Zotatifin - CAS:2098191-53-6

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Zotatifin (Synonyms:eFT226)

目录号 : KM3403 CAS No. : 2098191-53-6 纯度 : 98%

Data Sheet 产品使用指南

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)。

规格	价格	是否有货
1mg		In-stock
2mg		In-stock
5mg		In-stock
10mg	询价	In-stock
50mg	询价	In-stock

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生物活性

Zotatifin (eFT226) is a potent, selective, and well-tolerated eIF4A inhibitor. Zotatifin promotes eIF4A binding to specific mRNA sequences with recognition motifs in the 5’-UTRs (IC₅₀=2 nM) and interferes with the assembly of the eIF4F initiation complex. Zotatifin shows robust antiviral effects, it effectively reduces viral infectivity by inhibiting SARS-CoV-2 NP protein biogenesis (IC₉₀=37 nM). Zotatifin induces cell apoptosis.

体外研究

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.

Cell Viability Assay

Cell Line:	MDA-MB-231 tumor cells
Concentration:	0.0001 μM, 0.001 μM, 0.01 μM, 0.1 μM, 1 μM
Incubation Time:	72 hours
Result:	Inhibited cell growth with a GI₅₀ of 15 nM, and F163L mutant rescued anti-proliferative effects.

Cell Proliferation Assay

Cell Line:	DLBCL-ABC; DLBCL-GCB; Burkitt; and MCL tumor type cells
Concentration:	0.0001 μM, 0.001 μM, 0.01 μM, 0.1 μM, 1 μM
Incubation Time:	72 hours
Result:	Inhibited cell growth with GI₅₀ values ranging from 3 nM to 20 nM.

Cell Proliferation Assay

Cell Line:	TMD8 and Pfeiffer DLBCL tumor cells
Concentration:	30 μM; 100 μM
Incubation Time:	3 or 24 hours
Result:	Decreased MYC, CCND3, Bcl2,and MCL1 protein levels.

体内研究

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.

Animal Model:	B-cell lymphoma xenograft model
Dosage:	0.001 mg/kg; 0.1 mg/kg; 1 mg/kg
Administration:	Intravenous injection; 15 days
Result:	Showed efficacy in B-cell lymphoma xenograft models.

分子式

C₂₈H₂₉N₃O₅

分子量

487.55

CAS号

2098191-53-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

溶解性数据

In Vitro:

DMSO : 200 mg/mL (410.21 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.0511 mL	10.2554 mL	20.5107 mL
5 mM	0.4102 mL	2.0511 mL	4.1021 mL
10 mM	0.2051 mL	1.0255 mL	2.0511 mL

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 5 mg/mL (10.26 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (10.26 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 5 mg/mL (10.26 mM); Clear solution

此方案可获得 ≥ 5 mg/mL (10.26 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 50.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。