1. Protein Tyrosine Kinase/RTK
    Epigenetics
    Cell Cycle/DNA Damage
  2. FLT3
    FGFR
    Bcr-Abl
    Aurora Kinase

KW-2449 

Cat. No.: HY-10339 Purity: 99.85%
Handling Instructions

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.

For research use only. We do not sell to patients.
KW-2449 Chemical Structure

KW-2449 Chemical Structure

CAS No. : 1000669-72-6

Size Price Stock Quantity
Free Sample (0.5-1 mg)   Apply now  
10 mM * 1 mL in DMSO USD 66 In-stock
5 mg USD 60 In-stock
10 mg USD 84 In-stock
50 mg USD 312 In-stock
100 mg USD 576 In-stock
200 mg   Get quote  
500 mg   Get quote  

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  • Biological Activity

  • Protocol

  • Technical Information

  • Purity & Documentation

  • References

Description

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.

IC50 & Target

IC50: 6.6 nM (FLT3), 14 nM (ABL), 4 nM (ABLT315I), 48 nM (Aurora kinase)[1]

In Vitro

KW-2449 shows growth inhibitory activities against FLT3/ITD-, FLT3/D835Y-, and wt-FLT3/FL-expressing 32D cells, MOLM-13 and MV4;11 with GI50 values of 0.024, 0.046, 0.014, 0.024, and 0.011 μM, respectively. 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 increases the percentage of cells in the G1 phase of the cell cycle and reciprocally reduced the percentage of cells in the S phase, resulting in the increase of apoptotic cell population[1].

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].

Clinical Trial
References
Preparing Stock Solutions
Concentration Volume Mass 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
Please refer to the solubility information to select the appropriate solvent.
Cell Assay
[1]

Cell viability is determined by the sodium 3′-[1-(phenylaminocarbonyl)-3, 4-tetrazolium]-bis (4-methoxy-6-nitro) benzene sulfonic acid hydrate assay after incubation with or without KW-2449 for 72 hours at 37°C. The number of viable cells is determined using the Cell Proliferation Kit II[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration
[1]

KW-2449 is prepared in 0.5 wt/vol% MC400[1].

Mice: SCID mice are subcutaneously inoculated with MOLM-13 cells. Five days after inoculation, tumor volume is measured using the Antitumor test system II. The 25 mice with tumors ranging from 90 to 130 mm3 are selected and randomized using the Antitumor test system II. From the day of randomization, vehicle (0.5 wt/vol% MC400) or KW-2449 (2.5, 5.0, 10, and 20 mg/kg) is orally administered to mice twice a day for 14 days. Tumor volume is measured twice a week during the treatment[1]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.

References
Molecular Weight

332.4

Formula

C₂₀H₂₀N₄O

CAS No.

1000669-72-6

SMILES

O=C(C1=CC=C(/C=C/C2=NNC3=C2C=CC=C3)C=C1)N4CCNCC4

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

Solvent & Solubility

DMSO

* "<1 mg/mL" means slightly soluble or insoluble. "≥" means soluble, but saturation unknown.

Purity: 99.85%

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KW-2449
Cat. No.:
HY-10339
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