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首页-小分子抑制剂&激动剂-Nuclear Receptor/Transcription Factor-Eukaryotic Initiation Factor (eIF)-eFT226
eFT226

Chemical Structure : eFT226

CAS No.: 2098191-53-6

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eFT226 (Zotatifin, eFT 226)

货号: PC-63308Not For Human Use, Lab Use Only.

Zotatifin (eFT226) is a novel, potent and selective eIF4A inhibitor with anti-tumor activity in B-cell malignancies, promotes eIF4A binding to specific mRNA sequences and interferes with the assembly of the eIF4F initiation complex.

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5 mg ￥18800 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

Zotatifin (eFT226) is a novel, potent and selective eIF4A inhibitor with anti-tumor activity in B-cell malignancies, promotes eIF4A binding to specific mRNA sequences and interferes with the assembly of the eIF4F initiation complex.
Zotatifin (eFT226) selectively inhibits translation of mRNAs containing longer 5'-UTRs, an increased frequency of uORFs (upstream open reading frame), and polypurine and/or G-quadraplex recognition motifs.
Zotatifin (eFT226) demonstrates potent inhibition of reporter constructs containing a polypurine motif in the 5'-UTR with IC50 of 2 nM.
Zotatifin (eFT226) shows potent anti-proliferative activity (EC50<15 nM) and an induction of apoptosis against a panel of B-cell lymphoma cell lines, dose-dependently decreases the oncogenic drivers c-MYC, CCND1/3, BCL2 or MCL-1.
Zotatifin (eFT226) shows in vivo activity across hematological tumor models.

物理化学性质&存储条件

分子量 487.55
分子式 C28H29N3O5
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

4-[(5aR,6S,7S,8R,8aS)-7-[(Dimethylamino)methyl]-6,7,8,8a-tetrahydro-8,8a-dihydroxy-1,3-dimethoxy-6-phenyl-5aH-cyclopenta[4,5]furo[3,2-c]pyridin-5a-yl]benzonitrile

参考文献

1. Peggy A. Thompson, et al. Preclinical Evaluation of eFT226, a Novel, Potent and Selective eIF4A Inhibitor with Anti-tumor Activity in B-cell Malignancies.

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