CDK2 degrader 3
Based on 1 Customer Validation
CDK2 degrader 3 is a selective CDK2 molecular glue-like degrader. CDK2 degrader 3 induces G1 cell cycle arrest in CCNE1-amplified cancer cells. CDK2 degrader 3 is applicable to breast cancer-related research.
For research use only. We do not sell to patients.
- Purity : 99.81%
- CAS No.: 2862772-71-0
- Formula: C44H53ClN10O6S
- Molecular Weight:885.47
-
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]
-
Biological Activity
-
Chemical Information
-
Solvent & Solubility
- Protocols
- Purity & Documentation
- References
-
Help & FAQs
Biological Activity
Description
IC50 & Target
|
CDK2 |
In Vitro
CDK2 degrader 3 (compound 1) preferentially forms ternary complexes with CDK2/CCNE1 over CDK1/CCNB1[1].
CDK2 degrader 3 drives preferential ubiquitination of CDK2/cyclin E1 over CDK1/cyclin B1[1].
CDK2 degrader 3 (24 h) potently degrades CDK2 in TOV21G cells with high selectivity over CDK1 and CDK9, with an absDC50 of 8 nM[1].
CDK2 degrader 3 (14 h) potently degrades CDK2 in MKN1 CCNE1amp cells with 95% maximum degradation at an absDC50 of 11 nM[1].
CDK2 degrader 3 (14 h) potently degrades CDK2 in HCC1569 CCNE1amp cells with 94% maximum degradation at an absDC50 of 10 nM[1].
CDK2 degrader 3 (24 h) potently inhibits RB phosphorylation at S807/811 in MKN1 CCNE1amp cells with 96% maximum inhibition at an absIC50 of 27 nM[1].
CDK2 degrader 3 (24 h) inhibits RB phosphorylation at S807/811 in HCC1569 CCNE1amp cells with 87% maximum inhibition at an absIC50 of 34 nM[1].
CDK2 degrader 3 (7 day) potently inhibits proliferation in CCNE1amp cancer cells with significantly lower activity in CCNE1non-amp TOV21G cells, with relIC50 values of 7 nM (MKN1), 16 nM (HCC1569), 28 nM (OVCAR3), and 4000 nM (TOV21G)[1].
CDK2 degrader 3 (500 nM (10x DC90); 24 h) selectively degrades CDK2 in human PBMCs with minimal off-target protein modulation[1].
CDK2 degrader 3 (80 nM; 24 h) suppresses E2F target gene expression in MKN1 cells[1].
CDK2 degrader 3 (1 μM Palbociclib (co-treatment); 24 h) co-degrades CDK2 and cyclin E1 in Palbociclib-adapted MCF7 and Hs578t breast cancer cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
-
Cell Line:Palbociclib-adapted (PA) MCF7 and Hs578t breast cancer cells
-
Concentration:1 µM Palbociclib (co-treatment)
-
Incubation Time:7 day
-
Result:Inhibited proliferation in MCF7 PA and Hs578t PA cells, with greater potency compared to activity in CCNE1non-amp cells.
-
Cell Line:MKN1 CCNE1amp cells
-
Concentration:0.0128-5000 nM
-
Incubation Time:72 h
-
Result:Induced G1 cell cycle arrest in a dose-dependent manner.
Achieved a 125x selectivity window between maximum G1 arrest (on-target) and increased G2/M population (off-target).
Chemical Information
-
CAS No. 2862772-71-0
-
Appearance Solid
-
Molecular Weight 885.47
-
Formula C44H53ClN10O6S
-
Color White to light yellow
-
SMILES
O=C1N(C2CCCC2)C3=NC(NC4=C(C=C(C=C4)S(NCCO[C@H]5CC[C@@H](CC5)CN6CCC(C7=CC8=NC=C(N9C(NC(CC9)=O)=O)N8C=C7)CC6)(=O)=O)C)=NC=C3C=C1Cl
-
Shipping
Room temperature in continental US; may vary elsewhere.
-
Storage
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
Solvent & Solubility
In Vitro:
DMSO : 50 mg/mL (56.47 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)
In Vivo:
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.
In Vivo Dissolution Calculator
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. * 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.
Protocols
-
Flow cytometric DNA-content cell-cycle staining
Flow cytometric DNA-content cell-cycle staining measures the fluorescence intensity of DNA-bound fluorochromes in single cells or nuclei to estimate DNA content distributions, allowing assignment of populations to G0/G1, S, and G2/M phases by DNA histogram deconvolution. Propidium iodide (PI) intercalates into DNA, and PI fluorescence is proportional to cellular DNA content when staining is performed under conditions that make DNA accessible and minimize non-DNA signal. Cells with G2/M DNA content are expected to show approximately twice the fluorescence intensity of G0/G1 cells, while S-phase cells occupy intermediate fluorescence values. PI-based DNA-content analysis can also detect cells with fractional DNA content, often reported as sub-G1, when DNA fragmentation and extraction during staining reduce retained DNA signal in apoptotic cells. DAPI is an alternative DNA fluorochrome for univariate DNA-content analysis, while bivariate approaches combining DNA content with proliferation
-
BrdU Incorporation Assay
Bromodeoxyuridine (BrdU) incorporation assay is based on the principle that BrdU, a thymidine analog, is incorporated into newly synthesized DNA during the S phase of the cell cycle, thereby serving as a marker of DNA replication and cellular proliferation. Incorporated BrdU can be detected using anti-BrdU antibodies following DNA denaturation, enabling visualization or quantification of proliferating cells through immunochemical detection methods such as immunofluorescence or immunohistochemistry.
-
Protocol for Cell Cycle
Cell-cycle analysis by flow cytometry measures DNA content in single cells to estimate the fraction of cells in G0/G1, S, and G2/M phases. Propidium iodide intercalates into DNA, and after RNA removal with RNase, fluorescence intensity reflects cellular DNA content: 2N cells are assigned to G0/G1, cells between 2N and 4N to S phase, and 4N cells to G2/M. DNA-content analysis alone cannot reliably separate G0 from G1 or G2 from M. Ki-67 can distinguish quiescent G0 cells from cycling cells, EdU or BrdU incorporation marks active DNA synthesis in S phase, and phospho-histone H3 staining identifies mitotic cells within the 4N population.
-
Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
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 (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 | 1.1293 mL | 5.6467 mL | 11.2934 mL | 28.2336 mL |
| 5 mM | 0.2259 mL | 1.1293 mL | 2.2587 mL | 5.6467 mL | |
| 10 mM | 0.1129 mL | 0.5647 mL | 1.1293 mL | 2.8234 mL | |
| 15 mM | 0.0753 mL | 0.3764 mL | 0.7529 mL | 1.8822 mL | |
| 20 mM | 0.0565 mL | 0.2823 mL | 0.5647 mL | 1.4117 mL | |
| 25 mM | 0.0452 mL | 0.2259 mL | 0.4517 mL | 1.1293 mL | |
| 30 mM | 0.0376 mL | 0.1882 mL | 0.3764 mL | 0.9411 mL | |
| 40 mM | 0.0282 mL | 0.1412 mL | 0.2823 mL | 0.7058 mL | |
| 50 mM | 0.0226 mL | 0.1129 mL | 0.2259 mL | 0.5647 mL |
CDK2 degrader 3 Related Classifications
HY-164827 Related Classifications
Powered by Bioz