MAX-40279 hydrochloride
Based on 1 publication(s) in Google Scholar
MAX-40279 hydrochloride is a dual and orally active inhibitor of FLT3 kinase and FGFR kinase. MAX-40279 hydrochloride 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 hydrochloride inhibits NDRG1 phosphorylation at Ser330 and suppresses endothelial-to-mesenchymal transition (EndMT). MAX-40279 hydrochloride can be used for the research of acute myelogenous leukemia (AML).
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- CAS No.: 2388506-51-0
- 화학식: C22H24ClFN6OS
- 분자량:474.98
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
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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Biological Activity
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Chemical Information
- 순도&문서
- References
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Publications Citing Use of MedChemExpress (MCE) MAX-40279 hydrochloride
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Biological Activity
제품 설명
IC50 & Target
FLT3 and FGFR[1]
In Vitro
MAX-40279 (0.5-1 μM, 48 h) hydrochloride 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 (12 mg/kg, p,o., twice daily for 21-28 days) hydrochloride 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) hydrochloride significantly enhances the anti-PD-1 effect in mice breast cancer model[1].
MAX-40279 (p.o., single dose) hydrochloride 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 No. 2388506-51-0
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분자량 474.98
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화학식 C22H24ClFN6OS
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SMILES
FC1=CC(OC)=C(C2=C(C)SC3=C2N=C(NC4=CN(C5CCNCC5)N=C4)N=C3)C=C1.[H]Cl
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
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
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
MAX-40279 hydrochloride Related Classifications
HY-145723A Related Classifications
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