| Cat.No.: | BSM-0001 |
| Product Name: | KW 2449 |
| CAS No.: | 1000669-72-6 |
| 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. |
| Molecular Weight: | 332.4 |
| Purity: | >99% |
| Storage: | 2 years at -20°C |
| 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. |
| Warning: | For Research Use Only! Not For Use in Humans. |
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