JPH203 Dihydrochloride
(Synonyms: KYT-0353) 目录号 : GC19400
An inhibitor of LAT1
Cas No.:1597402-27-1
Sample solution is provided at 25 µL, 10mM.
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JPH203 Dihydrochloride is a tyrosine analog, acts as a selective inhibitor of L-type amino acid transporter 1 (LAT1), and is used in cancer research.
JPH203 Dihydrochloride is a selective inhibitor of LAT1. JPH203 (KYT-0353) inhibits 14C-leucine uptake in S2-hLAT1 and HT-29 cells, with IC50s of 0.14 uM and 0.06 uM. JPH203 (3-1000 uM) exhibits concentration-dependent inhibitory effects on S2-hLAT1 cell growth with an IC50 of 16.4 uM. JPH203 also displays inhibitory activities against HT-29 cell growth, with an IC50 value of 4.1 uM[1]. JPH203 (0.001-100 uM) inhibits the 14C-leucine (1.0 uM) uptake in a concentration dependent way by the YD-38 cells with an IC50 value of 0.79 ± 0.06 uM. JPH203 slightly shows such effects in normal human oral keratinocytes (NHOKs). JPH203 (0.01-30 mM, 1-4 d) completely inhibits the proliferation of YD-38 cells in a dose- and time-dependent manner. However, JPH203 slightly inhibits the proliferation of NHOKs. JPH203 (30 mM) induces apoptosis of YD-38 cells. JPH203 (3 mM) also increases the level of cleaved PARP in activation of the caspases cascade[2]. JPH203 (30 mM) induces mitochondria-dependent apoptosis in Saos2 human osteosarcoma cells. JPH203 (0.001-100 uM) inhibits 14C-leucine (1.0 uM) uptake slightly in FOB cells with an IC50 value of 92.12 ± 10.71 uM, but potently exihibts such effects in Saos2 cells with an IC50 value of 1.31 ± 0.27 uM. JPH203 (0.01 to 30 mM, 1-4 d) potently inhibits cell proliferation in Saos2 cells in a dose- and time-dependent manner, with an IC50 of 4.09-0.09 mM, but slightly inhibits that of FOB cells, with an IC50 of 24.1-2.8 mM[3].
JPH203 (6.3, 12.5, and 25.0 mg/kg, i.v. for 14 days) exhibits dose-dependent inhibition on HT-29 tumor growth in nude mice[1].
References:
[1]. Oda K, et al. L-type amino acid transporter 1 inhibitors inhibit tumor cell growth. Cancer Sci. 2010 Jan;101(1):173-9.
[2]. Yun DW, et al. JPH203, an L-type amino acid transporter 1-selective compound, induces apoptosis of YD-38 human oral cancer cells. J Pharmacol Sci. 2014;124(2):208-17. Epub 2014 Feb 4.
[3]. Choi DW, et al. JPH203, a selective L-type amino acid transporter 1 inhibitor,Choi DW, et al. JPH203, a selective L-type amino acid transporter 1 inhibitor, induces mitochondria-dependent apoptosis in Saos2 human osteosarcoma cells. Korean J Physiol Pharmacol. 2017 Nov;21(6):599-607.
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Cell experiment: |
Growth inhibition is evaluated by the MTT assay method. Namely, cell suspensions (1 × 104 cells/mL) in a volume of 135 μL are placed into the wells of a flat-bottom 96-well microtiter plate, and incubated in the atmosphere of 5% CO2 at 37°C (24 h). Drug solutions (15 μL) at various concentrations are added and incubated (96 h) under the same conditions. Next, MTT (15 μL; 5 mg/mL) dissolved in PBS is added and incubated (4.0 h). The incubation medium containing MTT is aspirated off. Cells are mixed (5 min) with DMSO (200 μL) and optical density read (540 nm) using a microtiter plate reader Emax; subsequently, IC50 values are determined[1]. |
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Animal experiment: |
Human-derived nude mouse HT-29 tumor growth inhibition is evaluated. HT-29 tumor blocks are injected subcutaneously to the right flank of male nude mice. After tumor volumes reach 100 to 300 mm3, the mice are divided into groups (n = 6). On the day of grouping (day 0), test compounds (JPH203) are administered intravenously daily for 14 days at three different doses (6.3, 12.5, and 25.0 mg/kg). Tumor volumes and body weights are measured two or three times a week for 42 days. Tumor volumes are expressed relative to initial tumor volume (day 0). Growth inhibition ratios for each treatment group is obtained from the mean tumor volume of the treated group compared to that of the control group[1]. |
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References: [1]. Oda K, et al. L-type amino acid transporter 1 inhibitors inhibit tumor cell growth. Cancer Sci. 2010 Jan;101(1):173-9. |
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| Cas No. | 1597402-27-1 | SDF | |
| 别名 | KYT-0353 | ||
| Canonical SMILES | N[C@@H](CC1=CC(Cl)=C(C(Cl)=C1)OCC2=C(OC(C3=CC=CC=C3)=N4)C4=CC(N)=C2)C(O)=O.[H]Cl.[H]Cl | ||
| 分子式 | C23H21Cl4N3O4 | 分子量 | 545.24 |
| 溶解度 | DMSO : ≥ 105.5 mg/mL (193.49 mM; use within 2 hours); Do not use water to dissolve. | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 1.8341 mL | 9.1703 mL | 18.3405 mL |
| 5 mM | 0.3668 mL | 1.8341 mL | 3.6681 mL |
| 10 mM | 0.1834 mL | 0.917 mL | 1.8341 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >98.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet