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首页-抗体药物偶连体和PROTACs-PROTAC-JET-209
JET-209

Chemical Structure : JET-209

CAS No.: 3033714-58-5

JET-209 (JET209, JET 209)

货号: PC-20885Not For Human Use, Lab Use Only.

JET-209 (JET209) is a potent, selective PROTAC degrader of CBP/p300 based on GNE-207 with DC50 of 0.05 nM for CBP and 0.2 nM for p300, Dmax >95% for both proteins in the RS4;11 leukemia cell line.

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

    生物&药学活性

    JET-209 (JET209) is a potent, selective PROTAC degrader of CBP/p300 based on GNE-207 with DC50 of 0.05 nM for CBP and 0.2 nM for p300, Dmax >95% for both proteins in the RS4;11 leukemia cell line.
    JET-209 is extremely potent and effective in the inhibition of cell growth in the RS4;11 cell line with IC50 = 0.1 nM and Imax ≥ 94%.
    JET-209 is also effective in the induction of cell cycle arrest in the RS4;11 cell line.
    JET-209 is at least 1000 times more potent than CCS1477 and A-485 in inducing G1 cell cycle arrest in the RS4;11 cell line.
    JET-209 is also a very potent inhibitor of cell growth in the MV4;11, HL-60, and MOLM-13 acute leukemia cell lines, achieving IC50 values of 0.04, 0.54, and 2.3 nM, respectively.
    JET-209 potently and effectively suppresses the expression of MYC and MYB genes in the RS4;11 cell line.
    JET-209 effectively depletes CBP/p300 proteins in RS4;11 xenograft tumors in mice, JET-209 (1 mg/kg twice a week or 3 mg/kg weekly for 2 weeks, IP injection) effectively inhibits tumor growth in xenograft tumor models.

    物理化学性质&存储条件

    分子量 821.94
    分子式 C46H47N9O6
    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

    5-(8-(5-acetyl-1-(tetrahydro-2H-pyran-4-yl)-4,5,6,7-tetrahydro-1H-pyrazolo[4,3-c]pyridin-3-yl)isoquinolin-3-yl)-N-(1-(2-(2,6-dioxopiperidin-3-yl)-1-oxoisoindolin-5-yl)piperidin-4-yl)picolinamide

    参考文献

    1. Junius Eugene Thomas II, et al. Journal of Medicinal Chemistry, June 5, 2023

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