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| Targets |
DAS-5-oCRBN targets c-Src kinase for degradation via the PROTAC mechanism. It binds to c-Src and simultaneously recruits CRBN (cereblon), an E3 ubiquitin ligase component, leading to ubiquitination and proteasomal degradation of c-Src. c-Src is a non-receptor tyrosine kinase involved in cell growth, proliferation, and survival, and is implicated in various cancers. The compound has antiproliferative activity in c-Src-dependent cell lines.
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| ln Vitro |
In vitro studies demonstrate that DAS-5-oCRBN is a selective and potent PROTAC degrader of c-Src kinase. It exhibits antiproliferative activity in both c-Src-dependent cell lines. By binding to CRBN, it modulates protein degradation pathways. Detailed in vitro activity data, including DC50 values and degradation kinetics, are not extensively documented in the available literature. It may enhance the efficacy of immunomodulatory drugs.
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| ln Vivo |
In vivo activity of DAS-5-oCRBN is inferred from its potential as a PROTAC degrader of c-Src kinase. By degrading c-Src, it may inhibit tumor growth and progression in c-Src-dependent cancers. It may offer a novel approach to treating hematological malignancies or other diseases. Detailed in vivo efficacy data from animal models are not extensively documented in the available literature.
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| Enzyme Assay |
The in vitro enzyme/receptor binding assay for DAS-5-oCRBN involves measuring its ability to induce degradation of c-Src kinase. The assay typically uses cell-based systems where the compound is incubated with cells expressing c-Src, and c-Src protein levels are measured by Western blot. The PROTAC-mediated degradation is quantified by determining the DC50 (concentration for 50% degradation). Binding to CRBN and c-Src may be assessed using biophysical methods such as surface plasmon resonance or isothermal titration calorimetry.
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| Cell Assay |
In vitro cell-based assays for DAS-5-oCRBN are conducted using c-Src-dependent cell lines. Cells are treated with the compound at various concentrations, and c-Src protein levels are measured by Western blot to assess degradation. Antiproliferative activity is evaluated using cell viability assays such as MTT or CCK-8. The effect on downstream signaling pathways is assessed by measuring phosphorylation of c-Src substrates. Standard protocols include appropriate controls such as PROTAC inactive analogs.
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| Animal Protocol |
In vivo animal studies for DAS-5-oCRBN would typically be conducted using xenograft mouse models implanted with c-Src-dependent cancer cells. Tumor-bearing mice would be administered the compound via appropriate routes, and tumor growth inhibition would be monitored. c-Src degradation in tumor tissues would be confirmed by Western blot. Pharmacokinetic parameters would be determined from plasma samples. However, detailed protocols and efficacy data are not available from the search results.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of DAS-5-oCRBN include a molecular weight of approximately 826.3 g/mol. As a PROTAC molecule, it has a larger molecular weight compared to traditional small-molecule inhibitors, which may affect oral bioavailability and tissue distribution. Detailed pharmacokinetic parameters such as half-life, Cmax, and bioavailability are not extensively documented in the available literature. The compound is intended for research use only.
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| Toxicity/Toxicokinetics |
Toxicity information for DAS-5-oCRBN is limited. Standard safety precautions for handling research chemicals should be followed. The compound is designated for research use only and is not for human or veterinary use. As a PROTAC degrader, it may have off-target effects and potential toxicity that should be evaluated in appropriate studies. No detailed toxicity data are available from the search results.
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| References | |
| Additional Infomation |
DAS-5-oCRBN is a selective and potent PROTAC degrader of c-Src kinase. It has antiproliferative activity in c-Src-dependent cell lines. By binding to CRBN, it modulates protein degradation pathways. It may enhance the efficacy of immunomodulatory drugs and offer a novel approach to treating hematological malignancies. It is intended for research use only and is not for human or veterinary use.
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| Molecular Formula |
C39H40CLN11O6S
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| Molecular Weight |
826.32
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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 (~121.02 mM; with sonication)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (3.03 mM) (saturation unknown) 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.
For example, if 1 mL of working solution is to be prepared,you can add 100 μL of 25.0 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.2102 mL | 6.0509 mL | 12.1018 mL | |
| 5 mM | 0.2420 mL | 1.2102 mL | 2.4204 mL | |
| 10 mM | 0.1210 mL | 0.6051 mL | 1.2102 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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