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首页-抗体药物偶连体和PROTACs-PROTAC-dCDK9-010
dCDK9-010

Chemical Structure : dCDK9-010

CAS No.:

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dCDK9-010 (CDK9 degrader)

货号: PC-26832Not For Human Use, Lab Use Only.

dCDK9-010 is a highly efficient and selective positive transcription elongation factor b (P-TEFb) complex PROTAC degrader with DC50 of 0.5 uM in NCI-H226 cells, recruits the MDM2 E3 ligase to induce proteasome-dependent degradation of CDK9 and all cyclin T isoforms.

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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

    生物&药学活性

    dCDK9-010 is a highly efficient and selective positive transcription elongation factor b (P-TEFb) complex PROTAC degrader with DC50 of 0.5 uM in NCI-H226 cells, recruits the MDM2 E3 ligase to induce proteasome-dependent degradation of CDK9 and all cyclin T isoforms.
    dCDK9-010 displays no activity against a panel of CDK proteins and CDK9‐interacting proteins BRD4, Cyclin K, AFF1, or AFF4.
    dCDK9-010 potently inhibits RNA polymerase II carboxy-terminal repeat domain phosphorylation and blocks MDM2-mediated p53 degradation, resulting in concurrent p53 pathway activation.
    dCDK9-010 depleted significantly endogenous CDK9 and cyclin T at 500 nM in NCI-H460 non-small cell lung cancer cells, U87 glioblastoma cells, HCT116 colon cancer cells, and HT1080 fibrosarcoma cells.
    dCDK9-010 is capable of inhibiting cell proliferation and inducing apoptosis.
    dCDK9-010 (20 mg/kg, every other day, i.v.) significantly inhibited tumor growth in the NCI-H226 and TC-32 xenograft models in immunocompromised mice.

    物理化学性质&存储条件

    分子量 1182.23
    分子式 C57H68Cl2F2N8O9S2
    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

    N-(5-(((5-(tert-butyl)oxazol-2-yl)methyl)thio)thiazol-2-yl)-4-(1-(4-((2R,3S,4R,5S)-3-(3-chloro-2-fluorophenyl)-4-(4-chloro-2-fluorophenyl)-4-cyano-5-neopentylpyrrolidine-2-carboxamido)-3-methoxyphenyl)-1-oxo-5,8,11-trioxa-2-azatetradecan-14-oyl)piperidine-1-carboxamide

    参考文献

    1. Xian Guan, et al. MedComm (2020). 2026 Apr 9:7:e70723.

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