SML2875

DCC-2618

≥98% (HPLC)

• Sinónimos: DCC 2618, DCC2618, N-(2,5-Difluoro-4-(2-(1-methyl-1H-pyrazol-4-yl)pyridin-4-yloxy)phenyl)-N′-phenylcyclopropane-1,1-dicarboxamide, c-Kit-IN-1
• Fórmula empírica (notación de Hill): C₂₆H₂₁F₂N₅O₃
• Número de CAS: 1225278-16-9
• Peso molecular: 489.47
• Número MDL: MFCD22571733
• Código UNSPSC: 12352200
• NACRES: NA.77

Propiedades

• Nivel de calidad: 100
• Análisis: ≥98% (HPLC)
• formulario: powder
• color: white to beige
• solubilidad: DMSO: 2 mg/mL, clear
• temp. de almacenamiento: −20°C
• cadena SMILES: O=C(NC1=CC=CC=C1)C2(CC2)C(NC(C=C3F)=C(F)C=C3OC4=CC(C5=CN(C)N=C5)=NC=C4)=O
• InChI: 1S/C26H21F2N5O3/c1-33-15-16(14-30-33)21-11-18(7-10-29-21)36-23-13-19(27)22(12-20(23)28)32-25(35)26(8-9-26)24(34)31-17-5-3-2-4-6-17/h2-7,10-15H,8-9H2,1H3,(H,31,34)(H,32,35)
• Clave InChI: WWOXKWLDMLMYQY-UHFFFAOYSA-N

Descripción

Acciones bioquímicas o fisiológicas

DCC-2618 is an orally active, potent type II switch pocket (SP) inhibitor against c-KIT (IC₅₀ = 4 nM/WT, 8 nM/V654A, 18 nM/T670I, 5 nM/D816H, 14 nM/D816V) and PDGFR. DCC-2618 locks c-KIT & PDGFR in an inactive conformation and is effective against multiple clinical forms of mutations resistant to type I ATP (catalytic)-site inhibitors Imatinib and Sunitinib. DCC-2618 inhibits cellular c-KIT activation (IC₅₀ = 36 nM/WT, 2 nM/ex 11 del, 7 nM/ex 11 del & V654A, 53 nM/V560D & D820A) and is efficacious against KIT mutants-mediated cancer growth in cultres (IC₅₀ = 2 nM; GIST with KIT D816Y) and in mice in vivo (50 mg/kg b.i.d. p.o.; GIST with KIT delW557K558/Y823D, AML with KIT N822K).

Información de seguridad

• Código de clase de almacenamiento: 11 - Combustible Solids
• Clase de riesgo para el agua (WGK): WGK 3
• Punto de inflamabilidad (°F): Not applicable
• Punto de inflamabilidad (°C): Not applicable