PROTAC RIPK1 Degrader-1
Based on 1 Customer Validation
PROTAC RIPK1 Degrader-1 is a selective RIPK1 PROTAC degrader. PROTAC RIPK1 Degrader-1 degrades RIPK1 in multiple cancer cell lines (e.g., A375, B16F10 cells). PROTAC RIPK1 Degrader-1 enhances the anti-cancer effect of radiotherapy in syngeneic and humanized mouse models. PROTAC RIPK1 Degrader-1 can be used to study cancers such as melanoma.
(Pink: RIPK1 ligand (HY-175371); Blue: VHL ligand (HY-112078); Black: linker (HY-175373)).
For research use only. We do not sell to patients.
- Purity: 99.66%
- Formula: C69H85N13O6S2
- Molecular Weight:1256.63
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Storage:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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
All PROTACs Isoforms
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Biological Activity
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VHL |
RIPK1 |
PROTAC RIPK1 Degrader-1 (Compound 225-5) (0-1 μM, 1-20 h) induces RIPK1 degradation through the association of RIPK1, VHL, proteasome, and Cullin-RING E3 ligase complex in HEK-293T-RIPK1-HiBiT (DC50 < 0.1 nM, Dmax = 93 %), A375 (DC50 = 41 nM, Dmax = 97 %), B16F10 (DC50 = 91 nM, Dmax = 92 %), PC3, LNCap, MCF7, NOMO1, RS$;11, U87 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:A375, B16F10, PC3, LNCap, MCF7, NOMO1, RS$;11, U87 cells
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Concentration:0.001 μM, 0.01 μM, 0.1 μM, 1 μM
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Incubation Time:1 h, 2 h, 4 h, 8 h, 16 h, 20 h
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Result:Induced RIPK1 degradation.
| Species | Dose | Route | T1/2 | Tmax | Cmax | AUClast | AUCinf |
|---|---|---|---|---|---|---|---|
| Mice[1] | 5 mg/kg | i.p. | 5.41 h | 0.5 h | 3270 ng/mL | 4279 ng·h/mL | 4316 ng·h/mL |
PROTAC RIPK1 Degrader-1 (10-20 mg/kg, i.p., once daily, 3-11 days) lowers RIPK1 levels in humanized A375 melanoma NSG mouse model[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:B16F10 (0.3 M) C57BL/6 mouse model[1]
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Dosage:50 mg/kg/10 mg/kg
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Administration:i.p., twice daily, 3 days/i.v., twice daily, 3 days
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Result:Lowered RIPK1 levels.
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Animal Model:Humanized (PBMC, 1 × 107) A375 (5 M) melanoma NSG mouse model[1]
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Dosage:10 mg/kg, 20 mg/kg
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Administration:i.p., once daily, 3 days
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Result:Lowered RIPK1 levels.
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Animal Model:B16F10 (0.3 M) syngeneic C57BL/6 mouse model[1]
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Dosage:40 mg/kg+20 mg/kg
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Administration:i.p., once daily, 3 days+ once daily, 8 days
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Result:Delayed tumor growth and extended median survival from 19 to 24 days when used in combination with radiation therapy.
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Animal Model:A375 (1 M) humanized (PBMC, 1 × 107) NSG mouse model[1]
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Dosage:20 mg/kg
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Administration:i.p., once daily, 11 days
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Result:Reduced tumor volume by 89% in combination with radiation therapy.
Chemical Information
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Appearance Solid
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Molecular Weight 1256.63
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Formula C69H85N13O6S2
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Color White to off-white
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SMILES
O=C(N1CCC(CC1)CN2CCC(CN3CCN(CC(N[C@H](C(N4[C@H](C(N[C@@H](C)C5=CC=C(C6=C(C)N=CS6)C=C5)=O)C[C@@H](O)C4)=O)C(C)(C)C)=O)CC3)CC2)CN7C=C(C=N7)C8=CN=C(N)C9=C8SC=C9C%10=CC=C%11N(C(CC%12=CC=CC=C%12)=O)CCC%11=C%10
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
DMSO : 100 mg/mL (79.58 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 (protect from light). 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 (protect from light). 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 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (1.99 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
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. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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 (275 KB)
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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)
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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 (protect from light). 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 | 0.7958 mL | 3.9789 mL | 7.9578 mL | 19.8945 mL |
| 5 mM | 0.1592 mL | 0.7958 mL | 1.5916 mL | 3.9789 mL | |
| 10 mM | 0.0796 mL | 0.3979 mL | 0.7958 mL | 1.9894 mL | |
| 15 mM | 0.0531 mL | 0.2653 mL | 0.5305 mL | 1.3263 mL | |
| 20 mM | 0.0398 mL | 0.1989 mL | 0.3979 mL | 0.9947 mL | |
| 25 mM | 0.0318 mL | 0.1592 mL | 0.3183 mL | 0.7958 mL | |
| 30 mM | 0.0265 mL | 0.1326 mL | 0.2653 mL | 0.6631 mL | |
| 40 mM | 0.0199 mL | 0.0995 mL | 0.1989 mL | 0.4974 mL | |
| 50 mM | 0.0159 mL | 0.0796 mL | 0.1592 mL | 0.3979 mL | |
| 60 mM | 0.0133 mL | 0.0663 mL | 0.1326 mL | 0.3316 mL |
PROTAC RIPK1 Degrader-1 Related Classifications
HY-175370 Related Classifications
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