LAT1-IN-1 (Synonyms: BCH)
LAT1-IN-1 (BCH) 是 L 型氨基酸轉(zhuǎn)運(yùn)蛋白 1 (LAT1) 的選擇性競爭性抑制劑，可xian著抑制細(xì)胞對氨基酸的攝取和 mTOR 磷酸化，從而抑制ai細(xì)胞生長并誘導(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：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)
H2O : 41.67 mg/mL (268.51 mM; Need ultrasonic)
DMSO : < 1 mg/mL (insoluble or slightly soluble)
| 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(chǔ)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(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?jiān)?6 個(gè)月內(nèi)使用，-20°C 儲(chǔ)存時(shí)，請?jiān)?1 個(gè)月內(nèi)使用。
以下溶解方案都請先按照 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(xiàn)
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