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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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FLT3 ligand impedes the efficacy of FLT3 inhibitors in vitro and in vivo
Blood, 117(12), 3286-3293 (2011)
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-mutant allelic burden and clinical status are predictive of response to FLT3 inhibitors in AML
Blood, 115(7), 1425-1432 (2010)
A pharmacodynamic study of the FLT3 inhibitor KW-2449 yields insight into the basis for clinical response
Blood, 113(17), 3938-3946 (2009)
Pharmacological enhancement of KCC2 gene expression exerts therapeutic effects on human Rett syndrome neurons and Mecp2 mutant mice
Science Translational Medicine (2019)
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