MT 63-78 是一种有效的直接AMPK激活剂，EC50为 25 μM。M 63-78 还诱导细胞有丝分裂阻滞和细胞凋亡 (apoptosis)。MT 63-78 通过抑制脂肪生成和mTORC1途径来阻止前列腺癌的生长。MT 63-78 具有抗肿瘤作用。
| 生物活性 | MT 63-78 is a specific and potent directAMPKactivator with anEC50of 25 μM. MT 63–78 also induces cell mitotic arrest andapoptosis. MT 63-78 blocks prostatecancergrowth by inhibiting the lipogenesis andmTORC1pathways. MT 63-78 has antitumor effects[1]. |
| IC50& Target[1] | |
体外研究
(In Vitro) | MT 63-78 (0-50 μM; 4 days; LNCaP and PC3 cells) treatment shows a dose-dependent decrease in cell number, and concomitant to the activation of AMPK signaling[1].
MT 63-78 (25 μM; 24 hours; LNCaP and CRPC cells) treatment induces a significant enrichement in the G2/M population[1].
MT 63-78 (0-50 μM; 24 hours; LNCaP, PC3, C4-4, C4-2B, CL1and 22RV1cells) treatment induces reduction of anti-apoptotic Mcl-1 in concert with accumulation of the pro-apoptotic BH3-only protein Puma[1].
MT 63-78 (0-50 μM; 30 minutes; LNCaP and PC3 cells) treatment shows a dose-dependent phosphorylation of the two major AMPK targets Acetyl-CoA Carboxylase (ACC) on Ser79 and of Raptor on Ser792. And also increases Thr172 phosphorylation on the AMPK α subunit[1].
Cell Viability Assay[1] | Cell Line: | LNCaP and PC3 cells | | Concentration: | 0 μM, 1 μM, 5 μM, 10 μM, 25 μM, 50 μM | | Incubation Time: | 4 days | | Result: | A dose-dependent decrease in cell number, concomitant to the activation of AMPK signaling was observed. |
Cell Cycle Analysis[1] | Cell Line: | LNCaP and CRPC cells | | Concentration: | 25 μM | | Incubation Time: | 24 hours | | Result: | Induced a significant enrichement in the G2/M population in both androgen sensitive and CRPC cell models. |
Apoptosis Analysis[1] | Cell Line: | LNCaP, PC3, C4-4, C4-2B, CL1and 22RV1cells | | Concentration: | 0 μM, 10 μM, 25 μM, 50 μM | | Incubation Time: | 24 hours | | Result: | Induced reduction of anti-apoptotic Mcl-1 in concert with accumulation of the pro-apoptotic BH3-only protein Puma in all PCa cells. |
Western Blot Analysis[1] | Cell Line: | LNCaP and PC3 cells | | Concentration: | 0 μM, 0.25 μM, 0.5 μM, 1 μM, 5 μM, 25 μM, 50 μM | | Incubation Time: | 30 minutes | | Result: | Observed a dose-dependent phosphorylation of the two major AMPK targets Acetyl-CoA Carboxylase (ACC) on Ser79 and of Raptor on Ser792. A corresponding increase in Thr172 phosphorylation on the AMPK α subunit was also observed. |
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体内研究
(In Vivo) | MT 63-78 (30 mg/kg; intraperitoneal injection; daily; for 14 days; C57 BL/6 male mice) treatment leads to a 33% inhibition of tumor growth[1].
| Animal Model: | C57 BL/6 male mice bearing LNCaP tumors[1] | | Dosage: | 30 mg/kg | | Administration: | Intraperitoneal injection; daily; for 14 days | | Result: | Led to a 33% inhibition of tumor growth. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, protect from light *In solvent : -80°C, 6 months; -20°C, 1 month (protect from light) |
| 溶解性数据 | In Vitro: DMSO : 125 mg/mL(383.02 mM;Need ultrasonic) 配制储备液 | 1 mM | 3.0642 mL | 15.3210 mL | 30.6419 mL | | 5 mM | 0.6128 mL | 3.0642 mL | 6.1284 mL | | 10 mM | 0.3064 mL | 1.5321 mL | 3.0642 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℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 储存时，请在 1 个月内使用。 In Vivo: 请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照In Vitro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. 请依序添加每种溶剂： 10% DMSO 40%PEG300 5%Tween-80 45% saline Solubility: ≥ 2.08 mg/mL (6.37 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (6.37 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.08 mg/mL (6.37 mM); Clear solution
此方案可获得 ≥ 2.08 mg/mL (6.37 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 900 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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