1. Cell Cycle/DNA Damage PROTAC
  2. CDK PROTACs
  3. PROTAC CDK2/4/6 Degrader-1

PROTAC CDK2/4/6 Degrader-1 is an orally active CDK2/CDK4/CDK6 PROTAC degrader. PROTAC CDK2/4/6 Degrader-1 is a prodrug derived from PROTAC CDK2/4/6 Degrader-2 via one-step reaction with chloromethyl pivalate. PROTAC CDK2/4/6 Degrader-1 can be used for malignant melanoma research.
(Pink: Aurora A ligand (HY-168440); Blue: Cereblon ligand (HY-10984); Black: linker).

For research use only. We do not sell to patients.

PROTAC CDK2/4/6 Degrader-1

PROTAC CDK2/4/6 Degrader-1 Chemical Structure

CAS No. : 2541626-55-3

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Description

PROTAC CDK2/4/6 Degrader-1 is an orally active CDK2/CDK4/CDK6 PROTAC degrader. PROTAC CDK2/4/6 Degrader-1 is a prodrug derived from PROTAC CDK2/4/6 Degrader-2 via one-step reaction with chloromethyl pivalate. PROTAC CDK2/4/6 Degrader-1 can be used for malignant melanoma research[1]. (Pink: Aurora A ligand (HY-168440); Blue: Cereblon ligand (HY-10984); Black: linker).

IC50 & Target[1]

CDK2/cyclinE

 

CDK6

 

CDK4

 

In Vitro

PROTAC CDK2/4/6 Degrader-1 (compound 11) is a prodrug derived from PROTAC CDK2/4/6 Degrader-2 (HY-185121) (compound 3) via one-step reaction with chloromethyl pivalate. PROTAC CDK2/4/6 Degrader-2 is a CDK2/CDK4/CDK6 PROTAC degrader degrading CDK2/4/6 proteins and their complexes, inducing cell cycle arrest and apoptosis in melanoma cells[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

PROTAC CDK2/4/6 Degrader (compound 11) (200 mg/kg, o.p.,once daily for 15 days) distinctly inhibits B16F10 tumor growth and mediate degradation of CDK2/4/6 in B16F10 xenograft mice model[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: B16F10 cells induced- C57BL/6J mice[1]
Dosage: 200 mg/kg
Administration: o.p., 15 days
Result: Significantly suppressed tumor sizes.
No Noticeable difference in body weight.
Molecular Weight

861.98

Formula

C46H55N9O8

CAS No.
SMILES

O=C(C1=CC=C(NC2=NC3=C(C=C(N3C4CCCC4)C(N(C)C)=O)C=N2)C=C1)NCCCCCCNC5=CC=CC(C(N6C7C(N(COC(C(C)(C)C)=O)C(CC7)=O)=O)=O)=C5C6=O

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Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation
References
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Product Name:
PROTAC CDK2/4/6 Degrader-1
Cat. No.:
HY-171826
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