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

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).

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

MAX-40279

MAX-40279 Chemical Structure

CAS No. : 2070931-57-4

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 In-stock
Solution
10 mM * 1 mL in DMSO In-stock
Solid
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25 mg In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Other Forms of MAX-40279:

MAX-40279 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE MAX-40279

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

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)[1][2][3].

IC50 & Target

FLT3 and FGFR[1]
In Vitro

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.

MAX-40279 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 (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 (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.

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.), twice 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.), twice 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

438.52

Formula

C22H23FN6OS
CAS No.
Appearance

Solid

Color

Off-white to light yellow

SMILES

FC1=CC(OC)=C(C2=C(C)SC3=C2N=C(NC4=CN(C5CCNCC5)N=C4)N=C3)C=C1
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

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.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2804 mL 11.4020 mL 22.8040 mL
5 mM 0.4561 mL 2.2804 mL 4.5608 mL
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. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

  • Molarity Calculator

  • Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass
=
Concentration
×
Volume
×
Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

=
Concentration (final)

C2

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Volume (final)

V2

In Vivo:

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.

  • Protocol 1

    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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
% 
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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.
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. 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
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MAX-40279 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-402792070931-57-4MAX40279MAX 40279FLT3FGFRCluster of differentiation antigen 135CD135Fms like tyrosine kinase 3Fibroblast growth factor receptordualacute myelogenous leukemiaInhibitorinhibitorinhibit

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