| Size | Price | Stock | Qty |
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| 50mg |
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| 100mg |
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| Other Sizes |
| Targets |
MY-1442 directly targets the colchicine binding site on β-tubulin, a key protein in microtubules. By binding to this site, it inhibits tubulin polymerization, thereby disrupting the formation of microtubules, which are essential for cell division and intracellular transport. This mechanism of action is characteristic of a class of anti-mitotic agents used in cancer therapy.
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| ln Vitro |
In vitro, MY-1442 exhibits potent anti-proliferative activity against a range of cancer cell lines. It shows IC50 values of 0.034 μM against MGC-803 (gastric cancer), 0.081 μM against HCT-116 (colorectal cancer), and 0.19 μM against KYSE30 (esophageal cancer) cells. Beyond inhibiting proliferation, MY-1442 effectively induces apoptosis and inhibits cell migration in MGC-803 gastric cancer cells. Mechanistically, it regulates the expression of cell cycle- and apoptosis-related proteins.
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| ln Vivo |
In vivo, MY-1442 has demonstrated significant anti-tumor efficacy. In an MGC-803 xenograft tumor model, the compound inhibited tumor growth with a tumor growth inhibition (TGI) rate of 65.5% at a dose of 30 mg/kg/day. This confirms its potential as an effective anti-cancer agent in preclinical models.
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| Enzyme Assay |
In vitro binding assays for MY-1442 involve assessing its interaction with tubulin. This is typically performed using a tubulin polymerization assay, where the compound's ability to inhibit the polymerization of purified tubulin is measured spectrophotometrically. Competition assays with [³H]colchicine can be used to confirm that MY-1442 binds to the colchicine binding site on β-tubulin. Molecular docking studies further validate the binding interactions.
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| Cell Assay |
In vitro cell-based assays for MY-1442 involve treating cancer cell lines (e.g., MGC-803, HCT-116, KYSE30) with varying concentrations of the compound. Cell viability is assessed using MTT or CCK-8 assays to determine IC50 values. The effects on apoptosis are evaluated using flow cytometry (Annexin V/PI staining) and by examining markers like cleaved PARP and caspase-3. Cell migration is assessed using wound-healing or transwell assays. The expression of cell cycle- and apoptosis-related proteins is analyzed by Western blotting.
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| Animal Protocol |
In vivo efficacy studies are performed using a mouse xenograft model with MGC-803 gastric cancer cells. MY-1442 is typically administered at a dose of 30 mg/kg/day. Tumor growth is monitored over time, and the tumor growth inhibition (TGI) rate is calculated. At the end of the study, tumors are harvested for further histological and molecular analysis to confirm target engagement and mechanism of action.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of MY-1442 are not extensively detailed in publicly available literature. The compound has a molecular weight of 307.34. For in vivo studies, it is typically administered at 30 mg/kg/day. Further detailed PK studies (e.g., half-life, bioavailability, tissue distribution) are needed to fully characterize its ADME properties.
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| Toxicity/Toxicokinetics |
Toxicological data for MY-1442 are limited as it is a research compound. In the MGC-803 xenograft model, the compound was well-tolerated at the efficacious dose of 30 mg/kg/day. Standard safety precautions should be taken when handling this compound, as with all research chemicals. No specific toxicity data (e.g., LD50, NOAEL) are available in the referenced sources.
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| References | |
| Additional Infomation |
Additional information: MY-1442 (CAS 3050871-87-6) has a molecular formula of C19H17NO3 and a molecular weight of 307.34. Its primary research application is in cancer biology, specifically as a tubulin polymerization inhibitor targeting the colchicine binding site. The compound is available from chemical suppliers and is not approved for clinical use. The primary reference for its discovery and characterization is Tian XY, et al. Eur J Med Chem. 2024.
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| Molecular Formula |
C19H17NO3
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| Molecular Weight |
307.34
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| Appearance |
Light yellow to yellow solid powder
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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 |
| 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 :~100 mg/mL (~325.37 mM; with sonication (<80°C))
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| Solubility (In Vivo) |
Solubility in Formulation 1: 5 mg/mL (16.27 mM) in 10% DMSO + 40% PEG300 + 5% Tween-80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one),clear solution; with ultrasonication.
For example, if 1 mL of working solution is to be prepared,you can add 100 μL of 50.0 mg/mL clear DMSO stock solution and add it to 400 μL PEG300 and mix well. Then add 50 μL Tween-80 to the above system and mix well. Then continue to add 450 μL of physiological saline to make up 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: 5 mg/mL (16.27 mM) 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; with ultrasonication. For example, if 1 mL of working solution is to be prepared,you can add 100 μL of 50.0 mg/mL clear DMSO stock solution and add it to 900 μL of 20% SBE-β-CD saline solution and mix well. 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. View More
Solubility in Formulation 3: 5 mg/mL (16.27 mM) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one),clear solution; with ultrasonication. |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.2537 mL | 16.2686 mL | 32.5373 mL | |
| 5 mM | 0.6507 mL | 3.2537 mL | 6.5075 mL | |
| 10 mM | 0.3254 mL | 1.6269 mL | 3.2537 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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