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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.
储存分类代码
11 - Combustible Solids
WGK
WGK 3
闪点(°F)
Not applicable
闪点(°C)
Not applicable
法规信息
新产品
历史批次信息供参考:
分析证书(COA)
Lot/Batch Number
Evaluation of Protein Kinase Inhibitors with PLK4 Cross-Over Potential in a Pre-Clinical Model of Cancer
International Journal of Molecular Sciences, 20 (2019)
KW-2449, a novel multikinase inhibitor, suppresses the growth of leukemia cells with FLT3 mutations or T315I-mutated BCR/ABL translocation
Blood, 114(8), 1607-1617 (2009)
Pharmacological enhancement of KCC2 gene expression exerts therapeutic effects on human Rett syndrome neurons and Mecp2 mutant mice
Science Translational Medicine (2019)
FLT3-mutant allelic burden and clinical status are predictive of response to FLT3 inhibitors in AML
Blood, 115(7), 1425-1432 (2010)
FLT3 ligand impedes the efficacy of FLT3 inhibitors in vitro and in vivo
Blood, 117(12), 3286-3293 (2011)
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