MAX-40279 hemiadipate
Based on 1 publication(s) in Google Scholar
MAX-40279 hemiadipate is a dual and orally active inhibitor of FLT3 kinase and FGFR kinase. MAX-40279 hemiadipate 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 hemiadipate inhibits NDRG1 phosphorylation at Ser330 and suppresses endothelial-to-mesenchymal transition (EndMT). MAX-40279 hemiadipate can be used for the research of acute myelogenous leukemia (AML).
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit: 99.26%
- CAS. Nr.: 2388506-44-1
- Formel: C22H23FN6OS·1/2C6H10O4
- Molecular Weight:511.60
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Speicherung:
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
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Biologische Aktivität
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Chemical Information
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Lösungsmittel & Löslichkeit
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) MAX-40279 hemiadipate
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Biologische Aktivität
FLT3 and FGFR[1]
MAX-40279 (0.5-1 μM, 48 h) hemiadipate 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) hemiadipate 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) hemiadipate significantly enhances the anti-PD-1 effect in mice breast cancer model[1].
MAX-40279 (p.o., single dose) hemiadipate 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.), once 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.), once 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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CAS. Nr. 2388506-44-1
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Appearance Solid
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Molecular Weight 511.60
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Formel C22H23FN6OS·1/2C6H10O4
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Color Off-white to light yellow
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SMILES
O=C(O)CCCCC(O)=O.FC1=CC(OC)=C(C2=C(C)SC3=C2N=C(NC4=CN(C5CCNCC5)N=C4)N=C3)C=C1
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
-20°C, sealed storage, away from moisture
* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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
Lösungsmittel & Löslichkeit
DMSO : 25 mg/mL (48.87 mM; ultrasonic and warming and heat to 60°C; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
DMF : 10 mg/mL (19.55 mM; ultrasonic and warming and heat to 60°C)
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 (sealed storage, away from moisture). 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 (sealed storage, away from moisture). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
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: ≥ 2.08 mg/mL (4.07 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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: ≥ 2.08 mg/mL (4.07 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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.
Reinheit & Dokumentation
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Data Sheet (286 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
Verweise
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 (sealed storage, away from moisture). 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 |
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| DMF / DMSO | 1 mM | 1.9547 mL | 9.7733 mL | 19.5465 mL | 48.8663 mL |
| 5 mM | 0.3909 mL | 1.9547 mL | 3.9093 mL | 9.7733 mL | |
| 10 mM | 0.1955 mL | 0.9773 mL | 1.9547 mL | 4.8866 mL | |
| 15 mM | 0.1303 mL | 0.6516 mL | 1.3031 mL | 3.2578 mL | |
| DMSO | 20 mM | 0.0977 mL | 0.4887 mL | 0.9773 mL | 2.4433 mL |
| 25 mM | 0.0782 mL | 0.3909 mL | 0.7819 mL | 1.9547 mL | |
| 30 mM | 0.0652 mL | 0.3258 mL | 0.6516 mL | 1.6289 mL | |
| 40 mM | 0.0489 mL | 0.2443 mL | 0.4887 mL | 1.2217 mL |
MAX-40279 hemiadipate Related Classifications
HY-145723C Related Classifications
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