PROTAC CDK2/4/6 Degrader-2
Based on 1 Customer Validation
PROTAC CDK2/4/6 Degrader-2 is a CDK2/4/6 PROTAC degrader. PROTAC CDK2/4/6 Degrader-2. PROTAC CDK2/4/6 Degrader-2 can be converted into the prodrug PROTAC CDK2/4/6 Degrader-1 (HY-171826) through a one-step reaction with chloromethyl pivalate. PROTAC CDK2/4/6 Degrader-2 degrades CDK2/4/6 and their complex in malignant melanomas cells. PROTAC CDK2/4/6 Degrader-2 induces cell cycle arrest and cell apoptosis in various cancer cells, in particular for melanomas. PROTAC CDK2/4/6 Degrader-2 can be used for malignant melanomas research.
(Pink: CDK2 and CDK4 and CDK6 ligand (HY-168440); Blue: Cereblon ligand (HY-10984); Black: linker).
For research use only. We do not sell to patients.
- Purity: 97.22%
- CAS No.: 2541626-49-5
- Formula: C40H45N9O6
- Molecular Weight:747.84
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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
Biological Activity
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CDK2 |
CDK3 |
CDK6 |
Caspase 3 |
CDK4 |
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| A-375 | IC50 |
0.1659 μM
Compound: 3
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Cytotoxicity against human A375 cells assessed as reduction in cell viability after 72 hrs by MTT assay
Cytotoxicity against human A375 cells assessed as reduction in cell viability after 72 hrs by MTT assay
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[PMID: 33256948] |
PROTAC CDK2/4/6 Degrader-2 (compound 3) (72 h) exhibits prominent anti-proliferative activity against B16F10 and A375, with IC50s of 0.09861 and 0.1659 μM, respectively[1].
PROTAC CDK2/4/6 Degrader-2 (0-2000 nM, 0-12 h) mediates CDK2/4/6 protein degradation and impairs downstream Rb signaling activation by hijacking the E3 ubiquitin ligase CRBN in B16F10 and A375 cells[1].
PROTAC CDK2/4/6 Degrader-2 (50-500 nM, 7 days) exerts significant anti-proliferative activity in B16F10 and A375 cells[1].
PROTAC CDK2/4/6 Degrader-2 (125-1000 nM,48 h) significantly induces apoptosis of A375 and B16F10 cells in a dose-dependent manner in B16F10 and A375 cells[1].
PROTAC CDK2/4/6 Degrader-2 (0-2000 nM, 48 h) induces caspase-dependent apoptosis via the common P53/Bcl-2/Bax apoptotic pathway in B16F10 and A375 cells[1].
PROTAC CDK2/4/6 Degrader-2 (25-1000 nM ,48 h) induces cell cycle arrest via the degradation of cell cycle-related proteins CDK2/4/6 in A375 and B16F10 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:B16F10 and A375 cells
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Concentration:0, 62.5, 100, 125, 250, 500, 1000 and 2000 nM
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Incubation Time:0, 3, 6, 9 and 12 h
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Result:Induced significant intracellular cleavage of all CDK 2, CDK 4 and CDK 6 proteins in both concentration-dependent and time dependent manners.
Mitigated downstream p-Rb signaling pathway activation of melanoma cells.
Induced CDK2/4/6 protein degradation via the proteasomal pathway at 100 nM and 6 h.
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Cell Line:B16F10 and A375
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Concentration:50, 100, 250, 500 nM
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Incubation Time:7 days
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Result:Exerted a remarkable inhibiting effect on colony formation in A375 and B16F10 in low nano molar concentration.
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Cell Line:B16F10 and A375 cells
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Concentration:125, 250, 500, 1000 nM
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Incubation Time:48 h
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Result:Significantly induced apoptosis.
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Cell Line:B16F10 and A375 cells
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Concentration:0, 62.5, 125, 250, 500, 1000 and 2000 nM
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Incubation Time:48 h
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Result:Upregulated casepase-3 and cleaved PARP protein expression.
Also significantly induced up-regulation of the pro-protein level of P-53 and Bax.
Downregulated the anti-apoptotic protein level of Bcl-2.
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Cell Line:B16F10 and A375 cells
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Concentration:0, 25, 50, 100, 250, 500, 1000 nM
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Incubation Time:48 h
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Result:Increased accumulation of A375 cell population in G0/G1 phase, but G2/M phase for B16F10 cell.
Chemical Information
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CAS No. 2541626-49-5
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Appearance Solid
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Molecular Weight 747.84
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Formula C40H45N9O6
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Color White to yellow
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SMILES
O=C(C1=CC=C(NC2=NC3=C(C=C(N3C4CCCC4)C(N(C)C)=O)C=N2)C=C1)NCCCCCCNC5=CC=CC(C(N6C7C(NC(CC7)=O)=O)=O)=C5C6=O
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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 : 200 mg/mL (267.44 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: ≥ 5 mg/mL (6.69 mM); Suspended solution
This protocol yields a suspended solution of ≥ 5 mg/mL (saturation unknown). Suspended solution can be used for oral and intraperitoneal injection.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 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 (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. 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 | 1.3372 mL | 6.6859 mL | 13.3718 mL | 33.4296 mL |
| 5 mM | 0.2674 mL | 1.3372 mL | 2.6744 mL | 6.6859 mL | |
| 10 mM | 0.1337 mL | 0.6686 mL | 1.3372 mL | 3.3430 mL | |
| 15 mM | 0.0891 mL | 0.4457 mL | 0.8915 mL | 2.2286 mL | |
| 20 mM | 0.0669 mL | 0.3343 mL | 0.6686 mL | 1.6715 mL | |
| 25 mM | 0.0535 mL | 0.2674 mL | 0.5349 mL | 1.3372 mL | |
| 30 mM | 0.0446 mL | 0.2229 mL | 0.4457 mL | 1.1143 mL | |
| 40 mM | 0.0334 mL | 0.1671 mL | 0.3343 mL | 0.8357 mL | |
| 50 mM | 0.0267 mL | 0.1337 mL | 0.2674 mL | 0.6686 mL | |
| 60 mM | 0.0223 mL | 0.1114 mL | 0.2229 mL | 0.5572 mL | |
| 80 mM | 0.0167 mL | 0.0836 mL | 0.1671 mL | 0.4179 mL | |
| 100 mM | 0.0134 mL | 0.0669 mL | 0.1337 mL | 0.3343 mL |
PROTAC CDK2/4/6 Degrader-2 Related Classifications
HY-185121 Related Classifications
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