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About This Item
Empirical Formula (Hill Notation):
C23H19Cl2N3O4 · xHCl
CAS Number:
Molecular Weight:
472.32 (free base basis)
UNSPSC Code:
12352200
MDL number:
Assay:
≥98% (HPLC)
Form:
powder
Storage condition:
desiccated
assay
≥98% (HPLC)
form
powder
storage condition
desiccated
color
white to beige
solubility
DMSO: 15 mg/mL, clear
storage temp.
2-8°C
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
Biochem/physiol Actions
A selective LAT1 inhibitor that blocks LAT1-dependent L-Leu uptake and cancer growth both in vitro and in vivo.
JPH203 (KYT-0353) selectively inhibits L-type amino acid transporter LAT1-dependent L-leucine uptake and growth in HT-29 and human LAT1-expressing S2 murine renal proximal tubule cell cultures, but not human LAT2-expressing S2 cells (IC50/GI50 = 0.06/4.1, 0.14/16.4, and >10/>1000 μM, respectively). When administered via intravenous injection (6.3-25 mg/kg/d from d0 to d13), JPH203 effectively inhibits HT-29-derived tumor growth in mice in vivo.
Storage Class
13 - Non Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
Regulatory Information
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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
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
Global Trade Item Number
| SKU | GTIN |
|---|---|
| SML1892-25MG | 04061833266267 |
| SML1892-5MG | 04061833266274 |