详情描述
LAT1-IN-1 (BCH) is a selective and competitive inhibitor of large neutral amino acid transporter 1 (LAT1) significantly inhibit cellular uptake of amino acids and mTOR phosphorylation, which induces the suppression of cancer growth and apoptosis.
Product information
CAS Number: 20448-79-7
Molecular Weight: 155.19
Formula: C8H13NO2
Synonym:
BCH
Chemical Name: 2-aminobicyclo[2.2.1]heptane-2-carboxylic acid
Smiles: NC1(CC2CC1CC2)C(O)=O
InChiKey: MPUVBVXDFRDIPT-UHFFFAOYSA-N
InChi: InChI=1S/C8H13NO2/c9-8(7(10)11)4-5-1-2-6(8)3-5/h5-6H,1-4,9H2,(H,10,11)
Technical Data
Appearance: Solid Power
Purity: ≥98% (or refer to the Certificate of Analysis)
Solubility: H2O : 12.5 mg/mL (80.55 mM; Need ultrasonic) DMSO : < 1 mg/mL (insoluble or slightly soluble)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis
Storage Condition: Dry, dark and -20 oC for 1 year or refer to the Certificate of Analysis.
Shelf Life: ≥360 days if stored properly.
Stock Solution Storage: 0 - 4 oC for 1 month or refer to the Certificate of Analysis.
Drug Formulation: To be determined
HS Tariff Code: 382200
How to use
In Vitro:
LAT1-IN-1 (1-100 mM; 3 days; KYSE30 and KYSE150 esophageal cancer cells) treatment suppresses cell proliferation in a dose-dependent manner. LAT1-IN-1 (30 mM; 24 and 48 hours; KYSE30 and KYSE150 cells) treatment significantly increases cell population in the G0/G1 phase in both KYSE30 and KYSE150 cells, indicating that LAT1-IN-1 induces cell cycle arrest at G1 phase. LAT1-IN-1 (30 mM; 0-24 hours; KYSE30 and KYSE150 cells) treatment decreases phosphorylation of 4E-BP1 and p70S6K at 30 minutes and the decrease is continued for 24 hours. The amount of mTOR, 4E-BP1, and p70S6K proteins is slightly decreased.
In Vivo:
LAT1-IN-1 (200 mg/kg; intravenous injection; daily; for 14 days; male BALB/c nude mice) treatment significantly delays tumor growth and decreases glucose metabolism, indicating that LAT1 inhibition potentially suppresses esophageal cancer growth in vivo.
References:
- Ohshima Y, et al. Efficacy of system l amino acid transporter 1 inhibition as a therapeutic target in esophageal squamous cell carcinoma. Cancer Sci. 2016 Oct;107(10):1499-1505.
- Singh N, et al. Discovery of Potent Inhibitors for the Large Neutral Amino Acid Transporter 1 (LAT1) by Structure-Based Methods. Int J Mol Sci. 2018 Dec 21;20(1).
- Wang Q, et al. L-type amino acid transport and cancer: targeting the mTORC1 pathway to inhibit neoplasia. Am J Cancer Res. 2015 Mar 15;5(4):1281-94. eCollection 2015.
Products are for research use only. Not for human use.