KYT 0353

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Cat.No. 5026 - KYT 0353 | C23H19Cl2N3O4.2HCl | CAS No. 1597402-27-1
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)
Datasheet
Citations
Reviews
Literature (1)

Biological Activity

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

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 Data

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

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

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References

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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