PROTAC DDR1 degrader-1
Based on 1 Customer Validation
PROTAC DDR1 degrader-1 is a potent and selective DDR1-targeting PROTAC degrader. PROTAC DDR1 degrader-1 selectively induces full-length DDR1 degradation via the ubiquitin proteasome system, blocking downstream signaling pathways. PROTAC DDR1 degrader-1 inhibits tumor cell migration and invasion. PROTAC DDR1 degrader-1 exhibits anti-tumor activity in mice. PROTAC DDR1 degrader-1 can be used for the research of DDR1-driven cancers.
(Pink: DDR1 ligand (HY-176185); Blue: Cereblon ligand (HY-W072954); Black: linker (HY-176186)).
For research use only. We do not sell to patients.
- Purity: 98.69%
- CAS No.: 3081612-73-6
- Formula: C43H40F3N9O7
- Molecular Weight:851.83
-
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]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Purity & Documentation
- References
-
Help & FAQs
All PROTACs Isoforms
More
Biological Activity
|
DDR1 |
PROTAC DDR1 degrader-1 (compound DP1) degrades DDR1 in MKN45, RM1, MDA-MB-468 cells, with DC50 values of 3.22, 0.99, and 3.90 nM, respectively[1].
PROTAC DDR1 degrader-1 (0-6 nM) inhibits DDR1 downstream signaling pathways in T47D human breast cancer cells by reducing DDR1, MMP2, MMP9, and pERK protein levels[1].
PROTAC DDR1 degrader-1 (10-100 nM; 0-24 h) potently inhibits the migration of T47D human breast cancer cells in a dose-dependent manner[1].
PROTAC DDR1 degrader-1 (10-100 nM; 24 h) potently inhibits the invasion of T47D human breast cancer cells in a dose-dependent manner[1].
PROTAC DDR1 degrader-1 (30 nM; 24 h) induces DDR1 degradation in T47D human breast cancer cells via the ubiquitin-proteasome system, dependent on binding to both DDR1 and E3 ligase[1].
PROTAC DDR1 degrader-1 (0-10000 nM; 24 h) does not induce degradation of DDR2 in SW579 or WM115 human cancer cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Cell Line:T47D human breast cancer cells
-
Concentration:10; 100 nM
-
Incubation Time:0; 24 h
-
Result:Significantly inhibited T47D cell migration in a dose-dependent manner, as shown by reduced wound closure compared to controls.
-
Cell Line:T47D human breast cancer cells
-
Concentration:10; 100 nM
-
Incubation Time:24 h
-
Result:Significantly inhibited T47D cell invasion in a dose-dependent manner, as shown by fewer invaded cells compared to controls.
-
Cell Line:SW579 and WM115 human cancer cells
-
Concentration:0; 10; 30; 100; 300; 1000; 3000; 10000 nM
-
Incubation Time:24 h
-
Result:Did not induce DDR2 degradation in SW579 or WM115 cells within 24 hours, even at a high concentration of 10 μM.
| Species | Dose | Route | Cmax | Tmax | T1/2 | AUC0-t | AUC0-∞ | MRT0-t | MRT0-∞ |
|---|---|---|---|---|---|---|---|---|---|
| Rat[1] | 10 mg/kg | i.v. | 48789 ng/mL | 0.05 h | 8.21 h | 105010 ng·h/mL | 105153 ng·h/mL | 6.62 h | 7.27 h |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
-
Animal Model:BALB/c mice (male, 7 weeks old, ~20g) subcutaneously injected with 4T1-hDDR1 or 4T1-WT cells[1]
-
Dosage:1; 10 mg/kg
-
Administration:i.v.; twice weekly; 2 weeks
-
Result:Reduced 4T1-hDDR1 tumor volume and weight significantly.
Increased CD8+ T cell infiltration into the tumor core to ~22% of total cells at high dose.
Increased CD3+ T cell infiltration to ~3.9% of tumor cells in the low-dose group and ~7.2% in the high-dose group.
Increased CD8+ T cell infiltration in the tumor margin.
Increased CD3+ T cell infiltration to ~1.8% of tumor cells at low dose.
Chemical Information
-
CAS No. 3081612-73-6
-
Appearance Solid
-
Molecular Weight 851.83
-
Formula C43H40F3N9O7
-
Color White to off-white
-
SMILES
COC1=CC=C(C=C1C#CC2=CN=C(N=C2)NC3CCN(CC3)CCC(NC4=CC=C5C(N(CC5=C4)C6CCC(NC6=O)=O)=O)=O)C(NC7=CC(C(N)=O)=CC(C(F)(F)F)=C7)=O
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
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 (117.39 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 (2.93 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:
-
-
-
-
Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
-
%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
-
%+
-
+%Tween-80 + +
-
%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
-
Data Sheet (273 KB)
-
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
-
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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.1739 mL | 5.8697 mL | 11.7394 mL | 29.3486 mL |
| 5 mM | 0.2348 mL | 1.1739 mL | 2.3479 mL | 5.8697 mL | |
| 10 mM | 0.1174 mL | 0.5870 mL | 1.1739 mL | 2.9349 mL | |
| 15 mM | 0.0783 mL | 0.3913 mL | 0.7826 mL | 1.9566 mL | |
| 20 mM | 0.0587 mL | 0.2935 mL | 0.5870 mL | 1.4674 mL | |
| 25 mM | 0.0470 mL | 0.2348 mL | 0.4696 mL | 1.1739 mL | |
| 30 mM | 0.0391 mL | 0.1957 mL | 0.3913 mL | 0.9783 mL | |
| 40 mM | 0.0293 mL | 0.1467 mL | 0.2935 mL | 0.7337 mL | |
| 50 mM | 0.0235 mL | 0.1174 mL | 0.2348 mL | 0.5870 mL | |
| 60 mM | 0.0196 mL | 0.0978 mL | 0.1957 mL | 0.4891 mL | |
| 80 mM | 0.0147 mL | 0.0734 mL | 0.1467 mL | 0.3669 mL | |
| 100 mM | 0.0117 mL | 0.0587 mL | 0.1174 mL | 0.2935 mL |
PROTAC DDR1 degrader-1 Related Classifications
HY-176184 Related Classifications
Powered by Bioz