LAT1-IN-1(Synonyms: BCH)

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LAT1-IN-1 (Synonyms: BCH) 纯度: ≥99.0%

LAT1-IN-1 (BCH) 是 L 型氨基酸转运蛋白 1 (LAT1) 的选择性竞争性抑制剂，可显著抑制细胞对氨基酸的摄取和 mTOR 磷酸化，从而抑制癌细胞生长并诱导细胞凋亡。

LAT1-IN-1(Synonyms: BCH)

LAT1-IN-1 Chemical Structure

CAS No. : 20448-79-7

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10 mM * 1 mL in Water ￥660 In-stock
50 mg ￥600 In-stock
100 mg ￥1000 In-stock
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500 mg   询价  

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LAT1-IN-1 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus
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  • Targeted Diversity Library

生物活性

LAT1-IN-1 (BCH) is a selective and competitive inhibitor of large neutral amino acid transporter 1 (LAT1) significantly inhibit cellular uptake of amino acids and mTOR phosphorylation, which induces the suppression of cancer growth and apoptosis[1][2][3].

IC50 & Target

LAT1[1]
体外研究
(In Vitro)

LAT1-IN-1 (1-100 mM; 3 days; KYSE30 and KYSE150 esophageal cancer cells) treatment suppresses cell proliferation in a dose-dependent manner[1].
LAT1-IN-1 (30 mM; 24 and 48 hours; KYSE30 and KYSE150 cells) treatment significantly increases cell population in the G0/G1 phase in both KYSE30 and KYSE150 cells, indicating that LAT1-IN-1 induces cell cycle arrest at G1 phase[1].
LAT1-IN-1 (30 mM; 0-24 hours; KYSE30 and KYSE150 cells) treatment decreases phosphorylation of 4E-BP1 and p70S6K at 30 minutes and the decrease is continued for 24 hours. The amount of mTOR, 4E-BP1, and p70S6K proteins is slightly decreased[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: KYSE30 and KYSE150 esophageal cancer cells
Concentration: 1 mM, 3 mM, 5 mM, 10 mM, 20 mM, 30 mM, 40 mM, 50 mM, or 100 mM
Incubation Time: 3 days
Result: Cell proliferation was suppressed in a dose-dependent manner.

Cell Cycle Analysis[1]

Cell Line: KYSE30 and KYSE150 cells
Concentration: 30 mM
Incubation Time: 24 and 48 hours
Result: Cell cycle arrest.

Western Blot Analysis[1]

Cell Line: KYSE30 and KYSE150 cells
Concentration: 30 mM
Incubation Time: 0 hour, 0.5 hour, 1 hour, 3 hours, 6 hours, 24 hours
Result: Phosphorylation of 4E-BP1 and p70S6K was decreased. The amount of mTOR, 4E-BP1, and p70S6K proteins was slightly decreased.

体内研究
(In Vivo)

LAT1-IN-1 (200 mg/kg; intravenous injection; daily; for 14 days; male BALB/c nude mice) treatment significantly delays tumor growth and decreases glucose metabolism, indicating that LAT1 inhibition potentially suppresses esophageal cancer growth in vivo[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Male BALB/c nude mice (5-week-old) with KYSE150 cells[1]
Dosage: 200 mg/kg
Administration: Intravenous injection; daily; for 14 days
Result: Significantly delayed tumor growth and decreased glucose metabolism.

分子量

155.19

Formula

C8H13NO2
CAS 号

20448-79-7
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, sealed storage, away from moisture

*In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
溶解性数据
In Vitro: 

H2O : 41.67 mg/mL (268.51 mM; Need ultrasonic)

DMSO : < 1 mg/mL (insoluble or slightly soluble)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 6.4437 mL 32.2186 mL 64.4371 mL
5 mM 1.2887 mL 6.4437 mL 12.8874 mL
10 mM 0.6444 mL 3.2219 mL 6.4437 mL

*

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, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-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。
参考文献

  • [1]. Ohshima Y, et al. Efficacy of system l amino acid transporter 1 inhibition as a therapeutic target in esophageal squamous cell carcinoma. Cancer Sci. 2016 Oct;107(10):1499-1505.

    [2]. Singh N, et al. Discovery of Potent Inhibitors for the Large Neutral Amino Acid Transporter 1 (LAT1) by Structure-Based Methods. Int J Mol Sci. 2018 Dec 21;20(1).

    [3]. Wang Q, et al. L-type amino acid transport and cancer: targeting the mTORC1 pathway to inhibit neoplasia. Am J Cancer Res. 2015 Mar 15;5(4):1281-94. eCollection 2015.

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