SML2674

Ki20227

≥98% (HPLC)

• Synonym(e): Ki 20227, N-[4-[(6,7-Dimethoxy-4-quinolinyl)oxy]-2-methoxyphenyl]-N′-[1-(2-thiazolyl)ethyl]urea, N-{4-[(6,7-Dimethoxy-4-quinolinyl)oxy]-2-methoxyphenyl}-N′-[1-(1,3-thiazol-2-yl)ethyl]urea
• Empirische Formel (Hill-System): C₂₄H₂₄N₄O₅S
• CAS-Nummer: 623142-96-1
• Molekulargewicht: 480.54
• MDL-Nummer: MFCD12024693
• UNSPSC-Code: 12352200
• NACRES: NA.77

Eigenschaften

• Assay: ≥98% (HPLC)
• Form: powder
• Farbe: white to beige
• Löslichkeit: DMSO: 2 mg/mL, clear
• Lagertemp.: 2-8°C
• SMILES String: [s]1c(ncc1)C(NC(=O)Nc2c(cc(cc2)Oc3c4c(ncc3)cc(c(c4)OC)OC)OC)C
• InChI: 1S/C24H24N4O5S/c1-14(23-26-9-10-34-23)27-24(29)28-17-6-5-15(11-20(17)30-2)33-19-7-8-25-18-13-22(32-4)21(31-3)12-16(18)19/h5-14H,1-4H3,(H2,27,28,29)
• InChIKey: SHPFDGWALWEPGS-UHFFFAOYSA-N

Beschreibung

Biochem./physiol. Wirkung

Ki20227 is an orally active, potent and selective M-CSF receptor c-Fms (CSF-1R) tyrosine kinase inhibitor (IC50 = 2 nM vs. 12 nM/KDR, 451 nM/c-Kit, 217 nM/PDGFβ; >1 μM/BTK, EGFR, FGFR2, FLT3, Fyn, Met, c-Src, PKA, PKCα) that inhibits M-CSF-dependent (50 ng/mL) c-Fms phosphorylation (by >90% at 10 nM; RAW264.7) and cell growth (IC50 = 14 nM; M-NFS-60). Ki20227 prevents osteolysis in a rat model of bone metastasis (50 mg/kg/day p.o.) by inhibiting A375 tumor-induced osteoclast formation and decreases the number of osteoclast-like cells on bone surfaces in ovariectomized rats (20 mg/kg/day p.o.) in vivo.

Sicherheitshinweise

• Lagerklassenschlüssel: 11 - Combustible Solids
• WGK: WGK 1
• Flammpunkt (°F): Not applicable
• Flammpunkt (°C): Not applicable