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Zotatifin

CAS No. : 2098191-53-6

MCE 站：Zotatifin

产品活性：Zotatifin (eFT226) 是一种有效，选择性和耐受性良好的 eIF4A 抑制剂。Zotatifin 可促进 eIF4A 与 5'-UTRs 中具有识别基序的特定 mRNA 序列结合 (IC₅₀=2 nM)，并干扰 eIF4F 起始复合物的组装。Zotatifin 表现出强效的抗病毒效果，通过抑制 SARS-CoV-2 NP protein 生物合成，从而有效减少病毒传染性 (IC₉₀=37 nM)。Zotatifin 诱导细胞凋亡 (apoptosis)。

研究领域：Cell Cycle/DNA Damage  |  Anti-infection  |  Apoptosis

作用靶点：Eukaryotic Initiation Factor (eIF)  |  SARS-CoV  |  Apoptosis

In Vitro: Zotatifin induces the formation of a stable ternary complex [eIF4A-RNA-eFT226]. Zotatifin increases the residence time for eIF4A1 binds to an AGAGAG RNA surface, the K_d values are 0.021 μM and 8.0 μM, respectively for eFT226 presence or absence.
Zotatifin inhibits in vitro translation as a sequence-dependent manner, the IC₅₀ values are 1.5 nM, 13.8 nM, 92.5 nM, and 217.5 nM, respectively in an MDA-MB-231 cell line with transiently transfected AGAGAG, GGCGGC, CCGCCG and CAACAA 5’-UTRs-containing sequences.
Zotatifin (0.0001 μM-1 μM; 72 hours) inhibits tumor cells growth as a dose-dependent manner. It shows a potent anti-proliferative activity (GI₅₀<15 nM) in MDA-MB-231 tumor cells, but eIF4A1 F163L mutation rescues eFT226 anti-proliferative activity.
Zotatifin (0.0001 μM-1 μM; 72 hours) inhibits tumor cell growth, exhibits GI₅₀ values for TMD8, SU-DHL-2, HBL1, Pfeiffer, SU-DHL-6, SU-DHL-10, VAL, Carnaval, U2973, Ramos, Jeko1, Mino, and Rec-1 cells are 4.1 nM, 3 nM, 5.6 nM, 3.7 nM, 5.3 nM, 7.3 nM, 6.6 nM, 4.4 nM, 4.2 nM, 4.6 nM, 7.9 nM, 11.2 nM and 11.8 nM, respectively.
Zotatifin (30 μM-100 μM; 3 or 24 hours) results in translational regulation of oncogenic protein, decreases MYC,CCND3,BCL2 and MCL1 protein expression as a time- and dose-dependent manner.
The anti-viral activity of Zotatifin is demonstrated by various assays: such as TCID50 assay, Plaque assay, NP-staining assay, et al.
Zotatifin (10 nM, 100 nM, 200 nM, 500 nM, 2 μM, 10 μM; 1 or 2 hours pre-treatment before virus isolates) decreases the detection of the viral NP protein and reduces viral infectivity in a concentration-dependent matter in Vero E6 cells cells infected with SARS-CoV-2 isolates.

In Vivo: Zotatifin (intravenous injection; 1 mg/kg; 14-22 days) decreases tumor volume, inhibits the TMD8 xenograft-bearing, HBL1 xenograft-bearing, Pfeiffer xenograft-bearing, SU-DHL-6 xenograft-bearing, SU-DHL-10 xenograft-bearing and Ramos-bearing animals’tumor growth as percentage of 97%, 87%, 70%, 83%, 37% and 75%, respectively.
Zotatifin (intravenous injection; 0.001 mg/kg-1 mg/kg; 15 days) inhibits the growth of B-cell lymphoma xenografts and is well-tolerated against B-cell lymphoma xenograft models in vivo.

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