MAX-40279
Based on 1 publication(s) in Google Scholar
MAX-40279 is a dual and orally active inhibitor of FLT3 kinase and FGFR kinase. MAX-40279 is also effective against the FLT3 mutants such as FLT3D835Y, suggesting that it can overcome resistance to Quizartinib (HY-13001) and Sorafenib (HY-10201). MAX-40279 inhibits NDRG1 phosphorylation at Ser330 and suppresses endothelial-to-mesenchymal transition (EndMT). MAX-40279 can be used for the research of acute myelogenous leukemia (AML).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 97.04%
- No. CAS: 2070931-57-4
- Fòrmula: C22H23FN6OS
- Peso molecular:438.52
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Almacenamiento:Powder -20°C, 3 years ; In solvent -80°C, 6 months , -20°C, 1 month
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
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Publications Citing Use of MedChemExpress (MCE) MAX-40279
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Actividad biológica
FLT3 and FGFR[1]
MAX-40279 (0.5-1 μM, 48 h) impedes EndMT by inhibiting NDRG1 phosphorylation at Ser-330 in HUVECs, MAECs, and MPLECs[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:HUVECs
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Concentration:0.5 and 1 μM
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Incubation Time:48 h
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Result:Attenuated migration of HUVEC induced by H2O2 and TGF-β.
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Cell Line:HUVECs, MAECs, and MPLECs
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Concentration:0.5 and 1 μM
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Incubation Time:48 h
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Result:Significantly inhibited the phosphorylation of NDRG1 at Ser-330.
Reduced the total protein level of NDRG1.
Inhibited the expression of mesenchymal markers such as ZEB1, α-SMA, Slug, Snail, and TAGLN.
MAX-40279 (12 mg/kg, p,o., twice daily for 21-28 days) significantly inhibited tumor growth in MV4-11 and KG-1 cells induced mice xenograft models[1].
MAX-40279 (7-15 mg/kg, p.o., twice daily for 2-3 weeks) significantly enhances the anti-PD-1 therapeutic effect in mice breast cancer model[1].
MAX-40279 (p.o., single dose) has much higher drug concentration in bone marrow than in plasma in SD rats[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Micro patient-derived xenotransplantation model established in 5-week-old nu/nu mice[1]
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Dosage:12 mg/kg
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Administration:Oral administration (p.o.), once daily for 7 days
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Result:Reduced the vitality of tumor cells.
The growth rates of tumour volume and weight were smaller but that the combined inhibition was more remarkable.
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Animal Model:MV4-11 and KG-1 cells induced xenograft model established in immunodeficient mice[1]
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Dosage:12 mg/kg
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Administration:Oral administration (p.o.), twice daily for 21-28 days
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Result:Significantly inhibited tumor growth, with no significant weight loss or toxicity observed.
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Animal Model:4T1 induced breast cancer model combination with anti-PD-1 established in mice[1]
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Dosage:7, 10 and 15 mg/kg
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Administration:Oral administration (p.o.), twice daily for 2-3 weeks
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Result:Significantly enhanced the efficacy of anti-PD-1 effect, and the combined treatment with anti-PD-1 antibodies yielded the best results.
Chemical Information
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No. CAS 2070931-57-4
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Appearance Solid
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Peso molecular 438.52
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Fòrmula C22H23FN6OS
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Color Off-white to light yellow
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SMILES
FC1=CC(OC)=C(C2=C(C)SC3=C2N=C(NC4=CN(C5CCNCC5)N=C4)N=C3)C=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years In solvent -80°C 6 months -20°C 1 month
Publications (1)
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Journal Impact Factor
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Most Recent
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Theranostics
2025 Jan 1;15(2):745-765. PMID: 39744686
Solvente y solubilidad
DMSO : ≥ 25 mg/mL (57.01 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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 (5.70 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.
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 (281 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.2804 mL | 11.4020 mL | 22.8040 mL | 57.0099 mL |
| 5 mM | 0.4561 mL | 2.2804 mL | 4.5608 mL | 11.4020 mL | |
| 10 mM | 0.2280 mL | 1.1402 mL | 2.2804 mL | 5.7010 mL | |
| 15 mM | 0.1520 mL | 0.7601 mL | 1.5203 mL | 3.8007 mL | |
| 20 mM | 0.1140 mL | 0.5701 mL | 1.1402 mL | 2.8505 mL | |
| 25 mM | 0.0912 mL | 0.4561 mL | 0.9122 mL | 2.2804 mL | |
| 30 mM | 0.0760 mL | 0.3801 mL | 0.7601 mL | 1.9003 mL | |
| 40 mM | 0.0570 mL | 0.2850 mL | 0.5701 mL | 1.4252 mL | |
| 50 mM | 0.0456 mL | 0.2280 mL | 0.4561 mL | 1.1402 mL |
MAX-40279 Related Classifications
HY-145723 Related Classifications
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