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Datasheet of KW-2449 Hydrochloride
Description: KW 2449 is a multikinase inhibitor of FLT3, ABL, ABL-T315I, and Aurora kinase. KW 2449 displays potent inhibition of growth effects on leukemia cells with FLT3 mutations via inhibition of the FLT3 kinase, resulting in the down-regulation of phosphorylated-FLT3/STAT5, G1 arrest, and apoptosis. KW 2449 induces the reduction of phosphorylated histone H3, G2/M arrest, and apoptosis in FLT3 wild-type human leukemia. KW 2449 contributes to release of the resistance by the simultaneous down-regulation of BCR/ABL and Aurora kinases in imatinib-resistant leukemia. KW 2449 inhibitory activity is not affected by the presence of human plasma protein, such as α1-acid glycoprotein. KW 2449 has potent growth inhibitory activity against various types of leukemia by several mechanisms of action. KW 2449 decreases phosphorylation levels of FLT3 and STAT5 in a dose-dependent manner. KW 2449 is a potent inhibitor of ABL-T315I, which is associated with IM resistance (IC50 of 4 nM). KW-2449 has the potent growth inhibitory activities against not only FLT3/ITD-expressing leukemia cells but also FLT3/KDM-activated and wild-type FLT3-overexpressing leukemia cells. KW 2449 suppresses the phosphorylations of FLT3 (P-FLT3) and its downstream molecule phospho-STAT5 (P-STAT5) in MOLM-13 cells in a dose-dependent manner. KW 2449 can dephosphorylate constitutively active WT-FLT3 kinase but not inhibit the proliferation of leukemia cells if they are not mainly addicted to FLT3 the kinase. KW 2449 mediates cytotoxicity through inhibition of FLT3/ITD. KW 2449 is a direct inhibitor of FLT3 and induces inhibition of its downstream target STAT5. KW 2449 interacts synergistically with HDACIs to induce apoptosis in Ph+ CML cells in a time- and concentration-dependent manner. KW 2449 moderately reduces phosphorylation of histone H3, an indicator of Aurora B activity, in nocodozole-treated K562 cells.
Chemical Information Catalog
DC9860
Purity of current batch:
>98%
Molecular Weight (MW)
368.86
Molecular Formula
C20H20N4O.HCl
CAS No.
1000669-72-6(free base)
Solubility (25°C)
DMSO
Storage
Store at -20°C (desiccating conditions).
Handling: Providing storage is as stated on the product vial and the vial is kept tightly sealed, the product can be stored for up to 24 months. Wherever possible, you should prepare and use solutions on the same day. However, if you need to make up stock solutions in advance, we recommend that you store the solution as aliquots in tightly sealed vials at -20°C. Generally, these will be useable for up to one month. Before use, and prior to opening the vial we recommend that you allow your product to equilibrate to room temperature for at least 1 hour.