| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
ABN-401 selectively targets c-MET (mesenchymal-epithelial transition factor), a receptor tyrosine kinase involved in cell growth, survival, and metastasis. c-MET is frequently overexpressed or mutated in various cancers. The compound is an ATP-competitive inhibitor, binding to the ATP pocket of c-MET.
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|---|---|
| ln Vitro |
ABN-401 is a potent c-MET inhibitor with an IC50 of 10 nM. It exhibits strong cytotoxicity against MET-addicted cancer cells with IC50 values ranging from 2 to 43 nM. It effectively inhibits c-MET phosphorylation in tumor tissues, blocking downstream signaling pathways that drive tumor growth.
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| ln Vivo |
In animal models, ABN-401 demonstrates significant antitumor activity by inhibiting c-MET phosphorylation in tumor tissues. Its oral activity, with bioavailability of 42.1-56.2% in rats and 27.4-37.7% in dogs, supports its potential for oral administration in cancer therapy.
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| Enzyme Assay |
The inhibitory activity against c-MET is measured using an in vitro kinase assay. Recombinant c-MET enzyme is incubated with a peptide substrate and ATP in the presence of varying concentrations of ABN-401. The IC50 (10 nM) is calculated by measuring the remaining enzymatic activity.
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| Cell Assay |
MET-addicted cancer cell lines (e.g., various carcinoma cells) are cultured and treated with ABN-401 across a concentration range (0.1 nM to 1 uM). Cell viability is assessed after 48-72 hours using MTT or CellTiter-Glo assays. The GI50 values (2-43 nM) are calculated from the dose-response curves.
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| Animal Protocol |
Subcutaneous xenograft tumor models are established in immunodeficient mice using MET-addicted cancer cells. Once tumors reach a certain volume, mice are orally administered ABN-401 daily for a specified period. Tumor volumes are measured regularly. Tumor tissues are harvested to assess c-MET phosphorylation by Western blot.
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| ADME/Pharmacokinetics |
ABN-401 is orally bioavailable, with bioavailability of 42.1-56.2% in rats and 27.4-37.7% in dogs. These data demonstrate its suitability for oral administration. Detailed PK parameters such as half-life, Cmax, and clearance are not extensively reported in standard supplier profiles.
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| Toxicity/Toxicokinetics |
Detailed toxicological data for ABN-401 are not extensively documented in standard profiles. As a research compound, comprehensive acute and sub-chronic toxicity studies have not been publicly reported. However, it is considered well-tolerated in animal efficacy studies.
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| References | |
| Additional Infomation |
ABN-401 is an ATP-competitive c-MET inhibitor that can be used for anti-cancer research. Its ability to target c-MET-addicted cancers makes it a valuable tool for studying c-MET-driven oncogenesis and for developing targeted therapies. It is not an approved clinical drug.
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| Molecular Formula |
C29H34N12O
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|---|---|
| Molecular Weight |
566.660063266754
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| Exact Mass |
566.297
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| CAS # |
2242563-15-9
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| PubChem CID |
118364782
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
0.9
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
11
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| Rotatable Bond Count |
7
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| Heavy Atom Count |
42
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| Complexity |
847
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C12N=NN(CC3OCCN(C4=NC=C(C5=CC=C(CN6CCN(C)CC6)C=C5)C=N4)C3)C1=NC(C1=CN(C)N=C1)=CN=2
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| InChi Key |
PQJGYYZYYMVBDF-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C29H34N12O/c1-37-7-9-39(10-8-37)17-21-3-5-22(6-4-21)23-13-31-29(32-14-23)40-11-12-42-25(19-40)20-41-28-27(35-36-41)30-16-26(34-28)24-15-33-38(2)18-24/h3-6,13-16,18,25H,7-12,17,19-20H2,1-2H3
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| Chemical Name |
4-[5-[4-[(4-methylpiperazin-1-yl)methyl]phenyl]pyrimidin-2-yl]-2-[[5-(1-methylpyrazol-4-yl)triazolo[4,5-b]pyrazin-3-yl]methyl]morpholine
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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 : ~10 mg/mL (~17.65 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (1.76 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 10.0 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of 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: ≥ 1 mg/mL (1.76 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 10.0 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 | 1.7647 mL | 8.8236 mL | 17.6473 mL | |
| 5 mM | 0.3529 mL | 1.7647 mL | 3.5295 mL | |
| 10 mM | 0.1765 mL | 0.8824 mL | 1.7647 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.
Link: https://clinicaltrials.gov/ct2/show/NCT05882292
Conditions:NeoplasmsLink: https://clinicaltrials.gov/ct2/show/NCT05248074
Conditions:Solid TumorProducts are for research use only; We do not sell to patients
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