SML1892
JPH203 盐酸盐
≥98% (HPLC)
别名:
(S)-2-氨基-3-(4-((5-氨基-2-苯基苯并[d]恶唑-7-基]甲氧基)-3,5-二氯苯基]丙酸 盐酸盐, JPH 203 盐酸盐, KYT 0353 盐酸盐, KYT-0353 盐酸盐, KYT0353 盐酸盐, O-(5-氨基-2-苯基苯并恶唑-7-基)甲基-3,5-二氯-L-酪氨酸 盐酸盐, O-[(5-氨基-2-苯基-7-苯并恶唑基)甲基]-3,5-二氯-L-酪氨酸 二盐酸盐, SCHEMBL17360639 盐酸盐
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关于此项目
经验公式（希尔记法）:
C23H19Cl2N3O4 · xHCl
化学文摘社编号:
分子量:
472.32 (free base basis)
UNSPSC Code:
12352200
MDL number:
SMILES string
O=C(O)[C@@H](N)CC1=CC(Cl)=C(OCC2=CC(N)=CC3=C2OC(C4=CC=CC=C4)=N3)C(Cl)=C1
assay
≥98% (HPLC)
form
powder
storage condition
desiccated
color
white to beige
solubility
DMSO: 15 mg/mL, clear
storage temp.
2-8°C
Biochem/physiol Actions
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。
一种选择性LAT1抑制剂，可在体外和体内阻断LAT1依赖性L-Leu的摄取和肿瘤生长。
存储类别
13 - Non Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
法规信息
新产品
此项目有
Gyujin Park et al.
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
Junko Toyoshima et al.
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
Koji Oda et al.
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
Michael F Wempe et al.
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
Yi-Heng Liu et al.
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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