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化驗
≥98% (HPLC)
形狀
powder
儲存條件
desiccated
顏色
white to beige
溶解度
DMSO: 15 mg/mL, clear
儲存溫度
2-8°C
SMILES 字串
O=C(O)[C@@H](N)CC1=CC(Cl)=C(OCC2=CC(N)=CC3=C2OC(C4=CC=CC=C4)=N3)C(Cl)=C1
生化/生理作用
JPH203(KYT-0353)可选择性抑制HT-29和表达S2 近端肾小管蛋白的LAT1细胞培养物中的LAT1依赖性L-亮氨酸的摄取和生长,但对于表达S2细胞的人LAT2无效(二者的 IC50/GI50 分别为 0.06/4.1、0.14/16.4 和 >10/>1000 μM。通过静脉注射(从d0到d13,剂量6.3-25 mg / kg / 天)给药时,JPH203在体内有效抑制HT-29分化肿瘤在小鼠体内生长。
儲存類別代碼
13 - Non Combustible Solids
水污染物質分類(WGK)
WGK 3
閃點(°F)
Not applicable
閃點(°C)
Not applicable
Cancer science, 101(1), 173-179 (2009-11-11)
Most tumor cell membranes overexpress L-type amino acid transporter 1, while normal cell membranes contain l-type amino acid transporter 2; both are Na(+)-independent amino acid transporters. Therefore, compounds that selectively inhibit L-type amino acid transporter 1 offer researchers with a
Drug metabolism and pharmacokinetics, 27(1), 155-161 (2011-09-15)
Many primary human tumors and tumor cell lines highly express human L-type amino acid transporter 1 (hLAT1); cancerous cells in vivo are strongly linked to LAT1 expression. Synthetic chemistry and in vitro screening efforts have afforded a variety of novel
JCI insight, 8(7) (2023-03-03)
Hypothalamic neurons regulate body homeostasis by sensing and integrating changes in the levels of key hormones and primary nutrients (amino acids, glucose, and lipids). However, the molecular mechanisms that enable hypothalamic neurons to detect primary nutrients remain elusive. Here, we
Journal of pharmaceutical sciences, 102(9), 3228-3238 (2013-05-29)
JPH203 has been developed as an anticancer drug that inhibits L-type amino acid transporter 1-mediated essential amino acid uptake into tumor cells. This study sought to elucidate which drug transporters may be involved in JPH203 hepatic elimination, and to estimate
International journal of molecular sciences, 22(20) (2021-10-24)
The l-type amino acid transporter 1 (LAT1) is a membranous transporter that transports neutral amino acids for cells and is dysregulated in various types of cancer. Here, we first observed increased LAT1 expression in pemetrexed-resistant non-small cell lung cancer (NSCLC)
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