is a member of the fibroblast growth factor receptor family, where amino acid sequence was highly conserved between members throughout evolution. FGFR family members 1-4 differ from one another in their ligand affinities and tissue distribution. A full-length representative protein consists of an extracellular region composed of three immunoglobulin-like domains, a single hydrophobic membrane-spanning segment and a cytoplasmic tyrosine kinase domain. The extracellular portion of the protein interacts with fibroblast growth factors, setting in motion a cascade of downstream signals, ultimately influencing mitogenesis and differentiation. The genomic organization of the FGFR-4 gene encompasses 18 exons. Although alternative splicing has been observed, there is no evidence that the C-terminal half of the Iglll domain of this protein varies between three alternate forms, as indicated for FGFR 1-3. |
|---|---|---|
| In Vivo | BLU-554 is well tolerated in these tumor models. Administration of BLU-554 induces tumor regression in liver cancer models |
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 1.9866 mL | 9.9329 mL | 19.8657 mL | 39.7314 mL |
| 5mM | 0.3973 mL | 1.9866 mL | 3.9731 mL | 7.9463 mL |
| 10mM | 0.1987 mL | 0.9933 mL | 1.9866 mL | 3.9731 mL |
| 20mM | 0.0993 mL | 0.4966 mL | 0.9933 mL | 1.9866 mL |
This equation is commonly abbreviated as: C1 V1 = C2 V2
- (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.