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KYT 0353 New
Potent and selective inhibitor of L-type amino acid transporter 1 (LAT1) (IC50 = 60 nM for 14C-leucine uptake in H-29 cells). Also suppreses 14C-leucine uptake in renal proximal tubule cells expressing LAT1 (IC50 = 140 nM). Displays ~500-fold selectivity for LAT1 over LAT2. Reduces cell viability and induces apoptosis in YD-38 oral cancer cells. Arrests growth in several tumor cell lines. Exhibits growth inhibitory effects on HT-29 cells in vivo.
|Storage||Store at -20°C|
The technical data provided above is for guidance only. For batch specific data refer to the Certificate of Analysis.
Tocris products are intended for laboratory research use only, unless stated otherwise.
|Solvent||Max Conc. mg/mL||Max Conc. mM|
Preparing Stock Solutions
The following data is based on the product molecular weight 545.24. Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.83 mL||9.17 mL||18.34 mL|
|5 mM||0.37 mL||1.83 mL||3.67 mL|
|10 mM||0.18 mL||0.92 mL||1.83 mL|
|50 mM||0.04 mL||0.18 mL||0.37 mL|
References are publications that support the biological activity of the product.
Toyoshima et al (2013) Investigation of the role of transporters on the hepatic elimination of an LAT1 selective inhibitor JPH203. J.Pharm.Sci. 102 3228 PMID: 23712732
Cormerais et al (2016) Genetic disruption of the multifunctional CD98/LAT1 complex demonstrates the key role of essential amino acid transport in the control of mTORC1 and tumor growth. Cancer Res. 2016 4481 PMID: 27302165
Otsuki et al (2017) Prostate cancer cells in different androgen receptor status employ different leucine transporters. Prostate 77 222 PMID: 27696482
Oda et al (2010) L-type amino acid transporter 1 inhibitors inhibit tumor cell growth. Cancer Sci. 101 173 PMID: 19900191
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Keywords: KYT 0353, KYT 0353 supplier, KYT0353, Selective, inhibitor, L-type, amino, acid, transporter, 1, LAT1, potent, JPH, 203, Other, Ion, Pumps/Transporters, 5026, Tocris Bioscience
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