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首页-小分子抑制剂&激动剂-Membrane Transporter/Ion Channel-Exportin-1 (CRM1,XPO1)-SZJK-0421
SZJK-0421

Chemical Structure : SZJK-0421

CAS No.: 2664050-18-2

SZJK-0421 (SZJK0421)

货号: PC-23457Not For Human Use, Lab Use Only.

SZJK-0421 is a potent, selective second-generation reversible exportin-1 (CRM1) inhibitor with IC50 of 87.1 nM against MM1S cells.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

SZJK-0421 is a potent, selective second-generation reversible exportin-1 (CRM1) inhibitor with IC50 of 87.1 nM against MM1S cells.
SZJK-0421 is more active than KPT-8602 in both hematological tumors Mv-4–11, MOLM-13 and solid tumors HCT-116, BXPC-3, AN3CA.
SZJK-0421 inhibits nuclear export of CRM1. SZJK-0421 effectively inhibited the growth of both hematological and solid tumors, with no significant side effects during administration.
SZJK-0421 covalently bound to CRM1 protein, but the binding was more reversible.

物理化学性质&存储条件

分子量 458.32
分子式 C18H12F6N6O2
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

(E)-3-(3-(3,5-Bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)-N-methoxy-2-(pyrimidin-5-yl)acrylamide

参考文献

1. Wang J, et al. Acta Pharm Sin B. 2024 Jul;14(7):3281-3285.

2. Miao H, et al. J Med Chem. 2024 Nov 7. doi: 10.1021/acs.jmedchem.4c02169.

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