SML3546

KW-2449

≥95% (HPLC)

• Sinónimos: (E)-1-{4-[2-(1H-Indazol-3-yl)vinyl]benzoyl}piperazine, KW 2449, KW2449, [4-[(E)-2-(1H-Indazol-3-yl)ethenyl]phenyl]-1-piperazinylmethanone, [4-[(E)-2-(1H-Indazol-3-yl)ethenyl]phenyl]-piperazin-1-ylmethanone
• Fórmula empírica (notación de Hill): C₂₀H₂₀N₄O
• Número de CAS: 841258-76-2
• Peso molecular: 332.40
• Código UNSPSC: 12352200
• NACRES: NA.77

Propiedades

• Nivel de calidad: 100
• Ensayo: ≥95% (HPLC)
• Formulario: powder
• color: white to beige
• solubilidad: DMSO: 2 mg/mL, clear
• temp. de almacenamiento: 2-8°C

Descripción

Acciones bioquímicas o fisiológicas

KW-2449 is an orally active potent kinase inhibitor against FLT3 (wt/D835Y IC50 = 6.6/1 nM), ABL (wt/T315I IC50 = 14/4 nM), FGFR1 (IC50 = 36 nM), and aurora A (IC50 = 48 nM). KW-2449 also inhibits JAK2, KIT, Src with reduced potency (IC50 = 150, 300, 400 nM, respectively), but not EGFR, Fms, IGF1R or PDGFRα (IC50 >1 μM). In addition to its anti-leukemia efficacy in cultures (GI50 10-650 nM) and in vivo (5-20 mg/kg b.i.d. p.o.), KW-2449 is also a K+/Cl- cotransporter 2 (KCC2) expression-enhancing compound (KEEC) that ameliorates disease phenotypes in a Rett syndrome (RTT) model in Mecp2 mutant mice (2 mg/kg/d i.p.).

Orally active FLT3, ABL, FGFR1, Aurora A inhibitor and a KCC2 expression-enhancing compound (KEEC) with in vivo leukemia & Rett syndrome (RTT) therapeutic efficacy.

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