| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| Other Sizes |
| Targets |
SMARCA2[1][2]
YD23 targets SMARCA2 for degradation. It is a PROTAC that induces the degradation of SMARCA2, which is synthetically lethal with SMARCA4 mutations. It selectively degrades SMARCA2 and inhibits the growth of SMARCA4-mutant lung cancer cell lines. This selective degradation is achieved through the ubiquitin-proteasome system. |
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| ln Vitro |
In vitro, YD23 potently degrades SMARCA2 with a median DC50 of 92.8 nM and achieves a Dmax of 90% on an additional panel of ten SMARCA4-WT cell lines. It selectively inhibits growth of SMARCA4-mutant lung cancer cell lines with an IC50 of 0.11 µM (SMARCA4-WT cells, IC50=6 µM). It reduces chromatin accessibility in SMARCA4-deficient cells, affecting gene enhancers related to cell cycle and growth regulation, leading to the downregulation of several cell cycle genes.
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| ln Vivo |
Specific in vivo activity data for YD23 are not detailed in the search results.
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| Enzyme Assay |
Non-cellular assays for YD23 are not typically performed, as it is a PROTAC that functions in a cellular context by hijacking the ubiquitin-proteasome system. Its activity is assessed by measuring the degradation of the SMARCA2 protein in cells.
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| Cell Assay |
In vitro cellular assays for YD23 are performed using SMARCA4-mutant lung cancer cell lines. Cells are treated with the compound, and the degradation of SMARCA2 is measured by Western blotting to determine the DC50. Cell proliferation assays are used to assess the compound's anticancer activity.
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| Animal Protocol |
In vivo animal experiments for YD23 would typically be conducted in mouse xenograft models using SMARCA4-mutant lung cancer cell lines. The compound would be administered via intraperitoneal or oral routes, and tumor growth inhibition and SMARCA2 degradation in tumor tissues would be assessed.
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| ADME/Pharmacokinetics |
YD23 has a molecular formula of C38H39FN8O7 and a molecular weight of 738.76. Its CAS number is 2951015-29-3. It has a purity of >98%. It should be stored as a powder at -20°C for 3 years or in solution at -20°C for 6 months.
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| Toxicity/Toxicokinetics |
Toxicological data for YD23 are not detailed in the search results. As a PROTAC, its toxicity profile would depend on its specificity and the importance of its target, SMARCA2, in normal cells.
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| References |
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| Additional Infomation |
YD23 is a PROTAC that induces the degradation of SMARCA2. It has anticancer activity and selectively inhibits the growth of SMARCA4-mutant lung cancer cells. It is a research compound used to study the synthetic lethality of SMARCA2 and SMARCA4.
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| Molecular Formula |
C38H39FN8O7
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|---|---|
| Molecular Weight |
738.76
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| CAS # |
2951015-29-3
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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 (~135.36 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 | 1.3536 mL | 6.7681 mL | 13.5362 mL | |
| 5 mM | 0.2707 mL | 1.3536 mL | 2.7072 mL | |
| 10 mM | 0.1354 mL | 0.6768 mL | 1.3536 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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