2. Membrane Transporter/Ion Channel
  3. Amino acid Transporter
  4. LAT1-IN-2 hydrochloride

LAT1-IN-2 hydrochloride 是一种口服有效的抗癌剂，也是 LAT1 底物与微管蛋白结合剂。LAT1-IN-2 hydrochloride 依赖 LAT1 实现细胞摄取，并通过结合微管蛋白的秋水仙碱位点破坏微管形成，同时诱导肌动蛋白解聚使细胞形态变为球形。LAT1-IN-2 hydrochloride 能有效抑制异种移植小鼠的肿瘤生长。LAT1-IN-2 hydrochloride 比 Etoposide (HY-13629) 的肿瘤组织分布率更高、在重要器官中的分布率更低，且耐受性更好。LAT1-IN-2 hydrochloride 已被应用于食管癌的相关研究中。

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LAT1-IN-2 hydrochloride

LAT1-IN-2 hydrochloride Chemical Structure

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LAT1-IN-2 hydrochloride 相关抗体

Top Publications Citing Use of Products

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

LAT1-IN-2 hydrochloride is an orally active anticancer agent, as well as a LAT1 substrate and tubulin-binding agent. LAT1-IN-2 hydrochloride relies on LAT1 for cellular uptake, disrupts microtubule formation by binding to the colchicine site of tubulin, and induces actin depolymerization to transform cells into a spherical shape. LAT1-IN-2 hydrochloride effectively inhibits tumor growth in xenograft mice. Compared with Etoposide (HY-13629), LAT1-IN-2 hydrochloride shows higher distribution in tumor tissues, lower distribution in major organs, and better tolerability. LAT1-IN-2 hydrochloride has been applied in studies related to esophageal cancer[1].

体外研究
(In Vitro)

LAT1-IN-2 hydrochloride (B11) (0.01-50 μM; 72 h) 可强效抑制 A549、Eca109、MM.1S 和 NUGC-4 细胞的增殖，其中对 Eca109 细胞的活性最高 (IC50=0.048 μM)[1]。
LAT1-IN-2 hydrochloride (0.1-10 μM; 24 h) 以浓度依赖的方式破坏 Eca109 细胞的肌动蛋白细胞骨架，诱导肌动蛋白解聚并使细胞呈现球形形态[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

LAT1-IN-2 hydrochloride 相关抗体:

Cell Proliferation Assay[1]

Cell Line: human lung carcinoma A549 cells, human esophageal carcinoma Eca109 cells, human multiple myeloma MM.1S cells, human gastric carcinoma NUGC-4 cells
Concentration: 0.01 μM, 0.05 μM, 0.1 μM, 0.5 μM, 1 μM, 10 μM, 50 μM
Incubation Time: 72 h
Result: Exhibited potent antiproliferative activity across all four cell lines, with IC50 values of 0.233 μM (A549), 0.048 μM (Eca109), 0.899 μM (MM.1S), and 0.252 μM (NUGC-4).
Showed significantly different IC50 values from the positive control etoposide for all cell lines except MM.1S.

Immunofluorescence[1]

Cell Line: human esophageal carcinoma Eca109 cells
Concentration: 0.1 μM, 10 μM
Incubation Time: 24 h
Result: Caused significant disruption of the actin cytoskeleton at 0.1 μM, with actin bundles largely absent and reduced F-actin distribution, resulting in spherical cell morphology.
Induced more intense cytoskeletal damage, membrane deformation, and nuclear deformation at 10 μM.
体内研究
(In Vivo)

LAT1-IN-2 hydrochloride (B11) (100-400 mg/kg；灌胃；每日；14 天) 在 ICR 小鼠中的最大灌胃耐受剂量为 400 mg/kg，14 天内未观察到不良反应[1]。
LAT1-IN-2 hydrochloride (20-40 mg/kg；口服；每日一次；连续 14 天) 可剂量依赖性地抑制 BALB/c 裸鼠的食管肿瘤生长[1]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: BALB/c nude mice with Esophageal cancer (female, 5 weeks old)[1]
Dosage: 20 mg/kg; 40 mg/kg
Administration: p.o.; daily; 14 days
Result: Achieved a tumor growth inhibition (TGI) of 41.50% based on tumor weight at 20 mg/kg.
Achieved a TGI of 64.58% based on tumor weight at 40 mg/kg.
Kept all animals in good health with no clinical behavioral or pathological differences observed during treatment.
分子量

594.01

Formula

C28H32ClNO11
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

LAT1-IN-2 hydrochloride 相关分类

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

LAT1-IN-2Amino acid Transporter氨基酸转运蛋白Eca109A549colchicine binding sitetubulinmicrotubule293T-LAT1 cellsactin cytoskeletonxenograft miceLAT1esophageal cancerInhibitorinhibitorinhibit

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