SML3368

CP-673451

≥95% (HPLC)

• Synonym(s): 1-[2-[5-(2-Methoxyethoxy)-1H-benzimidazol-1-yl]-8-quinolinyl]-4-piperidinamine, 1-[2-[5-(2-Methoxyethoxy)benzimidazol-1-yl]quinolin-8-yl]piperidin-4-ylamine, CP 673,451, CP 673451, CP-673,451, CP673,451, CP673451
• Empirical Formula (Hill Notation): C₂₄H₂₇N₅O₂
• CAS Number: 343787-29-1
• Molecular Weight: 417.50
• UNSPSC Code: 12352200
• NACRES: NA.77
• MDL number: MFCD11100329
• Assay: ≥95% (HPLC)
• Form: powder

Properties

• Quality Segment: 100
• assay: ≥95% (HPLC)
• form: powder
• color: white to beige
• solubility: DMSO: 2 mg/mL, clear
• storage temp.: −20°C
• SMILES string: N5(CCC(CC5)N)c1c2nc(ccc2ccc1)[n]3c4c(nc3)cc(cc4)OCCOC
• InChI: 1S/C24H27N5O2/c1-30-13-14-31-19-6-7-21-20(15-19)26-16-29(21)23-8-5-17-3-2-4-22(24(17)27-23)28-11-9-18(25)10-12-28/h2-8,15-16,18H,9-14,25H2,1H3
• InChI key: DEEOXSOLTLIWMG-UHFFFAOYSA-N

Description

Biochem/physiol Actions

ATP-competitive, potent and selective platelet-derived growth factor receptor (PDGFR) inhibitor against tumor growths in vivo.

CP-673451 is an ATP-competitive, potent and selective platelet-derived growth factor receptor inhibitor (PDGFR1 (β)/PDGFR2 (α) IC50 = 1/10 nM with 10 μM ATP; IC50 = 252 nM/c-kit, 450 nM/VEGFR-1/2; >450-fold reduced potency toward other angiogenic receptors and non-receptor kinases). CP-673451 potently inhibits PDGF-BB-induced receptor phosphorylation (IC50 = 6.4 nM; PDGFR1 transfectant) and effectively suppress human cancer xenografts-derived tumor in mice in vivo (ED50 ≤33 mg/kg via b.i.d. or q.d. p.o.) by inhibiting PDGFR phosphorylation and angiogenesis in tumor tissues.

Safety Information

• Storage Class: 11 - Combustible Solids
• wgk: WGK 3