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PROTAC CDK2-pRb degrader-1

CDK2 Degrader PROTAC

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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Specifications

Manufacturer	Adooq Bioscience
Actions	Degrader
CAS Number	3030276-48-0
Applications	CDK2 Degrader PROTAC
Formula	C₄₀H₅₀F₄N₈O₅S
Molecular Weight	830.93
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

Storage & Solubility

In Vitro Solubility

Reported Solubility

No reported solubility data are available for this product.

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.