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首页-小分子抑制剂&激动剂-Ras-Raf-MAPK-ERK Pathway-MNK-JDB153
JDB153

Chemical Structure : JDB153

CAS No.: 2644746-37-0

JDB153 (JDB-153)

货号: PC-27177Not For Human Use, Lab Use Only.

JDB153 is a highly potent, oral dual MNK/VEGFR2 inhibitor with IC50 of 26.6 nM, 27 nM and 3 nM for MNK1, MNK2 and VEGFR2 respectively.

规格 价格 库存 数量
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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

JDB153 is a highly potent, oral dual MNK/VEGFR2 inhibitor with IC50 of 26.6 nM, 27 nM and 3 nM for MNK1, MNK2 and VEGFR2 respectively.
JDB153 exhibits antiproliferative activity on lung cancer cell lines LL2 cell and H460 cell with IC50 of 6.6 uM and 8.3 uM.
JDB153 induces cell apoptosis and arrest lung cancer cells in the G0/G1 phase. cell migration, invasion and angiogenesis in H460 cells, and inhibits the phosphorylation of eIF4E and VEGFR2.
JDB153 shows synergistic antitumor effect with PD-1 in in LL2 subcutaneous tumor model, improves the antitumor immune of T cells in the TME.

物理化学性质&存储条件

分子量 513.55
分子式 C25H29F2N7O3
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

6'-((6-(2-(3,3-difluoropyrrolidin-1-yl)ethoxy)-5-methylpyrrolo[2,1-f][1,2,4]triazin-4-yl)amino)-8'-methyl-2'H-spiro[cyclopentane-1,3'-imidazo[1,5-a]pyridine]-1',5'-dione

参考文献

1. Xu M, et al. MedComm (2020). 2025 Apr 29;6(5):e70155.

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