CAS號	20448-79-7	產(chǎn)地	國產(chǎn)
規(guī)格	50mg	級別	化工級
證書	ISO系列證書

LAT1-IN-1 (Synonyms: BCH)

LAT1-IN-1 (BCH) 是 L 型氨基酸轉(zhuǎn)運蛋白 1 (LAT1) 的選擇性競爭性抑制劑，可xian著抑制細胞對氨基酸的攝取和 mTOR 磷酸化，從而抑制ai細胞生長并誘導(dǎo)細胞凋亡。

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]

體外研究(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].

MCE 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.

體內(nèi)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].

MCE 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

性狀：

Solid

Formula：C₈H₁₃NO₂

CAS 號：20448-79-7

運輸條件：Room temperature in continental US; may vary elsewhere.

儲存方式

4°C, sealed storage, away from moisture

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

溶解性數(shù)據(jù)

In Vitro:

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

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

配制儲備液

濃度溶劑體積質(zhì)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

請根據(jù)產(chǎn)品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復(fù)凍融造成的產(chǎn)品失效。
儲備液的保存方式和期限：-80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-80°C 儲存時，請在 6 個月內(nèi)使用，-20°C 儲存時，請在 1 個月內(nèi)使用。

In Vivo:

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：

——為保證實驗結(jié)果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當保存；體內(nèi)實驗的工作液，建議您現(xiàn)用現(xiàn)配，當天使用；以下溶劑前顯示的百
分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

1.

請依序添加每種溶劑： PBS
Solubility: 12.5 mg/mL (80.55 mM); Clear solution; Need ultrasonic and warming and heat to 60°C

參考文獻

[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.  [Content Brief]
[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).  [Content Brief]
[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.  [Content Brief]
注：產(chǎn)品僅用于科研