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BFH772 - 98%, high purity , Vascular endothelial growth factor receptor 2 inhibitor, CAS No.890128-81-1, Vascular endothelial growth factor receptor 2 inhibitor
VEGFR2 Selective Inhibitors
Basic Description Synonyms BCP18910 | MFCD30534392 | HMS3649L19 | T1IV236CVP | 6-[[6-(hydroxymethyl)-4-pyrimidinyl]oxy]-N-[3-(trifluoromethyl)phenyl]-1-naphthalenecarboxamide | AKOS032945111 | HY-100419 | s8188 | A915077 | BDBM50270425 | EX-A1157 | CS-6044 | UNII-T1IV236CVP | SCHEM Specifications & Purity ≥98% Biochemical and Physiological Mechanisms BFH772 is a novel potent oral VEGFR2 inhibitor, targeting VEGFR2 kinase with IC50 of 3 nM. Storage Temp Store at -20°C Shipped In Ice chest + Ice pads Action Type INHIBITOR Mechanism of action Vascular endothelial growth factor receptor 2 inhibitor Product Description Information
BFH772 is a novel potent oralVEGFR2inhibitor, targeting VEGFR2 kinase with IC50 of 3 nM.
Targets
VEGFR2 (Cell-free assay) 3 nM
In vitro
BFH772 was highly effective at targeting VEGFR2 kinase with an IC50 value of 3 nM, however, lost 500-fold potency on FLK-1, FLT-1, and FLT-4. BFH772 was highly selective, In addition to VEGFR2, it also targeted B-RAF, RET, and TIE-2, albeit with at least 40-fold lower potency. BFH772 inhibits the ligand induced autophosphorylation of RET, PDGFR, and KIT kinases, with IC50 values ranging between 30 and 160 nM.
In vivo
BFH772 all at 3 mg/kg orally dosed once per day potently inhibited melanoma growth (by 54−90% for primary tumor and 71−96% for metastasis growth).
Cell Research(from reference)
Cell lines：HUVEC endothelial cells
Concentrations：0-10 nM
Incubation Time：48 h
Product Properties ALogP 4.396 HBD Count 2 Rotatable Bond 6
Associated Targets(Human) Associated Targets(non-human) Names and Identifiers Pubchem Sid 488200678 Pubchem Sid Url https://pubchem.ncbi.nlm.nih.gov/substance/488200678 IUPAC Name 6-[6-(hydroxymethyl)pyrimidin-4-yl]oxy-N-[3-(trifluoromethyl)phenyl]naphthalene-1-carboxamide INCHI InChI=1S/C23H16F3N3O3/c24-23(25,26)15-4-2-5-16(10-15)29-22(31)20-6-1-3-14-9-18(7-8-19(14)20)32-21-11-17(12-30)27-13-28-21/h1-11,13,30H,12H2,(H,29,31) InChi Key JNLSTLQFDDAULK-UHFFFAOYSA-N Canonical SMILES C1=CC(=CC(=C1)NC(=O)C2=CC=CC3=C2C=CC(=C3)OC4=NC=NC(=C4)CO)C(F)(F)F Isomeric SMILES C1=CC(=CC(=C1)NC(=O)C2=CC=CC3=C2C=CC(=C3)OC4=NC=NC(=C4)CO)C(F)(F)F PubChem CID 24756034 Molecular Weight 439.39
Chemical and Physical Properties Solubility Solubility (25°C) In vitro DMSO: 87 mg/mL (198.0 mM); Ethanol: 87 mg/mL (198.0 mM); Water: Insoluble; DMSO(mg / mL) Max Solubility 87 DMSO(mM) Max Solubility 198.0017752 Water(mg / mL) Max Solubility ＜1
Safety and Hazards(GHS) Signal Warning Hazard Statements H315: Causes skin irritation
H319: Causes serious eye irritation
H335: May cause respiratory irritation
H302: Harmful if swallowed
Precautionary Statements P261: Avoid breathing dust/fume/gas/mist/vapors/spray.
P305+P351+P338: IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses if present and easy to do - continue rinsing.
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