2. Protein Tyrosine Kinase/RTK
    Epigenetics
    Cell Cycle/DNA Damage
    Apoptosis
  3. FLT3
    FGFR
    Bcr-Abl
    Aurora Kinase
    Apoptosis
  4. KW-2449

KW-2449 

Cat. No.: HY-10339 Purity: 99.85%
COA 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 (0.1 - 0.5 mg)   Apply Now  
Solution
10 mM * 1 mL in DMSO USD 73 In-stock
Solid + Solvent
10 mM * 1 mL
ready for reconstitution
 USD 73 In-stock
Solid
5 mg USD 66 In-stock
10 mg USD 92 In-stock
50 mg USD 343 In-stock
100 mg USD 634 In-stock
200 mg   Get quote  
500 mg   Get quote  

* Please select Quantity before adding items.

This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 5 publication(s) in Google Scholar

Top Publications Citing Use of Products

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FGFR FGFR1 FGFR2 FGFR3 FGFR4 FGF21

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Aurora Kinase Aurora A Aurora B Aurora C

  • Biological Activity

  • Protocol

  • Purity & Documentation

  • References

  • Customer Review

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[1]

Abl

4 nM (IC50)

ABL-T315I

14 nM (IC50)

FGFR1

36 nM (IC50)

Aurora A

48 nM (IC50)

FLT3/D835Y

1 nM (IC50)

FLT3

6.6 nM (IC50)

JAK2

150 nM (IC50)

SRC

400 nM (IC50)

PDFGRα

1700 nM (IC50)

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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
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].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
Molecular Weight

332.40

Appearance

Solid

Formula

C20H20N4O
CAS No.
SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : ≥ 50 mg/mL (150.42 mM)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent 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.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.5 mg/mL (7.52 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.5 mg/mL (7.52 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.5 mg/mL (7.52 mM); Clear solution

*All of the co-solvents are available by MCE.
Purity & Documentation

Purity: 99.85%

COA (253 KB) HNMR (179 KB) LCMS (369 KB)

Handling Instructions (2659 KB)
References
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]

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
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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Keywords:

KW-24491000669-72-6KW2449KW 2449FLT3FGFRBcr-AblAurora KinaseApoptosisCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Fibroblast growth factor receptorInhibitorinhibitorinhibit

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