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KW 2449
Cat No.
CEI-0063
Description
As a multi-target inhibitor, KW-2449 potently inhibits Flt3, Abl and Aurora A with IC50 of 6.6 nM, 14 nM and 48 nM.
CAS No.
1000669-72-6
Molecular Weight
332.4
Purity
>99%
Storage
2 years at -20 centigrade
Targets
Flt3, Abl, Aurora A
Molecular Formula
C20H20N4O
Chemical Name
(E)-(4-(2-(1H-indazol-3-yl)vinyl)phenyl)(piperazin-1-yl)methanone
Solubility
DSMO 67 mg/mL Water
In vitro
As a multi-target inhibitor, KW-2449 potently inhibits Flt3, Abl and Aurora A with IC50 of 6.6 nM, 14 nM and 48 nM, respectively. KW-2449 showed the potent growth inhibitory effects on leukemia cells with FLT3 mutations by inhibition of the FLT3 kinase, resulting in the down-regulation of hosphorylated-FLT3/STAT5, G(1) arrest, and apoptosis. In FLT3 wild-type human leukemia, it induced the reduction of phosphorylated histone H3, G(2)/M arrest, and apoptosis. In imatinib-resistant leukemia, KW-2449 contributed to release of the resistance by the simultaneous down-regulation of BCR/ABL and Aurora kinases.
In vivo
Oral administration of KW-2449 showed dose-dependent and significant tumor growth inhibition in FLT3-mutated xenograft model with minimum bone marrow suppression.
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