PROTAC CDK2 Degrader-2
Based on 1 Customer Validation
PROTAC CDK2 Degrader-2 is an orally active CDK2 PROTAC degrader, with DC50 values of 13 nM (MKN1cells) and 17 nM (TOV21G cells). PROTAC CDK2 Degrader-2 induces G1 phase arrest in MKN1 cells. PROTAC CDK2 Degrader-2 achieves tumor stasis in HCC1569 (CCNE1-amplified) xenograft models. PROTAC CDK2 Degrader-2 can be used for the study of CCNE1-amplified cancers.
For research use only. We do not sell to patients.
- Purity : 99.51%
- CAS No.: 3030279-55-8
- Formula: C39H46F6N8O5S
- Molecular Weight:852.89
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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
- Protocols
- Purity & Documentation
- References
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Help & FAQs
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Biological Activity
Description
IC50 & Target
[1]|
CDK2 13 nM (DC50, MKN1cells) |
CDK2 17 nM (DC50, TOV21G cells) |
CDK1 2130 nM (DC50) |
In Vitro
PROTAC CDK2 Degrader-2 (Compound 37) exhibits potent CDK2 degradation activity in MKN1 (CCNE1-amplified) and TOV21G (CCNE1-nonamplified) cells, with DC50 values of 13 nM and 17 nM[1].
PROTAC CDK2 Degrader-2 displays potent antiproliferative activity against MKN1 (CCNE1-amplified) cells with an IC50 of 9 nM, while showing weak activity against TOV21G (CCNE1-nonamplified) cells with an IC50 of 5760 nM[1].
PROTAC CDK2 Degrader-2 (4.88-5000 nM , 72 h) induces maximum G1 phase arrest (on-target effect) at 78 nM and shows off-target G2/M accumulation at 2500 nM in MKN1 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
Parmacokinetics
| Species | Dose | Route | CL | Vss | T1/2 | Tmax | Cmax | AUClast | F |
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| Dog[1] | 0.1 mg/kg | i.v. | 0.1 mL/min/kg | 3.9 L/kg | 14.4 h | / | / | / | / |
| Dog[1] | 1 mg/kg | p.o. | / | / | / | 4.0 h | 0.025 μM | 0.557 μM·h | 12 % |
| Monkey[1] | 0.07 mg/kg | i.v. | 9.1 mL/min/kg | 5.7 L/kg | 6.7 h | / | / | / | / |
| Monkey[1] | 1 mg/kg | p.o. | / | / | / | 4.0 h | 0.014 μM | 3.63 μM·h | 21 % |
| Rat[1] | 10 mg/kg | p.o. | / | / | / | 2.0 h | 0.261 μM | 3.63 μM·h | 21 % |
| Rat[1] | 2 mg/kg | i.v. | 10 mL/min/kg | 5 L/kg | 6.7 h | / | / | / | / |
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:HCC1569 human breast carcinoma cells (6 × 106 cells + Matrigel in 0.2 mL RPMI 1640 medium) were subcutaneously implanted into the central right flank of 7-day acclimated female NOG mice[1]
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Dosage:10 mg/kg, 25 mg/kg, 50 mg/kg
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Administration:p.o., once or twice daily, 28 days
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Result:Achieved tumor stasis in HCC1569 (CCNE1-amplified) xenograft model.
Chemical Information
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CAS No. 3030279-55-8
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Appearance Solid
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Molecular Weight 852.89
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Formula C39H46F6N8O5S
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Color White to off-white
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SMILES
O=S(C1=CC=C(NC2=NC=C(C(F)(F)F)C(N3C[C@@](C)(O)CCC3)=N2)C(F)=C1)(N[C@H]4[C@@H](F)CN(CC5CCN(C6=CC=C(C(CC7)C(NC7=O)=O)C=C6F)CC5)CC4)=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
In Vitro:
DMSO : 100 mg/mL (117.25 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)
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.
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.
In Vivo Dissolution Calculator
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.
Protocols
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Patient-Derived Xenograft (PDX)
Patient-derived xenograft (PDX) models are generated by engrafting primary human tumor tissue directly into immunodeficient mice, allowing in vivo propagation of patient tumor biology without initial in vitro adaptation. These models are used to preserve key histopathological and molecular characteristics of the original tumor and enable assessment of tumor growth dynamics and therapeutic response in a living organism. The biological readout is tumor engraftment and subsequent growth in the murine host, which reflects the ability of human tumor cells to survive, vascularize, and expand in an immunocompromised microenvironment.
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Splenic/Portal-Vein Liver Metastasis Xenograft
Splenic and portal-vein liver metastasis xenograft models deliver tumor cells into the portal circulation so that cells reach the liver first and form hepatic metastatic lesions; splenic injection uses the spleen as an access route to the portal system, while direct portal-vein injection introduces cells into the portal vein without requiring splenectomy. The assay detects liver colonization, intrahepatic tumor growth, tumor distribution, treatment response, survival, and liver-metastasis microenvironment changes; readouts include bioluminescence or fluorescence imaging, gross liver nodule counts, liver weight or tumor burden, histology, and survival.
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
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Orthotopic Cell-Line Xenograft
Orthotopic cell-line xenograft models involve implantation of human cancer cell lines into the anatomically corresponding organ of immunodeficient mice to reproduce tumor growth within a native microenvironment, enabling more clinically relevant tumor behavior compared with subcutaneous models. These models are widely used because orthotopic placement better recapitulates tumor progression, including invasion and metastatic spread, which are often underrepresented in heterotopic implantation systems. Compared with conventional xenografts, orthotopic implantation is described as more technically complex but provides improved simulation of tumor-microenvironment interactions and metastatic behavior, making it particularly valuable for translational oncology research. Surgical orthotopic implantation approaches have been emphasized as enabling faithful reproduction of clinical cancer features, including metastasis and disease progression patterns that align with the tumor’s organ of origi
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Intraperitoneal/Peritoneal Dissemination Xenograft
Intraperitoneal (IP) or peritoneal dissemination xenograft models are based on the introduction of human cancer cells into the peritoneal cavity of immunodeficient mice, where they attach to peritoneal surfaces, form multicellular aggregates or spheroids, and progressively generate disseminated tumor nodules that mimic advanced peritoneal metastatic disease. These models are widely used to study ovarian cancer progression, tumor-microenvironment interactions, and intraperitoneal therapeutic responses, often incorporating bioluminescence or fluorescence imaging to longitudinally monitor tumor burden in vivo. The biological principle relies on the capacity of tumor cells such as SKOV3 or related ovarian carcinoma lines to survive in suspension, aggregate within ascites-like fluid, adhere to mesothelial surfaces, and invade peritoneal organs, thereby recapitulating human peritoneal carcinomatosis patterns observed in advanced disease.
Purity & Documentation
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Data Sheet (277 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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 | 1.1725 mL | 5.8624 mL | 11.7248 mL | 29.3121 mL |
| 5 mM | 0.2345 mL | 1.1725 mL | 2.3450 mL | 5.8624 mL | |
| 10 mM | 0.1172 mL | 0.5862 mL | 1.1725 mL | 2.9312 mL | |
| 15 mM | 0.0782 mL | 0.3908 mL | 0.7817 mL | 1.9541 mL | |
| 20 mM | 0.0586 mL | 0.2931 mL | 0.5862 mL | 1.4656 mL | |
| 25 mM | 0.0469 mL | 0.2345 mL | 0.4690 mL | 1.1725 mL | |
| 30 mM | 0.0391 mL | 0.1954 mL | 0.3908 mL | 0.9771 mL | |
| 40 mM | 0.0293 mL | 0.1466 mL | 0.2931 mL | 0.7328 mL | |
| 50 mM | 0.0234 mL | 0.1172 mL | 0.2345 mL | 0.5862 mL | |
| 60 mM | 0.0195 mL | 0.0977 mL | 0.1954 mL | 0.4885 mL | |
| 80 mM | 0.0147 mL | 0.0733 mL | 0.1466 mL | 0.3664 mL | |
| 100 mM | 0.0117 mL | 0.0586 mL | 0.1172 mL | 0.2931 mL |
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