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KW-2449

HY-10339

(KW 2449; KW2449)

KW-2449

KW-2449 Chemical Structure

KW-2449 is a multiple-targeted inhibitor, mostly for Flt3 with IC50 of 6.6 nM, modestly potent to FGFR1, Bcr-Abl and Aurora A; little effect on PDGFRβ, IGF-1R, EGFR.

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10 mM * 1 mL in DMSO $88 In-stock
10 mg $80 In-stock
50 mg $300 In-stock
100 mg $550 In-stock
200 mg Get quote
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Size Price Stock Quantity
Free sample   Apply now  
10 mM * 1 mL in DMSO €86 In-stock
10 mg €78 In-stock
50 mg €294 In-stock
100 mg €539 In-stock
200 mg Get quote
500 mg Get quote

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Product name: KW-2449
Cat. No.: HY-10339

KW-2449 Data Sheet

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    Purity: 99.66%

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Biological Activity of KW-2449

KW-2449 is a multiple-targeted inhibitor, mostly for Flt3 with IC50 of 6.6 nM, modestly potent to FGFR1, Bcr-Abl and Aurora A; little effect on PDGFRβ, IGF-1R, EGFR.
IC50 value: 6.6 nM [1]
Target: Flt3
in vitro: Phosphorylation levels of FLT3 and STAT5 are decreased by KW-2449 in a dose-dependent manner. In addition, it potently inhibits ABL-T315I, which is associated with IM resistance, with IC50 of 4 nM. On the other hand, KW-2449 has little effect on PDGFRβ, IGF-1R, EGFR, and various serine/threonine kinases even at a concentration of 1 μM. 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 [1]. KW-2449 is rapidly absorbed and converted to a major metabolite M1.Preclinical studies reveal that KW-2449 is converted by monoamine oxidase-B (MAO-B) and aldehyde oxidase into its major metabolite M1.KW-2449 mediates cytotoxicity thru inhibition of FLT3/ITD.KW-2449 is a direct inhibitor of FLT3 and induces inhibition of its downstream target STAT5 [2]. KW2449 interacts synergistically with HDACIs to induce apoptosis in Ph+ CML cells in a time- and concentration-dependent manner. KW2449 synergistically enhances the lethality of vorinostat/SNDX275 in CML cells.KW-2449 regimens are active against additional IM-resistant Bcr/Abl+ leukemia cells. KW2449 moderately reduces phosphorylation of histone H3, an indicator of Aurora B activity, in nocodozole-treated K562 cells [3].
in vivo: In the MOLM-13 tumor xenograft model, oral administration of KW-2449 for 14 days shows a potent and significant antitumor effect in a dose-dependent manner [1].

Protocol (Extracted from published papers and Only for reference)

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Chemical Information

M.Wt 332.4 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C20H20N4O
CAS No 1000669-72-6
Solvent & Solubility

DMSO ≥63mg/mL Water <1.2mg/mL Ethanol ≥63mg/mL

Preparing Stock Solutions

1 mg 5 mg 10 mg
1 mM 3.0084 mL 15.0421 mL 30.0842 mL
5 mM 0.6017 mL 3.0084 mL 6.0168 mL
10 mM 0.3008 mL 1.5042 mL 3.0084 mL

References on KW-2449

Inhibitor Kit

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