| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
FLT3 and FGFR[1]
FLT3 kinase and FGFR kinase. As the same active moiety as MAX-40279, the hemiadipate salt retains the dual inhibitory activity against FLT3 and FGFR kinases, including resistance mutations like FLT3 D835Y. |
|---|---|
| ln Vitro |
MAX-40279 hemiadipate is a dual and potent inhibitor of FLT3 kinase and FGFR kinase. It is effective against FLT3 mutants such as FLT3 D835Y, suggesting it can overcome resistance to quizartinib and sorafenib. The hemiadipate salt form offers improved solubility for in vitro and in vivo studies.
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| ln Vivo |
MAX-40279 hemiadipate is an orally active compound with potential for AML research. Preclinical studies support its ability to inhibit FLT3 and FGFR signaling, leading to anti-tumor activity in FLT3-driven leukemia models. The hemiadipate salt enhances solubility, which may improve in vivo efficacy.
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| Enzyme Assay |
Cell-free FLT3 and FGFR kinase assays are performed using recombinant enzymes. The compound is incubated with the enzyme, a peptide substrate, and ATP for 30-60 minutes. Kinase activity is measured using a luminescence-based ADP detection kit. IC50 values are determined from dose-response curves.
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| Cell Assay |
FLT3-ITD-positive human leukemia cell lines (e.g., MV4-11) are seeded in 96-well plates and treated with increasing concentrations of MAX-40279 hemiadipate for 72 hours. Cell viability is measured using the MTT assay or CellTiter-Glo reagent. Apoptosis is measured by Annexin V/PI staining. FLT3 phosphorylation is assessed by Western blot.
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| Animal Protocol |
For in vivo studies, MAX-40279 hemiadipate is administered orally to mice bearing FLT3-ITD-driven tumor xenografts. Dosing is typically once or twice daily for 2-4 weeks. Tumor volumes are measured with calipers, and at study termination, tumors are excised for pharmacodynamic analysis, including FLT3 phosphorylation and downstream signaling.
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| ADME/Pharmacokinetics |
MAX-40279 hemiadipate is an orally active dual FLT3/FGFR kinase inhibitor. As a hemiadipate salt, it offers improved solubility and stability for research applications. It is typically formulated for in vivo studies with a vehicle such as 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% saline.
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| Toxicity/Toxicokinetics |
No specific toxicity data are available. As a dual FLT3/FGFR inhibitor, potential toxicities may include myelosuppression and FGFR class-related effects. Comprehensive toxicological assessments have not been published. The compound is a research-grade chemical and not intended for human use.
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| References | |
| Additional Infomation |
Other information: MAX-40279 hemiadipate (CAS 2388506-44-1) is the hemiadipate salt form of MAX-40279. It is derived from patent WO2021180032. The salt form offers improved physicochemical properties for research. It is not an FDA-approved drug and is for research use only.
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| Molecular Formula |
C28H33FN6O5S
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|---|---|
| Molecular Weight |
584.66
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| Exact Mass |
584.221
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| CAS # |
2388506-44-1
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| Related CAS # |
MAX-40279;2070931-57-4;MAX-40279 hemifumarate;2388506-43-0;MAX-40279 hydrochloride;2388506-51-0
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| PubChem CID |
157608770
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| Appearance |
Off-white to light yellow solid powder
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| Hydrogen Bond Donor Count |
4
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| Hydrogen Bond Acceptor Count |
12
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
41
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| Complexity |
712
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(CC(=O)O)CCC(=O)O.CC1SC2=CN=C(NC3C=NN(C4CCNCC4)C=3)N=C2C=1C1C=CC(F)=CC=1OC
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| InChi Key |
CKQKESWOXOJTTB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C22H23FN6OS.C6H10O4/c1-13-20(17-4-3-14(23)9-18(17)30-2)21-19(31-13)11-25-22(28-21)27-15-10-26-29(12-15)16-5-7-24-8-6-16;7-5(8)3-1-2-4-6(9)10/h3-4,9-12,16,24H,5-8H2,1-2H3,(H,25,27,28);1-4H2,(H,7,8)(H,9,10)
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| Chemical Name |
7-(4-fluoro-2-methoxyphenyl)-6-methyl-N-(1-piperidin-4-ylpyrazol-4-yl)thieno[3,2-d]pyrimidin-2-amine;hexanedioic acid
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO: 25 mg/mL (42.76 mM)
DMF: 10 mg/mL (17.10 mM) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.08 mg/mL (3.56 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (3.56 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7104 mL | 8.5520 mL | 17.1040 mL | |
| 5 mM | 0.3421 mL | 1.7104 mL | 3.4208 mL | |
| 10 mM | 0.1710 mL | 0.8552 mL | 1.7104 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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