CDK6 PROTAC 48a

Chemical Structure : CDK6 PROTAC 48a

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货号: 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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100 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	1268.58
分子式	C70H89N15O8
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	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

参考文献

1. Jeon E, et al. J Med Chem. 2025 Dec 2. doi: 10.1021/acs.jmedchem.5c02713.

CDK6 PROTAC 48a

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CDK6 PROTAC 48a

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