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Key Documents

SML3546

Sigma-Aldrich

KW-2449

≥95% (HPLC)

Synonym(s):

(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

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About This Item

Empirical Formula (Hill Notation):
C20H20N4O
CAS Number:
841258-76-2
Molecular Weight:
332.40
UNSPSC Code:
12352200
NACRES:
NA.77

Quality Level

100

Assay

≥95% (HPLC)

form

powder

color

white to beige

solubility

DMSO: 2 mg/mL, clear

storage temp.

2-8°C

Biochem/physiol Actions

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.).

Storage Class Code

11 - Combustible Solids

WGK

WGK 3

Flash Point(F)

Not applicable

Flash Point(C)

Not applicable

Certificates of Analysis (COA)

Search for Certificates of Analysis (COA) by entering the products Lot/Batch Number. Lot and Batch Numbers can be found on a product’s label following the words ‘Lot’ or ‘Batch’.

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Evaluation of Protein Kinase Inhibitors with PLK4 Cross-Over Potential in a Pre-Clinical Model of Cancer
International Journal of Molecular Sciences, 20 (2019)
Pharmacological enhancement of KCC2 gene expression exerts therapeutic effects on human Rett syndrome neurons and Mecp2 mutant mice
Science Translational Medicine (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)
HDAC inhibitors potentiate the activity of the BCR/ABL kinase inhibitor KW-2449 in imatinib-sensitive or -resistant BCR/ABL+ leukemia cells in vitro and in viv
Clinical Cancer Research, 17(10), 3219-3232 (2011)
FLT3 ligand impedes the efficacy of FLT3 inhibitors in vitro and in vivo
Blood, 117(12), 3286-3293 (2011)
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