| Size | Price | Stock | Qty |
|---|---|---|---|
| 10mg |
|
||
| 50mg |
|
||
| 100mg |
|
||
| 500mg | |||
| Other Sizes |
| Targets |
MY-1076 targets YAP for degradation, effectively reducing the protein's oncogenic activity. It also targets microtubules by inhibiting their polymerization, a classic mechanism of action for many anti-mitotic chemotherapeutic agents. By disrupting the microtubule network, MY-1076 interferes with spindle formation during mitosis, leading to cell cycle arrest. The combined effect of YAP degradation and tubulin polymerization inhibition results in a potent antiproliferative effect against cancer cells. This multi-targeted approach may offer advantages over single-target agents by attacking cancer cells through complementary pathways.
|
|---|---|
| ln Vitro |
In vitro, MY-1076 exhibits potent antiproliferative activity against a panel of cancer cell lines. It inhibits the proliferation of gastric cancer cell lines MGC-803 and SGC-7901, colorectal cancer cell line HCT-116, and esophageal cancer cell line KYSE450, with IC50 values of 0.019, 0.017, 0.020, and 0.044 μM, respectively. These low nanomolar IC50 values indicate that MY-1076 is a highly potent compound. Mechanistically, it dose-dependently induces G2/M phase block, promotes YAP degradation, and triggers apoptosis. The compound's ability to inhibit microtubule protein polymerization has been confirmed in biochemical assays. MY-1076 also alters the expression of cell cycle and apoptosis-related proteins, consistent with its mechanism of action.
|
| ln Vivo |
Specific in vivo activity data for MY-1076 are not detailed in the available literature. However, its potent in vitro activity against multiple cancer cell lines, particularly gastric cancer cells, strongly suggests that it would have significant efficacy in vivo. As a dual inhibitor of YAP and tubulin polymerization, MY-1076 is a promising candidate for evaluation in animal models of gastric cancer, such as xenograft or patient-derived xenograft (PDX) models. Such studies would be essential to confirm its antitumor activity, assess its pharmacokinetic properties, and evaluate its safety profile for further development.
|
| Enzyme Assay |
Non-cellular assays for MY-1076 focus on its ability to inhibit tubulin polymerization. In these assays, purified tubulin protein is incubated with the compound, and the polymerization process is monitored spectrophotometrically, typically by measuring the increase in turbidity at 340 nm. The compound's ability to inhibit this process is quantified, providing direct evidence of its interaction with the tubulin target. Additionally, binding studies, such as competitive binding assays with colchicine or other tubulin-binding agents, can be performed to further characterize the compound's interaction site on tubulin.
|
| Cell Assay |
In vitro cellular assays are used to evaluate the antiproliferative and mechanistic effects of MY-1076. Cancer cell lines, including MGC-803, SGC-7901, HCT-116, and KYSE450, are treated with varying concentrations of the compound for a defined period (typically 72 hours). Cell viability is then assessed using standard assays such as MTT, CCK-8, or CellTiter-Glo to determine IC50 values. To study the mechanism, cells are analyzed by flow cytometry to measure cell cycle distribution (G2/M arrest) and apoptosis. Western blotting is used to confirm YAP degradation and to assess changes in the expression of cell cycle and apoptosis-related proteins.
|
| Animal Protocol |
In vivo animal experiments for MY-1076 would typically involve the use of mouse xenograft models. Immunodeficient mice would be implanted with human gastric cancer cells, and after tumor establishment, MY-1076 would be administered, likely via intraperitoneal (IP) or oral (PO) routes. The primary endpoint would be tumor growth inhibition, measured by caliper measurements over time. Secondary endpoints would include analysis of tumor tissues for YAP degradation, assessment of apoptosis (e.g., by TUNEL assay or cleaved caspase-3 staining), and evaluation of proliferation markers like Ki-67. Pharmacokinetic parameters would also be determined from plasma samples.
|
| ADME/Pharmacokinetics |
Pharmacokinetic (PK) properties for MY-1076 are not detailed in the available sources. As a small molecule with a molecular weight of 539.57, its PK would be influenced by factors such as solubility, metabolic stability, and permeability. It is soluble in DMSO (80 mg/mL) and has been formulated for in vivo use in a mixture of 10% DMSO, 40% PEG300, 5% Tween 80, and 45% saline (3.3 mg/mL). These properties suggest that it can be administered systemically, and its PK profile would be characterized by parameters like half-life, clearance, volume of distribution, and oral bioavailability in preclinical studies.
|
| Toxicity/Toxicokinetics |
Toxicological data for MY-1076 are not provided in the available sources. As a research compound, its safety profile has not been extensively characterized. However, its potent activity against tubulin, a target also exploited by many approved chemotherapeutics, suggests that it may have dose-limiting toxicities, particularly affecting rapidly dividing cells in the bone marrow and gastrointestinal tract. Comprehensive toxicological studies, including acute and repeated-dose toxicity in rodents and non-rodents, would be required to define its safety margin and therapeutic index.
|
| References | |
| Additional Infomation |
MY-1076 (Catalog No. T77729) has a molecular formula of C29H33NO9 and a molecular weight of 539.57. Its CAS number is 3008262-76-5. The IUPAC name is (E)-N-[(3-hydroxy-4-methoxyphenyl)methyl]-N,3-bis(3,4,5-trimethoxyphenyl)prop-2-enamide. It is a white solid with a purity of 99.6% and is supplied for research purposes only. As a potent YAP inhibitor and tubulin polymerization inhibitor, MY-1076 represents a novel class of anti-cancer agents with a unique dual mechanism of action. It is not approved for clinical use.
|
| Molecular Formula |
C29H33NO9
|
|---|---|
| Molecular Weight |
539.57
|
| CAS # |
3008262-76-5
|
| Appearance |
White to off-white solid powder
|
| HS Tariff Code |
2934.99.9001
|
| 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)
|
| Solubility (In Vitro) |
May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
|
|---|---|
| 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 | 1.8533 mL | 9.2666 mL | 18.5333 mL | |
| 5 mM | 0.3707 mL | 1.8533 mL | 3.7067 mL | |
| 10 mM | 0.1853 mL | 0.9267 mL | 1.8533 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.
Products are for research use only; We do not sell to patients
Copyright 2020 InvivoChem LLC | All Rights Reserved
