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PROTAC CDK2-pRb degrader-1
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Catalog No. T218853 Copy Product Info
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PROTAC CDK2-pRb degrader-1 is an orally bioavailable degrader belonging to the PROTAC class, specifically targeting CDK2/cyclin E complexes. It functions by promoting the ubiquitination and proteasomal degradation of CDK2, thereby effectively inhibiting the phosphorylation of retinoblastoma protein (Rb) at serine residues 807/811. PROTAC CDK2-pRb degrader-1 demonstrates significant activity in human cells with EC50 values of 12 nM and 125 nM. In xenograft models, it inhibits tumor growth and induces tumor stasis, making it suitable for research on CCNE1-amplified cancers, including ovarian, gastric, and breast cancers.
PROTAC CDK2-pRb degrader-1
Cas No. 3030276-48-0
| Pack Size | Price | USA Stock | Global Stock | Quantity |
|---|---|---|---|---|
| 10 mg | Inquiry | Inquiry | Inquiry | |
| 50 mg | Inquiry | Inquiry | Inquiry |
For In stock only · Estimated delivery: USA Stock (1-2 days) Global Stock (5-7 days)
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For research use only—not for human use. No sales to individuals. Use as intended only.
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Product Introduction
Bioactivity
Chemical Properties
Storage & Solubility Information
| Description | PROTAC CDK2-pRb degrader-1 is an orally bioavailable degrader belonging to the PROTAC class, specifically targeting CDK2/cyclin E complexes. It functions by promoting the ubiquitination and proteasomal degradation of CDK2, thereby effectively inhibiting the phosphorylation of retinoblastoma protein (Rb) at serine residues 807/811. PROTAC CDK2-pRb degrader-1 demonstrates significant activity in human cells with EC50 values of 12 nM and 125 nM. In xenograft models, it inhibits tumor growth and induces tumor stasis, making it suitable for research on CCNE1-amplified cancers, including ovarian, gastric, and breast cancers. |
| In vitro | PROTAC CDK2-pRb degrader-1 (Compound 5) demonstrates the ability to degrade both CDK2 and Cyclin E1 simultaneously, showing enhanced activity in human cancer cell lines with CCNE1 amplification and restoring the inhibition of the RB pathway in Palbociclib-adapted breast cancer cells that overexpress Cyclin E1. At dose-response concentrations over 7 days, this compound exhibits CRBN-dependent antiproliferative effects in human cancer cell lines MKN1 and HCC1569. Additionally, in HCC1569 breast cancer cells that rely on functional RB protein, it shows antiproliferative activity. |
| In vivo | PROTAC CDK2-pRb degrader-1, when administered orally at a dose of 50 mg/kg twice daily, achieves nearly 90% pRB inhibition and 85% tumor growth suppression (approaching stasis) in OVCAR3 CCNE1-amplified ovarian cancer xenografts. It also induces tumor stasis or regression in CCNE1-amplified HCC1569 breast cancer xenograft models, resulting in 90% degradation of CDK2 and pRB inhibition. When administered once daily at the same dosage, it similarly causes tumor stasis or regression in CCNE1-amplified MKN1 gastric cancer xenografts, achieving 90% CDK2 degradation and pRB inhibition. |
| Molecular Weight | 830.93 |
| Formula | C40H50F4N8O5S |
| Cas No. | 3030276-48-0 |
| Smiles | C(F)(F)(F)C=1C(=NC(NC2=C(C)C=C(S(N[C@H]3CC[C@H](CN4CCN(CC4)C5=C(F)C=C(C=C5)C6C(=O)NC(=O)CC6)CC3)(=O)=O)C=C2)=NC1)N7C[C@@](C)(O)CCC7 |
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the stock solution preparation method and in vivo formula preparation method:
For example, if the intended dosage is 10 mg/kg for animals weighing 20 g , with a dosing volume of 100 μL per animal, and a total of 10 animals are to be administered, using a formulation of 
10% DMSO+ 40% PEG300+ 5% Tween 80+ 45% Saline/PBS/ddH2O , the resulting working solution concentration would be 2 mg/mL.Stock Solution Preparation:
Dissolve 2 mg of the compound in 100 μL DMSO to obtain a stock solution at a concentration of 20 mg/mL . If the required concentration exceeds the compound's known solubility, please contact us for technical support before proceeding.
Preparation of the In Vivo Formulation:
1) Add 100 μL of the DMSO stock solution to 400 µL PEG300 and mix thoroughly until the solution becomes clear.
2) Add 50 µL Tween 80 and mix well until fully clarified.
3) Add 450 µL Saline,PBS or ddH2O and mix thoroughly until a homogeneous solution is obtained.
This example is provided solely to demonstrate the use of the In Vivo Formulation Calculator and does not constitute a recommended formulation for any specific compound. Please select an appropriate dissolution and formulation strategy based on your experimental model and route of administration.
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Please see Inhibitor Handling Instructions for more frequently ask questions. Topics include: how to prepare stock solutions, how to store products, and cautions on cell-based assays & animal experiments, etc
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Related Tags: PROTAC CDK2-pRb degrader-1 in vivo | PROTAC CDK2-pRb degrader-1 in vitro | PROTAC CDK2-pRb degrader-1 formula | PROTAC CDK2-pRb degrader-1 molecular weight
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