KYT 0353

Product Description

KYT 0353 is a 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.

Solubility

Preparing Stock Solutions for KYT 0353

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 all affect the solvent volumes required to prepare stock solutions.

Select a batch to recalculate based on the batch molecular weight:

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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

Calculators

Background References

References are publications that support the biological activity of the product.

• Oda L-type amino acid transporter 1 inhibitors inhibit tumor cell growth. Cancer Sci. 2010 PMID: 19900191
• Cormerais 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 PMID: 27302165
• Otsuki Prostate cancer cells in different androgen receptor status employ different leucine transporters. Prostate 2017 PMID: 27696482
• Toyoshima Investigation of the role of transporters on the hepatic elimination of an LAT1 selective inhibitor JPH203. J.Pharm.Sci. 2013 PMID: 23712732