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Submit ReviewKYT 0353
说明： Potent and selective inhibitor of L-type amino acid transporter 1 (LAT1); active in vivo
别名： JPH 203
化学名： O-[(5-Amino-2-phenyl-7-benzoxazolyl)methyl]-3,5-dichloro-L-tyrosine dihydrochloride
纯度： ≥96% (HPLC)
生物活性 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.
技术数据 for KYT 0353
| 分子量 | 545.24 |
| 公式 | C23H19Cl2N3O4.2HCl |
| 储存 | Store at -20°C |
| 纯度 | ≥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 |
上方提供的技术数据仅供参考。批次相关数据请参见分析证书。
Tocris products are intended for laboratory research use only, unless stated otherwise.
溶解性数据 for KYT 0353
| 溶剂 | 最高浓度 mg/mL | 最高浓度 mM | |
|---|---|---|---|
| 溶解性 | |||
| DMSO | 54.52 | 100 |
制备储备液 for KYT 0353
以下数据基于产品分子量 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.
| 浓度/溶剂体积/质量 | 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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产品说明书 for KYT 0353
参考文献 for KYT 0353
参考文献是支持产品生物活性的出版物。
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
If you know of a relevant reference for KYT 0353, please let us know.
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关键词: 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
1 篇 KYT 0353 的引用文献
引用文献是使用了 Tocris 产品的出版物。 KYT 0353 的部分引用包括：
Brenda A et al (2021) The IMiD target CRBN determines HSP90 activity toward transmembrane proteins essential in multiple myeloma. Mol Cell 81 1170-1186.e10 PMID: 33571422
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