Network Version
KW-2449 Data Sheet
| Product Name: | KW-2449 |
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|---|---|---|
| CAS No.: | 1000669-72-6 | |
| Cat. No.: | HY-10339 | |
| MWt: | 332.4 | |
| Formula: | C20H20N4O | |
| Purity : | >98% | |
| Solubility: | DMSO : ≥ 50 mg/mL (150.42 mM) | |
| Mechanisms: | Target: Cancer | |
| Biological Activity: | ||
| KW-2449 is a multi-targeted kinase inhibitor of FLT3, ABL, ABLT315I and Aurora kinase with IC50s of 6.6, 14, 4 and 48 nM, respectively. IC50 & Target: IC50: 6.6 nM (FLT3), 14 nM (ABL), 4 nM (ABLT315I), 48 nM (Aurora kinase)[1] In Vitro: KW-2449 shows growth inhibitory activities against FLT3/ITD-, FLT3/D835Y-, and wt-FLT3/FL-expressing 32D cells, MOLM-13 and MV4;11 with GI50 values of 0.024, 0.046, 0.014, 0.024, and 0.011 μM, respectively. KW-2449 suppresses the phosphorylations of FLT3 (P-FLT3) and its downstream molecule phospho-STAT5 (P-STAT5) in MOLM-13 cells in a dose-dependent manner. KW-2449 increases the percentage of cells in the G1 phase of the cell cycle and reciprocally reduced the percentage of cells in the S phase, resulting in the increase of apoptotic cell population[1]. In Vivo: Oral administration of KW-2449 shows dose-dependent and significant tumor growth inhibition in FLT3-mutated xenograft model with minimum bone marrow suppression. In FLT3 wild-type human leukemia, it induces the reduction of phosphorylated histone H3, G2/M arrest, and apoptosis. In imatinib-resistant leukemia, KW-2449 contributes to release of the resistance by the simultaneous down-regulation of BCR/ABL and Aurora kinases. Furthermore, the antiproliferative activity of KW-2449 is confirmed in primary samples from AML and imatinib-resistant patients. The inhibitory activity of KW-2449 is not affected by the presence of human plasma protein, such as α1-acid glycoprotein[1]. | ||
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