KW-2449
Based on 8 publication(s) in Google Scholar
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.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.91%
- No. CAS: 1000669-72-6
- Fòrmula: C20H20N4O
- Peso molecular:332.40
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) KW-2449
More- Sci Transl Med. 2018 Jul 18;10(450):eaaq1093. [Abstract]
- Cell Rep Med. 2026 May 19;7(5):102787. [Abstract]
- Cell Rep. 2023 Mar 20;42(3):112275. [Abstract]
- Biochem Pharmacol. 2021 Jun:188:114542. [Abstract]
- Int J Mol Sci. 2019 Apr 29;20(9):2112. [Abstract]
- Inflammation. 2025 Jan 22. [Abstract]
- SSRN. 2025 Aug 6.
- bioRxiv. 2024 October 03.
Customer Validation & Images
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Bio/Physico-chemical Assay
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Cell Imaging/Staining
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Bio/Physico-chemical Assay
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Bio/Physico-chemical Assay
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Cell Proliferation/Viability Assay
Ver todos los productos específicos de isoformas Aurora Kinase
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Actividad biológica
Descripciòn
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) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| K562 | GI50 |
0.27 μM
Compound: KW-2449
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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
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[PMID: 35551036] |
| K562 | GI50 |
0.27 μM
Compound: KW-2449
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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
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[PMID: 35551036] |
| MOLM-14 | IC50 |
14.8 nM
Compound: 5, KW-2449
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Inhibition of FLT3-mediated STAT5 phosphorylation in human MOLM14 cells
Inhibition of FLT3-mediated STAT5 phosphorylation in human MOLM14 cells
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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
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
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 1000669-72-6
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Appearance Solid
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Peso molecular 332.40
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Fòrmula C20H20N4O
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Color White to light yellow
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SMILES
O=C(C1=CC=C(/C=C/C2=NNC3=C2C=CC=C3)C=C1)N4CCNCC4
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Envío
Room temperature in continental US; may vary elsewhere.
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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
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Most Recent
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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
KW-2449 purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2026 May 19;7(5):102787. [Abstract]
Dose-response curve for KW-2449 (0.001-100 μM) neuroprotection of paclitaxel-induced axon degeneration, % response compared to DMSO after 96 h of treatment.
KW-2449 purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2026 May 19;7(5):102787. [Abstract]
Representative phase images of iPSC-derived sensory neurons pre-treatment (0 h) and post-treatment (96 h) with DMSO, paclitaxel (PTX), KW-2449 alone, or paclitaxel (PTX) and KW-2449.
KW-2449 purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2026 May 19;7(5):102787. [Abstract]
Scatterplot showing average ratio of neurite length post- vs. pre-treatment of all compounds screened, identified hits, and positive (paclitaxel + KW-2449) and negative control (paclitaxel).
KW-2449 purchased from MedChemExpress. Usage Cited in: Cell Rep Med. 2026 May 19;7(5):102787. [Abstract]
Dose-response curves representing % maximal response compared to KW-2449’s rescue of paclitaxel-induced axon degeneration at 96 h post-treatment.
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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
KW-2449 purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2021 Jun:188:114542. [Abstract]
MEF cells were pre-treated with various concentrations of KW-2449 (0-1 μM) as indicated followed by stimulation with cisplatin (50 µM) for 16 hr and the cell viability was determined by luminescent cell viability assay kit. The EC50 of KW-2449 was calculated as 98 nM.
KW-2449 purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2021 Jun:188:114542. [Abstract]
The chemical structure of KW-2449 and representative images (25 × ) of MEF cells that were pretreated with DMSO or KW-2449 (0.5 μM) followed by stimulation with cisplatin for 16 hr.
KW-2449 purchased from MedChemExpress. Usage Cited in: Biochem Pharmacol. 2021 Jun:188:114542. [Abstract]
Cisplatin-induced cell death were determined by Annexin V/PI staining assays in MEF cells. MEF cells were pre-treated with DMSO or KW-2449(0.5 μM) followed by stimulation with cisplatin for 16 hr.
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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 -
Inflammation
2025 Jan 22. PMID: 39843680 -
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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.
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (282 KB)
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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)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
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.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| 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 |
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