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首页-抗体药物偶连体和PROTACs-PROTAC-Reziciclideg
Reziciclideg

Chemical Structure : Reziciclideg

CAS No.: 3011828-23-9

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Reziciclideg (BTX-9341, BTX9341)

货号: PC-27493Not For Human Use, Lab Use Only.

Reziciclideg (BTX-9341) is a potent, seletive, blood-brain barrier permeable cereblon-mediated bifunctional degrader of CDK4 and CDK6 with Kd of 31 nM (CDK6).

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

    生物&药学活性

    Reziciclideg (BTX-9341) is a potent, seletive, blood-brain barrier permeable cereblon-mediated bifunctional degrader of CDK4 and CDK6 with Kd of 31 nM (CDK6), DC50 of <1 nM (Dmax>85%)
    BTX-9341 is more selective than the CDK4/6i palbociclib at 100 nM, and proteomics indicates minimal off-target degradation.
    BTX-9341 is blood-brain barrier permeable and shows sustained intracranial exposure for more than 12 hours.
    BTX-9341 functionally inhibits cell proliferation in multiple GBM cell lines with IC50s in the nanomolar range.
    BTX-9341 inhibits Rb phosphorylation in different GBM cell lines with pRb IC50s below 10 nM.
    BTX-9341 induces cell cycle arrest at low nanomolar concentrations in GBM cell lines.
    BTX-9341 exhibits dose dependent tumor growth inhibition in U-87 intracranial xenograft model (MGMT-negative), shows superior survival as compared to abemaciclib and Palbociclib.
    BTX-9341 inhibits tumor growth in U-118 xenograft model (MGMT-positive).

    物理化学性质&存储条件

    分子量 745.93
    分子式 C42H51N9O4
    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

    2,6-Piperidinedione, 3-[4-[4-[2-[1-[6-[(6-acetyl-8-cyclopentyl-7,8-dihydro-5-methyl-7-oxopyrido[2,3-d]pyrimidin-2-yl)amino]-3-pyridinyl]-4-piperidinyl]ethyl]-1-piperazinyl]phenyl]-

    参考文献

    1. Patent WO2023220640 A1 2023-11-16.

    2. Hannah Majeski, et al. J Clin Oncol 42, 3111(2024).

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