2. Protein Tyrosine Kinase/RTK
  3. FLT3 FGFR
  4. MAX-40279 hemifumarate

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).

For research use only. We do not sell to patients.

MAX-40279 hemifumarate

MAX-40279 hemifumarate Chemical Structure

CAS No. : 2388506-43-0

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Based on 1 publication(s) in Google Scholar

Other Forms of MAX-40279 hemifumarate:

MAX-40279 hemifumarate Related Antibodies

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1 Publications Citing Use of MCE MAX-40279 hemifumarate

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  • Purity & Documentation

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  • Customer Review

Description

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)[1][2][3].

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.

MAX-40279 hemifumarate Related Antibodies

Cell Migration Assay [3]

Cell Line: HUVECs
Concentration: 0.5 and 1 μM
Incubation Time: 48 h
Result: Attenuated migration of HUVEC induced by H2O2 and TGF-β.

Western Blot Analysis[3]

Cell Line: HUVECs, MAECs, and MPLECs
Concentration: 0.5 and 1 μM
Incubation Time: 48 h
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., once daily for 7 days) is effective in 43% of patient tumor samples in mouse Mini-PDX assay[1].
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.

Animal Model: Micro patient-derived xenotransplantation model established in 5-week-old nu/nu mice[1]
Dosage: 12 mg/kg
Administration: Oral administration (p.o.), once daily for 7 days
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.
Animal Model: MV4-11 and KG-1 cells induced xenograft model established in immunodeficient mice[1]
Dosage: 12 mg/kg
Administration: Oral administration (p.o.), once daily for 21-28 days
Result: Significantly inhibited tumor growth, with no significant weight loss or toxicity observed.
Animal Model: 4T1 induced breast cancer model combination with anti-PD-1 established in mice[1]
Dosage: 7, 10 and 15 mg/kg
Administration: Oral administration (p.o.), once daily for 2-3 weeks
Result: Significantly enhanced the efficacy of anti-PD-1 effect, and the combined treatment with anti-PD-1 antibodies yielded the best results.
Clinical Trial
Molecular Weight

554.59

Formula

C22H23FN6OS.1/2C4H4O4
CAS No.
Appearance

Solid

Color

Off-white to light yellow

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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

-20°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

Solvent & Solubility
In Vitro: 

DMF : 1.96 mg/mL (3.53 mM; ultrasonic and warming and adjust pH to 5 with HCl and heat to 60°C)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8031 mL 9.0157 mL 18.0313 mL
5 mM --- --- ---
View the 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.

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In Vivo Dissolution Calculator
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Purity & Documentation
References

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 1.8031 mL 9.0157 mL 18.0313 mL 45.0783 mL
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MAX-40279 hemifumarate Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

MAX-40279 hemifumarate2388506-43-0FLT3FGFRCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Fibroblast growth factor receptordualacute myelogenous leukemiaInhibitorinhibitorinhibit

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