| Size | Price | Stock | Qty |
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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 hemifumarate salt retains the dual inhibitory activity against FLT3 and FGFR kinases, including resistance mutations like FLT3 D835Y. |
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| ln Vitro |
MAX-40279 hemifumarate 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 hemifumarate salt enhances bioavailability and stability.
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| ln Vivo |
Preclinical studies support favorable pharmacokinetics, antitumor activity, and safety profile for MAX-40279 hemifumarate, making it a promising candidate for CRPC treatment development. Its ability to inhibit FLT3 and FGFR kinases suggests potential for AML research as well, with anti-tumor activity in FLT3-driven models.
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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) or prostate cancer cell lines are seeded in 96-well plates and treated with increasing concentrations of MAX-40279 hemifumarate for 72 hours. Cell viability is measured using the MTT assay or CellTiter-Glo reagent. Apoptosis is measured by Annexin V/PI staining.
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| Animal Protocol |
For in vivo studies, MAX-40279 hemifumarate is administered orally to mice bearing FLT3-driven leukemia xenografts or prostate cancer xenografts. Dosing is typically once or twice daily for 2-4 weeks. Tumor volumes are measured with calipers, and at termination, tumors are excised for pharmacodynamic analysis.
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| ADME/Pharmacokinetics |
MAX-40279 hemifumarate is an orally active dual FLT3/FGFR kinase inhibitor. The hemifumarate salt form enhances bioavailability and stability, supporting favorable pharmacokinetics and antitumor activity in preclinical studies. It is typically formulated for in vivo studies with a suitable vehicle.
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| Toxicity/Toxicokinetics |
Preclinical studies support the safety profile of MAX-40279 hemifumarate at therapeutic doses, with no severe toxicities reported. As a dual FLT3/FGFR inhibitor, potential risks include class-specific toxicities such as myelosuppression. Comprehensive toxicological data have not been fully published.
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| References | |
| Additional Infomation |
Other information: MAX-40279 hemifumarate (CAS 2388506-43-0) is the hemifumarate salt form of MAX-40279. It is derived from patent WO2021180032 and has been studied in castration-resistant prostate cancer (CRPC) preclinical models. It is not an FDA-approved drug and is for research use only. Synonyms: MAX-40279 hemifumarate.
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| Molecular Formula |
C26H27FN6O5S
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|---|---|
| Molecular Weight |
554.59
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| Exact Mass |
992.338
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| CAS # |
2388506-43-0
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| Related CAS # |
MAX-40279;2070931-57-4;MAX-40279 hemiadipate;2388506-44-1;MAX-40279 hydrochloride;2388506-51-0
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| PubChem CID |
134687611
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| Appearance |
Off-white to light yellow solid powder
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| Hydrogen Bond Donor Count |
6
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| Hydrogen Bond Acceptor Count |
20
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| Rotatable Bond Count |
12
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| Heavy Atom Count |
70
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| Complexity |
717
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(/C(=O)O)=C\C(=O)O.CC1SC2=CN=C(NC3C=NN(C4CCNCC4)C=3)N=C2C=1C1C=CC(F)=CC=1OC
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| InChi Key |
BCHMKHOVSSCBHQ-WXXKFALUSA-N
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| InChi Code |
InChI=1S/2C22H23FN6OS.C4H4O4/c2*1-13-20(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;5-3(6)1-2-4(7)8/h2*3-4,9-12,16,24H,5-8H2,1-2H3,(H,25,27,28);1-2H,(H,5,6)(H,7,8)/b;;2-1+
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| Chemical Name |
(E)-but-2-enedioic acid;7-(4-fluoro-2-methoxyphenyl)-6-methyl-N-(1-piperidin-4-ylpyrazol-4-yl)thieno[3,2-d]pyrimidin-2-amine
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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) |
DMF: 1.96 mg/mL (3.53 mM)
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|---|---|
| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.8031 mL | 9.0157 mL | 18.0313 mL | |
| 5 mM | 0.3606 mL | 1.8031 mL | 3.6063 mL | |
| 10 mM | 0.1803 mL | 0.9016 mL | 1.8031 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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