A potent multi-kinase inhibitor of FLT3

KW 2449 – 25 mg

Brand:
Cayman
CAS:
1000669-72-6
Storage:
-20
UN-No:
Non-Hazardous - /

KW 2449 is a potent multi-kinase inhibitor of fml-like tyrosine kinase 3 (FLT3), Abelson tyrosine-protein kinase 1 (ABL), ABL-T315I, and Aurora kinase (IC50s = 6.6, 14, 4, and 48 nM, respectively).{40201} It has growth inhibitory activity against leukemia cells expressing FLT3 with activating mutations (GI50s = 11-46 nM) and suppresses phosphorylation of FLT3 and STAT5 in MOLM-13 cells in a dose-dependent manner in vitro. KW 2499 (100 nM) inhibits colony formation of human primary acute myeloid leukemia (AML) cells with wild-type or activated mutant FLT3. It also induces MOLM-13 xenograft regression in a dose-dependent manner in vivo. Formulations containing KW 2499 are being investigated in clinical trials for treatment of relapsed or refractory AML.  

 

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Description

A potent multi-kinase inhibitor of FLT3, ABL, ABL-T315I, and Aurora kinase (IC50s = 6.6, 14, 4, and 48 nM, respectively); has growth inhibitory activity against leukemia cells expressing FLT3 with activating mutations (GI50s = 11-46 nM); suppresses phosphorylation of FLT3 and STAT5 in MOLM-13 cells in a dose-dependent manner in vitro; inhibits colony formation of human primary AML cells with wild-type or activated mutant FLT3; induces MOLM-13 xenograft regression in a dose-dependent manner in vivo

Formal name: [4-[2-(1H-indazol-3-yl)ethenyl]phenyl]-1-piperazinyl-methanone

Synonyms: 

Molecular weight: 332.4

CAS: 1000669-72-6

Purity: ≥98%

Formulation: A crystalline solid

Product Type|Biochemicals|Kinase Inhibitors|Abl Family & Bcr-Abl||Product Type|Biochemicals|Kinase Inhibitors|Aurora||Product Type|Biochemicals|Kinase Inhibitors|PDGFR Family||Product Type|Biochemicals|Small Molecule Inhibitors|Kinases||Research Area|Cancer|Cell Signaling|Abl family & Bcr-Abl Signaling||Research Area|Cancer|Cell Signaling|Aurora Signaling||Research Area|Cancer|Cell Signaling|Growth Factor Receptor Signaling

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