Name: JPH203
Brand: TargetMol
SKU: TQ0081
Price: 297 CNY
Availability: InStock
Rating: 5 (10 reviews)

规格

价格

库存

数量

1 mg

¥ 297

In stock

2 mg

¥ 442

In stock

5 mg

¥ 727

In stock

10 mg

¥ 1,090

In stock

25 mg

¥ 1,950

In stock

50 mg

¥ 2,930

In stock

100 mg

¥ 4,560

In stock

200 mg

¥ 6,380

In stock

产品介绍

生物活性

产品描述	JPH203 (KYT-0353) is a potent and specific inhibitor of L-type amino acid transporter protein 1 (LAT-1). JPH203 inhibits cellular uptake of leucine, inhibits cell proliferation, induces apoptosis, and possesses anti-inflammatory and anti-tumor activities.
靶点活性	HT29 cells:4.1 μM, LAT1:0.14 μM, SAOS-2 cells:4.09-0.09 mM, LAT1 (S2-hLAT1 cells):0.14 µM, L-Leucine:0.06 μM
体外活性	方法：HT-29、S2-LAT1 和 S2-LAT2 细胞用含 14C-leucine 和 JPH203 (0.01-10 µM) 的培养基孵育 1.0 min，使用 scintillation counter 计数细胞裂解物的放射性。结果：JPH203 以浓度依赖的方式抑制 S2-hLAT1 细胞对 14C-leucine 的摄取，IC50 为 0.14 µM。JPH203 几乎不抑制 S2-hL 细胞对 14C-leucine 的摄取，因此具有高的体外 hLAT1 抑制选择性。[1] 方法：人骨肉瘤细胞 Saos2 和人成骨细胞 FOB 用 JPH203 (0.01-30 mM) 处理 1-4 天，使用 MTT Assay 检测细胞活力。结果：JPH203 以剂量和时间依赖的方式有效抑制 Saos2 细胞中的细胞增殖。JPH203 仅轻微抑制 FOB 细胞的增殖。[2]
体内活性	方法：为检测体内抗肿瘤活性，将 JPH203 (6.5-25 mg/kg) 静脉注射给携带人结直肠癌肿瘤 HT-29 的 nude 小鼠，每天一次，持续十四天。结果：JPH203 对肿瘤生长具有剂量依赖性抑制作用。6.3、12.5 和 25.0 mg/kg 时的最大抑制率分别为 58.2% (第 42 天)、65.9% (第 30 天) 和 77.2% (第 38 天）。[1] 方法：为检测体内抗肿瘤活性，将 JPH203 (50 mg/kg in SBECD) 腹腔注射给富含基质的 CRC 小鼠模型，每天一次，持续十四天。结果：JPH203 治疗显著减少了肿瘤大小和转移，基于 RNA 测序的通路分析表明，不仅肿瘤生长和氨基酸代谢通路，而且基质激活相关通路都受到抑制。[3]
细胞实验	Growth inhibition is evaluated by the MTT assay method. Namely, cell suspensions (1 × 10^4 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].
动物实验	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), JPH203 is 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].
别名	KYT-0353

化学信息

分子量	472.32
分子式	C₂₃H₁₉Cl₂N₃O₄
CAS No.	1037592-40-7
Smiles	N[C@@H](Cc1cc(Cl)c(OCc2cc(N)cc3nc(oc23)-c2ccccc2)c(Cl)c1)C(O)=O
密度	1.458 g/cm3 (Predicted)
颜色	Yellow
物理性状	Solid

储存&溶解度

存储

store under nitrogen,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

DMSO: 237.5 mg/mL (502.84 mM), Sonication is recommended.

5%TFA: 2.31 mg/mL (4.89 mM), Heating to 50℃ is recommended.

体内实验配方

5% DMSO+40% PEG300+5% Tween 80+50% Saline: 5 mg/mL (10.59 mM), Solution.

请按顺序添加溶剂，在添加下一种溶剂之前，尽可能使溶液澄清。如有必要，可通过加热、超声、涡旋处理进行溶解。工作液建议现配现用。以上配方仅供参考，体内配方并不是绝对的，请根据不同情况进行调整。

溶液配制表

5%TFA/DMSO

	1mg	5mg	10mg	50mg
1 mM	2.1172 mL	10.5860 mL	21.1721 mL	105.8604 mL

DMSO

	1mg	5mg	10mg	50mg
5 mM	0.4234 mL	2.1172 mL	4.2344 mL	21.1721 mL
10 mM	0.2117 mL	1.0586 mL	2.1172 mL	10.5860 mL
20 mM	0.1059 mL	0.5293 mL	1.0586 mL	5.2930 mL
50 mM	0.0423 mL	0.2117 mL	0.4234 mL	2.1172 mL
100 mM	0.0212 mL	0.1059 mL	0.2117 mL	1.0586 mL

体内实验配液计算器