1037592-40-7
JPH203
CAS: 1037592-40-7
Molecular Formula: C23H19Cl2N3O4
1037592-40-7 - Names and Identifiers
1037592-40-7 - Physico-chemical Properties
| Molecular Formula | C23H19Cl2N3O4 |
| Molar Mass | 472.32 |
| Density | 1.458±0.06 g/cm3(Predicted) |
| Melting Point | 191 - 193°C |
| Boling Point | 672.0±55.0 °C(Predicted) |
| Solubility | DMF (Slightly, Heated), DMSO (Slightly) |
| Appearance | Solid |
| Color | Pale Yellow |
| pKa | 2.14±0.30(Predicted) |
| Storage Condition | -20°C Freezer |
| In vitro study | In YD-38 and NHOKs cells, JPH203 completely or slightly inhibited L-Leucine uptake with an IC50 of 0.79 μm and greater than 100 μm, respectively. JPH203 inhibited the growth of HT-29 cells with an IC50 of 4.1 μm; The IC50 value (0.06 μm) that inhibited the absorption of L-Leucine did not inhibit the growth of HT-29 cells. JPH203 is able to activate mitochondria-dependent apoptotic signaling pathways by up-regulating the activated forms of pro-apoptotic factors such as Bad, Bax, Bak and caspase-9, and down-regulating anti-apoptotic factors such as Bcl-2, Bcl-xL. JPH203 can distinguish the relative abundance of LAT1 and LAT2, which has high selectivity for lat1. JPH203 is metabolically stable in mouse, rat, dog, monkey and human liver microsomes. JPH203 can induce cell cycle arrest in G2/M and G0/G1 phase, and reduce the number of S phase cells, while changing the expression of cyclin D1, CDK4 and CDK6 in cell cycle progression. |
| In vivo study | In the KKU-213 cholangiocarcinoma cell xenograft model, intravenous injection of 12.5 mg/kg and 25 mg/kg of JPH203 per day significantly transplanted tumor growth, without causing significant changes in animal body weight, do not cause changes in the morphology of internal organs. Therefore, JPH203 has anti-tumor activity in a model carrying human CCA cell xenografts without significant toxic side effects. |
1037592-40-7 - Reference Information
| biological activity | JPH203 (KYT-0353, JPH-203SBECD) is a selective L-type amino acid transporter 1 inhibitor, which has significant inhibitory effects on leucine absorption and cell growth in HT-29, YD-38 and leukemia cells, with IC50 of 0.06 μM and 4.1 μM respectively. |
| target | TargetValue LAT1 (Cell-free say) |
| Target | Value |
| in vitro study | in YD-38 and NHOKs cells, JPH203 can completely or slightly inhibit L-Leucine absorption with IC50 of 0.79 μM and more than 100 μM respectively. JPH203 inhibits the growth of HT-29 cells with IC50 of 4.1 μM. However, the IC50 value (0.06 μM) that can inhibit L-Leucine absorption cannot inhibit the growth of HT-29 cells. JPH203 can activate mitochondrial-dependent apoptosis signaling pathways by up-regulating activated forms of pro-apoptotic factors such as Bad, Bax, Bak and caspase-9, and down-regulating anti-apoptotic factors such as Bcl-2 and Bcl-xL. JPH203 can distinguish the relative abundance of LAT1 and LAT2, and it has high selectivity for LAT1. JPH203 is metabolically stable in liver microsomes of mice, rats, dogs, monkeys and humans. JPH203 can induce cell cycle arrest in G2/M and G0/G1 phases, and reduce the number of S phase cells, while changing the expression of cyclin D1, CDK4 and CDK6 in cell cycle progression. |
| in vivo study | in the xenograft model of KKU-213 bile duct cell type liver cancer cells, daily intravenous injection of 12.5 mg/kg and 25 mg/kg of JPH203 can significantly transplant its tumor growth without causing obvious changes in animal weight, does not cause changes in the tissue morphology of internal organs. Therefore, JPH203 has anti-tumor activity and no obvious toxic and side effects in the model of transplanted tumor carrying human CCA cells. |
Last Update：2024-04-09 21:01:54
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