Referencia número: HY-10339

KW-2449

8 Cited Publications

Revisión del cliente

Based on 8 publication(s) in Google Scholar

KW-2449 is a multi-targeted kinase inhibitor of FLT3, ABL, ABL^T315I and Aurora kinase with IC₅₀s of 6.6, 14, 4 and 48 nM, respectively.

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Pureza: 99.91%
No. CAS: 1000669-72-6
Fòrmula: C₂₀H₂₀N₄O
Peso molecular:332.40

Almacenamiento:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

KW-2449 Chemical Structure

No. CAS: 1000669-72-6

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Actividad biológica
- Descripciòn
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Ensayo clínico
Chemical Information
Publications (8)
Solvente y solubilidad
- In Vitro
- In Vivo
Protocolo
Pureza y Documentación
Referencias
Help & FAQs
Classifications
Bioz

Actividad biológica

Descripciòn

KW-2449 is a multi-targeted kinase inhibitor of FLT3, ABL, ABL^T315I 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)

Ver todos los productos específicos de isoformas Bcr-Abl :

Abl
Bcr-Abl

Ver todos los productos específicos de isoformas Aurora Kinase :

Cellular Effect

Cell Line	Type	Value	Description	References
K562	GI₅₀	0.27 μM Compound: KW-2449	Antiproliferative activity against imatinib resistant human K562 cells harbouring ABL-T315I mutant assessed as cell growth inhibition by XTT assay Antiproliferative activity against imatinib resistant human K562 cells harbouring ABL-T315I mutant assessed as cell growth inhibition by XTT assay	[PMID: 35551036]
K562	GI₅₀	0.27 μM Compound: KW-2449	Antiproliferative activity against imatinib resistant human K562 cells harbouring wild type ABL assessed as cell growth inhibition by XTT assay Antiproliferative activity against imatinib resistant human K562 cells harbouring wild type ABL assessed as cell growth inhibition by XTT assay	[PMID: 35551036]
MOLM-14	IC₅₀	14.8 nM Compound: 5, KW-2449	Inhibition of FLT3-mediated STAT5 phosphorylation in human MOLM14 cells Inhibition of FLT3-mediated STAT5 phosphorylation in human MOLM14 cells	10.1039/C1MD00175B

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].

MedChemExpress (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].

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

Ensayo clínico

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

No. CAS 1000669-72-6
Appearance Solid
Peso molecular 332.40
Fòrmula C₂₀H₂₀N₄O
Color White to light yellow
SMILES

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

Room temperature in continental US; may vary elsewhere.

Almacenamiento

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (8)

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Journal Impact Factor

Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
Cell Rep Med

A human iPSC-derived sensory neuron platform for high-throughput discovery of neuroprotectants against chemotherapy-induced peripheral neuropathy. [Abstract]

2026 May 19;7(5):102787. PMID: 42097147
Cell Rep

Pharmacological boosting of cGAS activation sensitizes chemotherapy by enhancing antitumor immunity. [Abstract]

2023 Mar 20;42(3):112275. PMID: 36943864
Biochem Pharmacol

The multitargeted kinase inhibitor KW-2449 ameliorates cisplatin-induced nephrotoxicity by targeting RIPK1-mediated necroptosis. [Abstract]

2021 Jun:188:114542. PMID: 33819469
Inflammation

KW-2449 Ameliorates Cardiac Dysfunction in a Rat Model of Sepsis-Induced Cardiomyopathy. [Abstract]

2025 Jan 22. PMID: 39843680
Int J Mol Sci

Evaluation of Protein Kinase Inhibitors with PLK4 Cross-Over Potential in a Pre-Clinical Model of Cancer. [Abstract]

2019 Apr 29;20(9):2112. PMID: 31035676
SSRN

2025 Aug 6.
bioRxiv

2024 October 03.

Solvente y solubilidad

In Vitro:

DMSO : ≥ 50 mg/mL (150.42 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

* "≥" means soluble, but saturation unknown.

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

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. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Calculadora de molaridad

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculadora de dilución

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 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

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocolo

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].

MedChemExpress (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].

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

Pureza y Documentación

Select Batch:

Pureza: 99.98%

Assay: 99.98%

ee.: 99.98%

Ficha de datos (282 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instrucciones de manejo (2659 KB)

Referencias

[1]. Shiotsu Y, et al. KW-2449, a novel multikinase inhibitor, suppresses the growth of leukemia cells with FLT3 mutations or T315I-mutated BCR/ABL translocation. Blood. 2009 Aug 20;114(8):1607-17. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	3.0084 mL	15.0421 mL	30.0842 mL	75.2106 mL
	5 mM	0.6017 mL	3.0084 mL	6.0168 mL	15.0421 mL
	10 mM	0.3008 mL	1.5042 mL	3.0084 mL	7.5211 mL
	15 mM	0.2006 mL	1.0028 mL	2.0056 mL	5.0140 mL
	20 mM	0.1504 mL	0.7521 mL	1.5042 mL	3.7605 mL
	25 mM	0.1203 mL	0.6017 mL	1.2034 mL	3.0084 mL
	30 mM	0.1003 mL	0.5014 mL	1.0028 mL	2.5070 mL
	40 mM	0.0752 mL	0.3761 mL	0.7521 mL	1.8803 mL
	50 mM	0.0602 mL	0.3008 mL	0.6017 mL	1.5042 mL
	60 mM	0.0501 mL	0.2507 mL	0.5014 mL	1.2535 mL
	80 mM	0.0376 mL	0.1880 mL	0.3761 mL	0.9401 mL
	100 mM	0.0301 mL	0.1504 mL	0.3008 mL	0.7521 mL

Keywords

KW-2449

8 Cited Publications

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KW-2449

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MCE Bioactive Compound Library

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Bioactive Compound Library

Anti-Fibrosis Compound Library

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Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

Posttranslational Modification Library

Publications Citing Use of MedChemExpress (MCE) KW-2449

Ver todos los productos específicos de isoformas Bcr-Abl

Ver todos los productos específicos de isoformas Aurora Kinase

Actividad biológica

Chemical Information

Publications (8)

Solvente y solubilidad

Protocolo

Pureza y Documentación

Referencias

Help & FAQs

Complete Stock Solution Preparation Table

KW-2449 Related Classifications

HY-10339 Related Classifications