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LAT1-IN-1

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  • 型號(hào)

    HY-108540

  • 品牌

    MCE

  • 廠商性質(zhì)

    代理商

  • 所在地

    杭州市

規(guī)格

50mg 600元 10000支可售

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CAS號(hào) 20448-79-7 產(chǎn)地 國(guó)產(chǎn)
規(guī)格 50mg 級(jí)別 化工級(jí)
證書(shū) ISO系列證書(shū)
LAT1-IN-1 (BCH) 是 L 型氨基酸轉(zhuǎn)運(yùn)蛋白 1 (LAT1) 的選擇性競(jìng)爭(zhēng)性抑制劑,可較好抑制細(xì)胞對(duì)氨基酸的攝取和 mTOR 磷酸化,從而抑制ai細(xì)胞生長(zhǎng)并誘導(dǎo)細(xì)胞凋亡。

LAT1-IN-1  (Synonyms: BCH)

LAT1-IN-1 (BCH) 是 L 型氨基酸轉(zhuǎn)運(yùn)蛋白 1 (LAT1) 的選擇性競(jìng)爭(zhēng)性抑制劑,可xian著抑制細(xì)胞對(duì)氨基酸的攝取和 mTOR 磷酸化,從而抑制ai細(xì)胞生長(zhǎng)并誘導(dǎo)細(xì)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(hào):20448-79-7


運(yùn)輸條件:Room temperature in continental US; may vary elsewhere.


儲(chǔ)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(chǔ)備液
濃度溶劑體積質(zhì)量1 mg5 mg10 mg
1 mM6.4437 mL32.2186 mL64.4371 mL
5 mM1.2887 mL6.4437 mL12.8874 mL
10 mM0.6444 mL3.2219 mL6.4437 mL
*

請(qǐng)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(chǔ)備液;一旦配成溶液,請(qǐng)分裝保存,避免反復(fù)凍融造成的產(chǎn)品失效。
儲(chǔ)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(chǔ)存時(shí),請(qǐng)?jiān)?6 個(gè)月內(nèi)使用,-20°C 儲(chǔ)存時(shí),請(qǐng)?jiān)?1 個(gè)月內(nèi)使用。

In Vivo:

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

——為保證實(shí)驗(yàn)結(jié)果的可靠性,澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件,適當(dāng)保存;體內(nèi)實(shí)驗(yàn)的工作液,建議您現(xiàn)用現(xiàn)配,當(dāng)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(guò)程中出現(xiàn)沉淀、析出現(xiàn)象,可以通過(guò)加熱和/或超聲的方式助溶

  • 1.


    請(qǐng)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(xiàn)

  • [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


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