PROTAC CDK4/6/9 degrader 1 

PROTAC CDK4/6/9 degrader 1 is a CDK4/6/9 PROTAC degrader. PROTAC CDK4/6/9 degrader 1 degrades CDK4, CDK6, and CDK9 in TNBC cells and inhibits TNBC cell proliferation. PROTAC CDK4/6/9 degrader 1 induces G1 phase arrest, promotes apoptosis, and suppresses cell migration and invasion in TNBC cells. PROTAC CDK4/6/9 degrader 1 can be used for the study of triple-negative breast cancer (TNBC). (Pink: CDK4/6/9 ligand (HY-168440), Blue: CRBN Ligand (HY-14658), Black: Linker (HY-178512), E3 ligase ligand-linker conjugate (HY-178515))^[1].

PROTAC CDK4/6/9 degrader 1 (Compound B5) (0.1-1 nM, 96 h) shows potent antiproliferative activity against multiple TNBC cell lines including MDA-MB-231, CAL51, SUM-159, MDA-MB-453, Hs578T, MDA-MB-468, MDA-MB-436, 4T1, and EO771, with IC₅₀ values of 0.26 nM, 0.21 nM, 0.38 nM, 0.13 nM, 0.27 nM, 0.21 nM, 0.45 nM, 0.53 nM, and 0.59 nM, respectively^[1].
PROTAC CDK4/6/9 degrader 1 (0.1-1 nM, 24 h) exhibits potent CDK degradation activity in MDA-MB-231 cells, with DC₅₀ values of 0.71 nM for CDK4, 0.44 nM for CDK6, and 0.52 nM for CDK9^[1].
PROTAC CDK4/6/9 degrader 1 (0.1-1 nM, 24 h) shows potent CDK degradation activity in CAL51 cells, with DC₅₀ values of 0.79 nM for CDK4, 0.61 nM for CDK6, and 0.51 nM for CDK9^[1].
PROTAC CDK4/6/9 degrader 1 (1 nM, 3-48 h) demonstrates time-dependent degradation activity against CDK4, CDK6, and CDK9 in MDA-MB-231 and CAL51 cells^[1].
PROTAC CDK4/6/9 degrader 1 (100 nM, 8 h) displays selective inhibitory activity against CDK family members in TNBC cells, with inhibition rates of 98% for CDK4/CycD3, 98% for CDK6/CycD3, 92% for CDK9/CycT1, 91% for CDK6/CycD1, and weak inhibition on CDK13/CycK (51%), CDK5/p35NCK (47%)^[1].
PROTAC CDK4/6/9 degrader 1 (0.5-1 nM, 48 h) shows potent pro-apoptotic activity in MDA-MB-231 and CAL51 cells, significantly increasing the percentage of apoptotic cells^[1].
PROTAC CDK4/6/9 degrader 1 (0.5-1 nM, 24 h) exerts potent cell cycle arrest activity in MDA-MB-231 and CAL51 cells, inducing pronounced G1 phase arrest^[1].
PROTAC CDK4/6/9 degrader 1 (0.5-1 nM) exhibits potent anti-migratory and anti-invasive activity in MDA-MB-231 and CAL51 cells^[1].

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

955.11

C₅₁H₆₂N₁₂O₇

3064994-97-1

O=C(C1=CC2=C(N=C(N=C2)NC3=CC=C(C=C3)C(CN4CCN(CC4)CC5CCN(CC5)CC(N6CCN(CC6)C7=CC=C(C8=C7)C(N(C8=O)C9CCC(NC9=O)=O)=O)=O)=O)N1C%10CCCC%10)N(C)C

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• [1]. Hu H, et al. Translational Research on the Oral Delivery of the Cytotoxic PROTAC Molecule via Tumor-Targeting Prodrug Strategy for Triple-Negative Breast Cancer Treatment. J Med Chem. 2025 Oct 9;68(19):20464-20486.  [Content Brief]