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BCH

L型氨基酸转运蛋白LAT1抑制剂,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。

目录号: PC12394 纯度: ≥98%

CAS No. :20448-79-7

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中文名称	BCH
中文别名	2-氨基-2-降莰烷羧酸;2-氨基-2-去甲菠烷羧酸;2-氨基双环[2.2.1]庚烷-2-羧酸
英文名称	BCH
英文别名	Bicyclo[2.2.1]heptane-2-carboxylicacid, 2-amino-;2-AMINO-2-NORBORNANE- CARBOXYLIC ACID;3-aminobicyclo[2.2.1]heptane-3-carboxylic acid;BCH;2-aminonorbornane-2-carboxylic acid;b-BCH;2-Amino-bicyclo[2.2.1]heptane-2-carboxylic acid;LAT1-IN-1
Cas No.	20448-79-7
分子式	C₈NO₂H₁₃
分子量	155.19
包装储存	4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)

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.

性状

Solid

IC50 & Target[1][2]

LAT1

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.
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.
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.

Medlife has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

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

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

Western Blot Analysis

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.

Medlife 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
Dosage:	200 mg/kg
Administration:	Intravenous injection; daily; for 14 days
Result:	Significantly delayed tumor growth and decreased glucose metabolism.

运输条件

Room temperature or refrigerated transportation.

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)

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. [Information]

[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). [Information]

[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. [Information]

溶解度数据

体外研究:

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

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

配制储备溶液

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

产品不同，其溶解度不同。建议根据产品选择合适的溶剂配制储备溶液；配成溶液后，建议分装保存，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，建议在 6 个月内使用，-20°C 储存时，建议在 1 个月内使用。

体内研究:

建议根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都建议先按照 体外研究 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

建议依照次序添加每种溶剂： PBS
Solubility: 12.5 mg/mL (80.55 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

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产品使用指南

Data Sheet

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

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