DAS-5-oCRBN
Based on 1 Customer Validation
DAS-5-oCRBN is a PROTAC molecule with both c‑Src kinase inhibitory activity and target protein degradation activity, with an EC50 of 45 nM for c‑Src binding. DAS-5-oCRBN binds non-covalently to Cereblon and mediates target protein degradation via the ubiquitin-proteasome pathway. DAS-5-oCRBN can catalytically deplete intracellular c‑Src protein, while blocking both the kinase catalytic function of c‑Src and the non-catalytic protein interactions mediated by its SH2 and SH3 domains. DAS-5-oCRBN inhibits tumor cell proliferation and exerts significant anti-proliferative effects on both c‑Src kinase activity-dependent MDA-MB-231 cells and c‑Src protein level-dependent CAL51 cells. DAS-5-oCRBN can be used in cancer-related research such as studies on triple-negative breast cancer and chronic myeloid leukemia.
(Pink: c-Src ligand (HY-107447); Blue: Cereblon ligand (HY-148834); Black: linker).
For research use only. We do not sell to patients.
- Purity: 99.21%
- CAS No.: 3044084-97-8
- Formula: C39H40ClN11O6S
- Molecular Weight:826.32
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Storage:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
DAS-5-oCRBN potently degrades c-Src in CAL148 cells, with a DC50 of 3 nM and a degradation rate of 78% after treatment with 100 nM for 18 h; alternatively, it has a DC50 of 4 nM and a maximum degradation rate of up to 95% within 18 h. It potently inhibits the biochemical activity of c-Src kinase, with an IC50 of less than 30 nM under the condition of 1 mM ATP[1].
DAS-5-oCRBN (100 nM; 18 h) selectively degrades c-Src and Csk, with much higher selectivity for c-Src than for Bcr-Abl, and only degrades 4% of Bcr-Abl in KCL22 cells. It mediates the degradation of c-Src in CAL148 cells via a proteasomal pathway dependent on simultaneous binding to cereblon and the ATP-binding site of c-Src[1].
DAS-5-oCRBN (18 h) potently degrades c-Src in KCL22 cells with a DC50 of 5 nM, reaching a maximum degradation rate of 91% within 18 h; it potently degrades c-Src in MDA-MB-231 cells with a DC50 of 2.0 nM, reaching a maximum degradation rate of 95% within 18 h; it also potently degrades c-Src in CAL51 cells with a DC50 of 18 nM, reaching a maximum degradation rate of 88% within 18 h[1].
DAS-5-oCRBN (100 nM; 18 h) degrades 95% of c-Src in CAL148 cells; 96 h after compound washout, the protein level of c-Src recovers to 72% of the baseline level[1].
DAS-5-oCRBN (30-1000 nM; 1 h) acts as an intracellular c-Src inhibitor by suppressing the autophosphorylation of c-Src at the Y-419 site in SUM149 cells[1].
DAS-5-oCRBN potently inhibits the proliferation of MDA-MB-231 and CAL51 cells, with GI50 values of 6 nM and 74 nM, respectively; moreover, its antiproliferative effect at 400 nM is similar to that of c-Src siRNA knockdown[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:CAL148 cells
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Concentration:100 nM (DAS-5-oCRBN)
1 μM Bortezomib (HY-10227), 1 μM DGY-06-116 (HY-136605), 10 μM pomalidomide (HY-10984) (pre-treatment) -
Incubation Time:18 h
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Result:Pre-treatment with bortezomib, pomalidomide, or DGY-06-116 completely prevented c-Src degradation by DAS-5-oCRBN.
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Cell Line:CAL148 cells
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Concentration:30, 100, 300, 1000 nM
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Incubation Time:18 h; 96 h post-washout
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Result:Degraded 95% of c-Src over 18 h at 100 nM.
After washout, c-Src levels recovered to 72% of DMSO-treated control levels after 96 h, with full recovery estimated to require ~12 days.
Chemical Information
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CAS No. 3044084-97-8
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Appearance Solid
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Molecular Weight 826.32
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Formula C39H40ClN11O6S
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Color Light yellow to yellow
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SMILES
CC1=C(NC(C2=CN=C(NC3=CC(N4CCN(CC(N5CCN(C6=C7C(N(C8CCC(NC8=O)=O)C(C7=CC=C6)=O)=O)CC5)=O)CC4)=NC(C)=N3)S2)=O)C(Cl)=CC=C1
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
Solvent & Solubility
DMSO : 100 mg/mL (121.02 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (3.03 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (276 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.2102 mL | 6.0509 mL | 12.1018 mL | 30.2546 mL |
| 5 mM | 0.2420 mL | 1.2102 mL | 2.4204 mL | 6.0509 mL | |
| 10 mM | 0.1210 mL | 0.6051 mL | 1.2102 mL | 3.0255 mL | |
| 15 mM | 0.0807 mL | 0.4034 mL | 0.8068 mL | 2.0170 mL | |
| 20 mM | 0.0605 mL | 0.3025 mL | 0.6051 mL | 1.5127 mL | |
| 25 mM | 0.0484 mL | 0.2420 mL | 0.4841 mL | 1.2102 mL | |
| 30 mM | 0.0403 mL | 0.2017 mL | 0.4034 mL | 1.0085 mL | |
| 40 mM | 0.0303 mL | 0.1513 mL | 0.3025 mL | 0.7564 mL | |
| 50 mM | 0.0242 mL | 0.1210 mL | 0.2420 mL | 0.6051 mL | |
| 60 mM | 0.0202 mL | 0.1008 mL | 0.2017 mL | 0.5042 mL | |
| 80 mM | 0.0151 mL | 0.0756 mL | 0.1513 mL | 0.3782 mL | |
| 100 mM | 0.0121 mL | 0.0605 mL | 0.1210 mL | 0.3025 mL |
DAS-5-oCRBN Related Classifications
HY-163144 Related Classifications
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