Chemical Structure : CDK6 PROTAC 48a
CAS No.:
CDK6 PROTAC 48a
Catalog No.: PC-25892Not For Human Use, Lab Use Only.
CDK6 PROTAC 48a is a potent, selective, KLHDC2-mediated CDK6 PROTAC degrader with DC50 of 37 nM in MOLM-14 cells, selectively degrades CDK6 among 8642 proteins and within the CDK family.
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Purity & Documentation Purity:
>98% (HPLC)
Biological Activity
CDK6 PROTAC 48a is a potent, selective, KLHDC2-mediated CDK6 PROTAC degrader with DC50 of 37 nM in MOLM-14 cells, selectively degrades CDK6 among 8642 proteins and within the CDK family.
CDK6 PROTAC 48a exhibits high KLHDC2 binding affinity (KLHDC2 KD=5 nM).
CDK6 PROTAC 48a induces CDK6 degradation via a proteasome-dependent mechanism.
CDK6 PROTAC 48a exhibits antiproliferative effect in MOLM-14 cells with GI50 of 0.76 uM and 0.23 uM in MOLM-13 cells.
CDK6 PROTAC 48a induces dose-dependent reduction in phosphorylated Rb (pRb) levels in MOLM-14 cells, induces a reduction in c-Myc and cyclin D3 and an elevation in cleaved PARP levels.
CDK6 PROTAC 48a (5 mg/kg and 10 mg/kg, i.v.) reduced tumor burden and CDK6 levels in MOLM-14 xenograft mouse models.
Physicochemical Properties
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M.Wt
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1268.58
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Formula
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C70H89N15O8
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Appearance
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Solid
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CAS No.
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Storage
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- Solide Powder
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-20°C 12 Months; 4°C 6 Months
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- In Solvent
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-80°C 6 Months; -20°C 6 Months
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Shipping
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Solubility
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10 mM in DMSO
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Chemical Name/SMILES
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Methyl 2-(4-(((S)-N-(2-((1R,4S)-4-(2-(4-(4-(6-((6-Acetyl-8-cyclopentyl-5-methyl-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-yl)amino)pyridin-3-yl)piperazine-1-carbonyl)piperidin-1-yl)-7-azaspiro[3.5]nonane-7-carbonyl)cyclohexane-1-carboxamido)ethyl)-1-(isoquinolin-4-yl)piperidine-3-carboxamido)methyl)-1H-pyrazol-1-yl)acetate
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References
1. Jeon E, et al. J Med Chem. 2025 Dec 2. doi: 10.1021/acs.jmedchem.5c02713.
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