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Chemical Structure| 1000669-72-6 Chemical Structure| 1000669-72-6

Structure of KW-2449
CAS No.: 1000669-72-6

Chemical Structure| 1000669-72-6

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KW-2449 is a multi-target kinase inhibitor with IC50 values of 6.6, 14, 4, and 48 nM against FLT3, ABL, ABLT315I, and Aurora kinase, respectively.

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Product Details of KW-2449

CAS No. :1000669-72-6
Formula : C20H20N4O
M.W : 332.40
SMILES Code : O=C(C1=CC=C(C=CC2=NNC3=C2C=CC=C3)C=C1)N4CCNCC4
MDL No. :MFCD18385006

Safety of KW-2449

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Related Pathways of KW-2449

epigenetics
DNA
RTK

Isoform Comparison

Biological Activity

Target
  • Aurora A

    Aurora A, IC50:48 nM

  • Abl

    Abl, IC50:14 nM

    Abl (T315I), IC50:4 nM

In Vitro:

Cell Line
Concentration Treated Time Description References
neurons 1 µM 20 days to treat morphological deficits in MECP2-KO neurons, significantly enhancing dendritic length, branch number, and morphological complexity PMC9795779
cerebral organoids 1 µM 49 days to treat developmental defects in MECP2-KO cerebral organoids, restoring the proportion of cycling hNPs and the number of TBR1+ and CTIP2+ post-mitotic neurons PMC9795779
RAW 264.7 cells 1 µM 24 h KW2449 reduced LZ-induced necroptosis and decreased the expression of inflammatory cytokines. PMC10040599
mouse embryonic fibroblast cells (MEFs) 1 μM 30 min KW-2449 inhibited cisplatin-induced lipid peroxidation and ferroptosis. PMC11493980
human fibrosarcoma HT1080 cells 1 μM 30 min KW-2449 inhibited Erastin-induced ferroptosis. PMC11493980
liver cancer HepG2 cells 1 μM 30 min KW-2449 inhibited Erastin-induced ferroptosis. PMC11493980
human renal proximal tubule HK2 cells 1 μM 30 min KW-2449 inhibited RSL3-induced ferroptosis. PMC11493980
human lung cancer H1299 cells 1 μM 30 min KW-2449 inhibited RSL3-induced ferroptosis. PMC11493980
human colon cancer HT29 cells 1 μM 30 min KW-2449 inhibited RSL3-induced ferroptosis. PMC11493980
K562 0.4 µM 72 h To evaluate the effect of KW2449 combined with HDAC inhibitors on apoptosis, results showed that combined treatment significantly increased apoptosis. PMC3096723
LAMA84 0.4 µM 48 h To evaluate the effect of KW2449 combined with HDAC inhibitors on apoptosis, results showed that combined treatment significantly increased apoptosis. PMC3096723
BV173/E255K 0.4 µM 48 h To evaluate the effect of KW2449 combined with HDAC inhibitors on apoptosis, results showed that combined treatment significantly increased apoptosis. PMC3096723
Adult/T315I 0.4 µM 48 h To evaluate the effect of KW2449 combined with HDAC inhibitors on apoptosis, results showed that combined treatment significantly increased apoptosis. PMC3096723
K562 0.4 µM 72 h KW2449 synergistically increased apoptosis with HDACIs PMC3096723
LAMA84 0.4 µM 48 h KW2449 synergistically increased apoptosis with HDACIs PMC3096723
BV173/E255K 0.4 µM 48 h KW2449 synergistically increased apoptosis with HDACIs PMC3096723
Adult/T315I 0.4 µM 48 h KW2449 synergistically increased apoptosis with HDACIs PMC3096723

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Rats Collagen-induced arthritis (CIA) model Oral gavage 7 mg/kg Once daily for 28 days KW2449 reduced joint swelling, joint bone destruction, tissue damage, and plasma inflammatory cytokine levels in CIA rats. PMC10040599
C57BL/6 mice cisplatin-induced acute kidney injury (AKI) model oral gavage 10 mg/kg once daily for 72 hours KW-2449 alleviated cisplatin-induced renal damage by inhibiting lipid peroxidation and ferroptosis. PMC11493980
BALB/C mice IM-resistant ALL xenograft model Oral or intraperitoneal injection 32 mg/kg 5 days/week for 4 weeks To evaluate the therapeutic effect of KW2449 combined with HDAC inhibitors on IM-resistant ALL, results showed that combined treatment significantly prolonged survival and reduced tumor signal. PMC3096723
BALB/C mice IM-resistant ALL xenograft model Oral and intraperitoneal injection 32 mg/kg 5 days/week, continuous treatment Combination of KW2449 with HDACIs significantly prolonged the survival of mice bearing IM-resistant ALL cells PMC3096723

Clinical Trial:

NCT Number Conditions Phases Recruitment Completion Date Locations
NCT00779480 Acute Myelogenous Leukemia (AM... More >>L) Less << PHASE1 TERMINATED 2025-12-10 University of Maryland, Greene... More >>baum Cancer Center, Baltimore, Maryland, 21201, United States|Johns Hopkins University, Baltimore, Maryland, 21231, United States|University of Pennsylvania, Philadelphia, Pennsylvania, 19104, United States|St. Francis Hospital, Greenville, South Carolina, 29601, United States Less <<
NCT00346632 Acute Myelogenous Leukemia|Acu... More >>te Lymphoblastic Leukemia|Myelodysplastic Syndromes|Chronic Myelogenous Leukemia Less << PHASE1 TERMINATED 2025-04-08 Johns Hopkins Hospital, Baltim... More >>ore, Maryland, 21287, United States|Contact Kyowa, Princeton, New Jersey, 08540, United States|Weill Cornell/New York Presbyterian Hospital, New York, New York, 10021, United States|M.D. Anderson Cancer Center, Houston, Texas, 77030, United States Less <<

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

3.01mL

0.60mL

0.30mL

15.04mL

3.01mL

1.50mL

30.08mL

6.02mL

3.01mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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