IITZ-01 是一个具有抗肿瘤活性的、有效的亲溶酶体的自噬抑制剂,其对 PI3Kγ 的IC50值为 2.62 μM。
生物活性 | IITZ-01 is a potent lysosomotropicautophagyinhibitor with single-agent antitumor activity, with anIC50of 2.62 μM forPI3Kγ. |
IC50& Target | PI3Kγ 2.62 μM (IC50) | Autophagy |
|
体外研究 (In Vitro) | IITZ-01 (0-2 μM, 24 h) enhances autophagosomes formation as indicated by increased expression of LC3-II levels time- and dose-dependently in triple-negative breast cancer (TNBC) cell lines (MDA-MB-231 and MDA-MB-453). IITZ-01 also demonstrates potent autophagy inhibitory activity in other breast, lung, and colon cancer cells[1].
Western Blot Analysis[1] Cell Line: | Triple-negative breast cancer (TNBC) cell lines (MDA-MB-231 and MDA-MB-453). | Concentration: | 0-2 μM. | Incubation Time: | 24 hours. | Result: | Enhanced autophagosomes formation as indicated by increased expression of LC3-II levels. |
|
体内研究 (In Vivo) | IITZ-01 (45 mg/kg, i.p. every alternate day for 4 weeks) inhibits average breast tumor growth when compared with control from third day of treatment in triple-negative breast tumor models in mice[1].
Animal Model: | MDA-MB-231 (TNBC)/green fluorescent protein (GFP) orthotropic breast cancer xenografts were developed in CrTac:NCr-FoxnnuBALB/c female nude mice[1]. | Dosage: | 45 mg/kg. | Administration: | Intraperitoneal every alternate day for 4 weeks. | Result: | Inhibited average breast tumor growth when compared with control from third day of treatment. |
|
分子量 | |
性状 | |
Formula | |
CAS 号 | |
运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Powder | -20°C | 3 years | | 4°C | 2 years | In solvent | -80°C | 6 months | | -20°C | 1 month |
|
溶解性数据 | In Vitro: DMSO : 150 mg/mL(310.87 mM;Need ultrasonic) 配制储备液 1 mM | 2.0725 mL | 10.3625 mL | 20.7250 mL | 5 mM | 0.4145 mL | 2.0725 mL | 4.1450 mL | 10 mM | 0.2072 mL | 1.0362 mL | 2.0725 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。-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: ≥ 2.5 mg/mL (5.18 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.18 mM,饱和度未知) 的澄清溶液。 以 1 mL 工作液为例,取 100 μL 25.0 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: 2.5 mg/mL (5.18 mM); Suspended solution; Need ultrasonic
此方案可获得 2.5 mg/mL (5.18 mM) 的均匀悬浊液,悬浊液可用于口服和腹腔注射。 以 1 mL 工作液为例,取 100 μL 25.0 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。 3. 请依序添加每种溶剂: 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (5.18 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (5.18 mM,饱和度未知) 的澄清溶液,此方案不适用于实验周期在半个月以上的实验。 以 1 mL 工作液为例,取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中,混合均匀。 *以上所有助溶剂都可在本网站选购。
|