SML3546
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
Sign In to View Organizational & Contract Pricing.
Select a Size
Change View
About This Item
Empirical Formula (Hill Notation):
C20H20N4O
CAS Number:
Molecular Weight:
332.40
NACRES:
NA.77
UNSPSC Code:
12352200
Quality Level
assay
≥95% (HPLC)
form
powder
color
white to beige
solubility
DMSO: 2 mg/mL, clear
storage temp.
2-8°C
Biochem/physiol Actions
Orally active FLT3, ABL, FGFR1, Aurora A inhibitor and a KCC2 expression-enhancing compound (KEEC) with in vivo leukemia & Rett syndrome (RTT) therapeutic efficacy.
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
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Regulatory Information
新产品
This item has
Choose from one of the most recent versions:
Already Own This Product?
Find documentation for the products that you have recently purchased in the Document Library.
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)
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)
Global Trade Item Number
| SKU | GTIN |
|---|---|
| SML3546-10MG | 04065268039458 |
| SML3546-50MG | 04065268039465 |