Product Data Sheet
PROTAC CDK2-pRb degrader-1
Catalog No. B21941
PROTAC CDK2-pRb degrader-1 is an orally active PROTAC that targets cyclin-dependent kinase 2 (CDK2) for degradation. This compound effectively inhibits the phosphorylation of retinoblastoma protein (Rb) at serine 807/811 by promoting the ubiquitination and proteasomal degradation of CDK2. Demonstrating significant biological activity with EC50 values of 12 nM and 125 nM in human cells, PROTAC CDK2-pRb degrader-1 is particularly useful in research focused on CCNE1-amplified cancers, including ovarian, gastric, and breast cancers, as it inhibits tumor growth and induces tumor stasis in xenograft models.
Chemical Information
| Catalog Num | B21941 |
|---|---|
| M. Wt | 830.93 |
| Formula | C40H50F4N8O5S |
| Purity | >98% |
| Storage | at -20 °C 3 years (powder form); at -20 °C 6 months (Solution base) |
| CAS No. | 3030276-48-0 |
| Synonyms | |
| SMILES | FC(F)(C1=CN=C(NC2=C(C=C(C=C2)S(N[C@H]3CC[C@@H](CC3)CN4CCN(C5=C(C=C(C6C(NC(CC6)=O)=O)C=C5)F)CC4)(=O)=O)C)N=C1N7C[C@@](O)(CCC7)C)F |
Biological Activity
| Description | PROTAC CDK2-pRb degrader-1 is an orally active PROTAC that targets cyclin-dependent kinase 2 (CDK2) for degradation. This compound effectively inhibits the phosphorylation of retinoblastoma protein (Rb) at serine 807/811 by promoting the ubiquitination and proteasomal degradation of CDK2. Demonstrating significant biological activity with EC50 values of 12 nM and 125 nM in human cells, PROTAC CDK2-pRb degrader-1 is particularly useful in research focused on CCNE1-amplified cancers, including ovarian, gastric, and breast cancers, as it inhibits tumor growth and induces tumor stasis in xenograft models. |
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RETURN POLICY
Adooq’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
Adooq’s Unconditional Return Policy ensures a smooth online shopping experience for our customers. If you are in any way unsatisfied with your purchase, you may return any item(s) within 7 days of receiving it. In the event of product quality issues, either protocol related or product related problems, you may return any item(s) within 365 days from the original purchase date. Please follow the instructions below when returning products.
SHIPPING AND STORAGE
Adooq products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Adooq Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Adooq products are stable under the recommended conditions.
Adooq products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Adooq Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Adooq products are stable under the recommended conditions.
