KYT 0353

Name: KYT 0353
Brand: Tocris Bioscience
SKU: 5026

Tocris Bioscience, part of Bio-Techne | Catalog # 5026

Citations (5)

COA / SDS

Potent and selective inhibitor of L-type amino acid transporter 1 (LAT1); active in vivo

Key Product Details

Description:	Potent and selective inhibitor of L-type amino acid transporter 1 (LAT1); active in vivo
Alternative Names:	JPH 203
Chemical Name:	O-[(5-Amino-2-phenyl-7-benzoxazolyl)methyl]-3,5-dichloro-L-tyrosine dihydrochloride
Purity:	≥96% (HPLC)
Molecular Weight:	545.24

View Full Technical Details for KYT 0353

Technical Data
Citations

Biological Activity for KYT 0353

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.

Technical Data for KYT 0353

M. Wt	545.24
Formula	C₂₃H₁₉Cl₂N₃O₄.2HCl
Storage	Store at -20°C
Purity	≥96% (HPLC)
CAS Number	1597402-27-1
PubChem ID	122553374
InChi Key	MJSAOPNUSNNYQL-NTEVMMBTSA-N
Smiles	N[C@H](C(O)=O)CC1=CC(Cl)=C(C(Cl)=C1)OCC2=C3OC(C4=CC=CC=C4)=NC3=CC(N)=C2.Cl.Cl

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.

Solubility for KYT 0353

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
Solubility	DMSO	54.52	100

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 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

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References for KYT 0353

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