[4-[2-(1H-Indazol-3-yl)ethenyl]phenyl]-1-piperazinylmethanone CAS#: 1000669-72-6

ChemicalBook > Product Catalog > Biochemical Engineering > Inhibitors > Angiogenesis > FLT3 inhibitors > [4-[2-(1H-Indazol-3-yl)ethenyl]phenyl]-1-piperazinylmethanone

[4-[2-(1H-Indazol-3-yl)ethenyl]phenyl]-1-piperazinylmethanone

Basic information Safety Supplier Related

[4-[2-(1H-Indazol-3-yl)ethenyl]phenyl]-1-piperazinylmethanone Basic information

Product Name:

[4-[2-(1H-Indazol-3-yl)ethenyl]phenyl]-1-piperazinylmethanone

Synonyms:

[4-[2-(1H-Indazol-3-yl)ethenyl]phenyl]-1-piperazinylmethanone
KW 2449
(E)-(4-(2-(1H-indazol-3-yl)vinyl)phenyl)(piperazin-1-yl)methanone
KW2449(E)-(4-(2-(1H-indazol-3-yl)vinyl)phenyl)(piperazin-1-yl)methanonehydrochloride
KW-2449;KW 2449; KW2449
[4-[(E)-2-(1H-indazol-3-yl)ethenyl]phenyl]-piperazin-1-ylmethanone
KW-2449 100MG
{4-[(E)-2-(1H-Indazol-3-yl)vinyl]phenyl}(1-piperazinyl)methanone

CAS:

1000669-72-6

MF:

C20H20N4O

MW:

332.4

Product Categories:

Inhibitors
Inhibitor

Mol File:

1000669-72-6.mol

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[4-[2-(1H-Indazol-3-yl)ethenyl]phenyl]-1-piperazinylmethanone Chemical Properties

Boiling point:: 604.1±55.0 °C(Predicted)
Density: 1.28
storage temp.: -20°C
solubility: Soluble in DMSO (>25 mg/ml)
pka: 13.76±0.40(Predicted)
form: solid
color: Pale yellow
Stability:: Stable for 1 year from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 1 month.

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[4-[2-(1H-Indazol-3-yl)ethenyl]phenyl]-1-piperazinylmethanone Usage And Synthesis

Description

KW-2449 is a potent multikinase inhibitor (IC50’s: FLT3 = 7 nM, FGFR1 = 36 nM, Abl = 14 nM, Abl-T315 = 4 nM) with anti-leukemic effects.1,2,3

Uses

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.

Definition

ChEBI: [4-[2-(1H-indazol-3-yl)ethenyl]phenyl]-(1-piperazinyl)methanone is a member of indazoles.

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].

target

FLT3

IC 50

Abl: 4 nM (IC₅₀); ABL-T315I: 14 nM (IC₅₀); FGFR1: 36 nM (IC₅₀); Aurora A: 48 nM (IC₅₀); FLT3/D835Y: 1 nM (IC₅₀); FLT3: 6.6 nM (IC₅₀); JAK2: 150 nM (IC₅₀); SRC: 400 nM (IC₅₀); PDFGRα: 1700 nM (IC₅₀)

References

Shiotsu et al. (2007) KW-2449, a Novel Multi-Kinase Inhibitor Against FLT3, Abl, FGFR1, and Aurora, Suppresses the Growth of AML Both In Vitro and In Vivo; Blood; 110 1832 Shiotsu et al. (2009) KW-2449, a Novel Multi-Kinase Inhibitor, suppresses the growth of leukemia cells with FLTY3 mutations or T315l-mutated BCR/ABL translocation; Blood; 114 1607 Pratz et al. (2009) A pharmacodynamic study of the FLT3 inhibitor KW-2449 yields insight into the basis for clinical response; Blood; 113 3938

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