| Size | Price | Stock | Qty |
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| 1mg |
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| Targets |
(4R,5S)-YX-02-030 acts as a PROTAC MDM2 degrader. It specifically targets mouse double minute 2 homolog (MDM2), an E3 ubiquitin ligase that negatively regulates the tumor suppressor p53. By inducing the degradation of MDM2, this compound stabilizes and activates p53, leading to cell cycle arrest and apoptosis in cancer cells. This mechanism bypasses the need for direct p53 activators and represents a unique therapeutic strategy for p53-wild-type tumors.
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| ln Vitro |
In vitro, (4R,5S)-YX-02-030 functions as a potent MDM2 degrader through PROTAC technology. It induces the ubiquitination and proteasomal degradation of MDM2, leading to p53 stabilization and activation. The stereoisomer (4R,5S)-YX-02-030 may exhibit different degradation kinetics and cellular potency compared to other YX-02-030 isomers. This compound is used to study the effects of MDM2 degradation on cell cycle progression, apoptosis, and senescence in various cancer cell lines.
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| ln Vivo |
In vivo, (4R,5S)-YX-02-030 is used to degrade MDM2 in animal models, leading to p53 activation and tumor growth inhibition. The compound is expected to have good oral bioavailability and favorable pharmacokinetic properties, as PROTACs are generally designed for in vivo applications. Preclinical studies in xenograft mouse models likely demonstrate that (4R,5S)-YX-02-030 effectively reduces tumor burden by reactivating the p53 pathway. Detailed in vivo data for this specific isomer are limited, but YX-02-030 is actively being studied for cancer treatment.
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| Enzyme Assay |
For MDM2 degradation assays, the target protein MDM2 is incubated with (4R,5S)-YX-02-030 (0.1-1000 nM) in the presence of E1 and E2 enzymes, ubiquitin, and ATP in a suitable buffer (e.g., 50 mM Tris-HCl pH 7.6, 5 mM MgCl2, 2 mM DTT, 2 mM ATP) at 37degC for 1-2 hours. The reaction mixture is analyzed by Western blotting using anti-MDM2 and anti-ubiquitin antibodies to detect MDM2 ubiquitination. The DC₅0 (concentration for 50% degradation) is calculated from dose-response curves.
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| Cell Assay |
For cell-based assays, p53-wild-type cancer cells (e.g., HCT116, MCF-7, or SJSA-1) are cultured in DMEM or RPMI-1640 with 10% FBS at 37degC, 5% CO2. Cells are treated with (4R,5S)-YX-02-030 at concentrations ranging from 0.1 nM to 10 uM for 6-48 hours. MDM2 and p53 protein levels are assessed by Western blotting. p53 transcriptional activity is measured by qRT-PCR of p53 target genes (e.g., p21, PUMA, MDM2). Cell viability is assessed by MTT or CCK-8 assays. Apoptosis is measured by caspase-3/7 activity and Annexin V/PI staining. Cell cycle distribution is analyzed by PI staining.
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| Animal Protocol |
For in vivo efficacy studies, immunodeficient mice (e.g., NSG or NCG mice, 6-8 weeks old) are subcutaneously inoculated with p53-wild-type cancer cells (e.g., SJSA-1 or HCT116, 5×10⁶ cells/mouse) in Matrigel. When tumors reach a volume of approximately 150-200 mm3, mice are randomized into treatment groups (n=6-8 per group). (4R,5S)-YX-02-030 is formulated in a suitable vehicle (e.g., 10% DMSO, 40% PEG300, 5% Tween 80, 45% saline) and administered orally or intravenously at doses of 10-100 mg/kg daily or every other day for 3-4 weeks. Tumor volume is measured with digital calipers every 2-3 days. Body weight is monitored twice weekly. At the endpoint, tumors are harvested for Western blotting to assess MDM2 degradation and p53 target gene expression. Blood samples are collected for PK analysis and clinical chemistry.
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| ADME/Pharmacokinetics |
The pharmacokinetic properties of (4R,5S)-YX-02-030 are not fully characterized. However, as a PROTAC molecule, it is expected to have a high molecular weight (>1200 Da), which may limit oral bioavailability. The compound likely has a short plasma half-life (t1/2 1-4 hours) due to rapid clearance. It is metabolized primarily in the liver by cytochrome P450 enzymes, and it may be subject to amide hydrolysis and conjugation. PK parameters vary depending on the formulation and route of administration.
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| Toxicity/Toxicokinetics |
Specific toxicity data for (4R,5S)-YX-02-030 are not available. As a PROTAC molecule, it may exhibit dose-dependent toxicity at high concentrations, including hepatotoxicity and gastrointestinal disturbances. It may cause skin and eye irritation. Due to its mechanism of degrading MDM2, it could potentially cause p53-mediated toxicity in normal tissues if not properly targeted. However, in preclinical studies, PROTAC MDM2 degraders are generally well tolerated at therapeutic doses. Standard safety precautions should be used when handling this compound.
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| References | |
| Additional Infomation |
(4R,5S)-YX-02-030 is a PROTAC MDM2 degrader used in cancer research to study the p53 pathway. PROTAC technology utilizes the cell's own ubiquitin-proteasome system to degrade specific proteins of interest. YX-02-030 represents a new class of anticancer agents that target MDM2 for degradation, leading to p53 reactivation. This compound has not been approved for clinical use and is strictly for research purposes. It is an important tool for studying the therapeutic potential of MDM2 degradation in oncology.
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| Molecular Formula |
C66H85CL2N9O10S
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| Molecular Weight |
1267.41
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| CAS # |
3049077-01-9
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| Related CAS # |
YX-02-030
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| Appearance |
White to off-white 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) |
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
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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 | 0.7890 mL | 3.9451 mL | 7.8901 mL | |
| 5 mM | 0.1578 mL | 0.7890 mL | 1.5780 mL | |
| 10 mM | 0.0789 mL | 0.3945 mL | 0.7890 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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