MAX-40279 hemifumarate
Based on 1 publication(s) in Google Scholar
MAX-40279 hemifumarate is a dual and orally active inhibitor of FLT3 kinase and FGFR kinase. MAX-40279 hemifumarate 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 hemifumarate inhibits NDRG1 phosphorylation at Ser330 and suppresses endothelial-to-mesenchymal transition (EndMT). MAX-40279 hemifumarate can be used for the research of acute myelogenous leukemia (AML).
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza : 99.52%
- No. CAS: 2388506-43-0
- Fòrmula: C22H23FN6OS·1/2C4H4O4
- Peso molecular:496.57
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Almacenamiento:
-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
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
- Protocolo
- Pureza y Documentación
- Referencias
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Help & FAQs
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Publications Citing Use of MedChemExpress (MCE) MAX-40279 hemifumarate
More
Actividad biológica
Descripciòn
IC50 & Target
FLT3 and FGFR[1]
In Vitro
MAX-40279 (0.5-1 μM, 48 h) hemifumarate 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.
In Vivo
MAX-40279 hemifumarate (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 hemifumarate (7-15 mg/kg, p.o., twice daily for 2-3 weeks) significantly enhances the anti-PD-1 effect in mice breast cancer model[1].
MAX-40279 hemifumarate (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.), 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.
Ensayo clínico
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | 2011-05 | PHASE1 |
Chemical Information
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No. CAS 2388506-43-0
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Appearance Solid
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Peso molecular 496.57
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Fòrmula C22H23FN6OS·1/2C4H4O4
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Color Off-white to light yellow
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SMILES
OC(/C=C/C(O)=O)=O.CC1=C(C2=C(C=C(C=C2)F)OC)C3=NC(NC4=CN(C5CCNCC5)N=C4)=NC=C3S1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
-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
Solvente y solubilidad
In Vitro:
DMF : 1.96 mg/mL (3.95 mM; ultrasonic and warming and adjust pH to 5 with HCl 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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Pureza y Documentación
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Ficha de datos (287 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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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 (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 |
|---|---|---|---|---|---|
| DMF | 1 mM | 2.0138 mL | 10.0691 mL | 20.1381 mL | 50.3454 mL |
MAX-40279 hemifumarate Related Classifications
HY-145723B Related Classifications
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