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

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.

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LAT1-IN-2 hydrochloride

LAT1-IN-2 hydrochloride Chemical Structure

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LAT1-IN-2 hydrochloride Related Antibodies

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Description

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].

In Vitro

LAT1-IN-2 hydrochloride (B11) (0.01-50 μM; 72 h) potently inhibits the proliferation of A549, Eca109, MM.1S, and NUGC-4 cells, with the highest activity against Eca109 cells (IC50 = 0.048 μM)[1].
LAT1-IN-2 hydrochloride (0.1-10 μM; 24 h) disrupts the actin cytoskeleton of Eca109 cells in a concentration-dependent manner, inducing actin depolymerization and spherical cell morphology[1].

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

LAT1-IN-2 hydrochloride Related Antibodies

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.
In Vivo

LAT1-IN-2 hydrochloride (B11) (100-400 mg/kg; i.g.; daily; 14 days) exhibits a maximum tolerated dose of 400 mg/kg in ICR mice via intragastric administration, with no observed adverse effects over 14 days[1].
LAT1-IN-2 hydrochloride (20-40 mg/kg; p.o.; daily; 14 days) dose-dependently inhibits esophageal tumor growth in BALB/c nude mice[1].

MedChemExpress (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.
Molecular Weight

594.01

Formula

C28H32ClNO11
SMILES

O=C(O)[C@@H](N)CCCC(O[C@@H]1[C@]2([H])[C@@](C(OC2)=O)([H])[C@H](C3=CC(OC)=C(OC)C(OC)=C3)C4=C1C=C5OCOC5=C4)=O.Cl
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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LAT1-IN-2 hydrochloride Related Classifications

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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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