Raptinal 直接激活caspase-3,可启动 caspase 依赖性的细胞凋亡内源性途径。Raptinal 能够通过直接激活效应 caspase-3来快速诱导癌细胞死亡,绕过启动子 caspase-8 和 caspase-9的激活。
生物活性 | Raptinal, a agent that directly activatescaspase-3, initiates intrinsic pathway caspase-dependentapoptosis. Raptinal is able to rapidly inducecancercell death by directly activating the effector caspase-3, bypassing the activation of initiatorcaspase-8and caspase-9[1][2]. |
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体外研究 (In Vitro) | H. pylori infection-induced apoptosis resistance in gastric epithelial cells triggered by Raptinal[1]. Treatment with 10 μM of Raptinal for 2 h induces the cleavage of pro-caspase-3 into it’s active form in human gastric cancer cell lines AGS, MKN28, MKN45[1]. Raptinal initiates intrinsic pathway caspase-dependent apoptosis within minutes in multiple cell lines. Raptinal induces death against various cancer and non-cancerous cell lines with 24 hour IC50 values between 0.7-3.4 μM, indicating activity across a wide variety of cell lines[2].
Cell Viability Assay[2] Cell Line: | Human Lymphoma U-937, SKW 6.4, or Jurkat cell lines | Concentration: | 0.7-3.4 μM | Incubation Time: | 24 hours | Result: | The IC50 values of Raptinal against U-937, SKW 6.4, or Jurkat cell lines were 1.1±0.1, 0.7±0.3, 2.7±0.9 μM, respectively. |
Western Blot Analysis[1] Cell Line: | Human gastric cancer cell lines AGS, MKN28, MKN45 | Concentration: | 10 μM | Incubation Time: | 2 hours | Result: | Induced apoptosis by activating caspase-3 within 30 min at a concentration of 10 μM. Treatment with 10 μM of Raptinal for 2 h induced the cleavage of pro-caspase-3 into it’s active form in all three cell lines. |
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体内研究 (In Vivo) | Raptinal is an unusually rapid inducer of caspase-dependent apoptosis in multiple cell lines and in vivo systems[1]. Raptinal (20 mg/kg; administered intraperitoneally; once daily for 3 consecutive days for B16-F10 and 4 consecutive days for 4T1 models) exerts anticancer activity in vivo[2]. C57BL/6 mice are administered intravenous Raptinal across a range of dosages as a one-time injection. When administered intravenously at a dosage of 37.5 mg/kg, the peak plasma concentration and elimination half-life of Raptinal are 54.4±0.9 μg/mL and 92.1±5.8 minutes, respectively. Single-dose intravenous Raptinal is well tolerated across a wide dose range (15-60 mg/kg) and does not cause hematologic toxicity as assessed 7 days post-administration[2].
Animal Model: | C57BL/6 and BALB/c female mice (6-8 weeks old) bearing the B16-F10 model or 4T1 models[2] | Dosage: | 20 mg/kg | Administration: | Administered intraperitoneally; once daily for 3 consecutive days for B16-F10 and 4 consecutive days for 4T1 models | Result: | Retard tumor volume and tumor mass by 60% relative to controls in the B16-F10 model. Similar efficacy was observed for the 4T1 murine breast cancer tumor model with 50% growth inhibition after treatment. |
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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 |
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溶解性数据 | In Vitro: DMSO : 20 mg/mL(51.75 mM;ultrasonic and warming and heat to 60℃) 配制储备液 1 mM | 2.5877 mL | 12.9386 mL | 25.8772 mL | 5 mM | 0.5175 mL | 2.5877 mL | 5.1754 mL | 10 mM | 0.2588 mL | 1.2939 mL | 2.5877 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 (6.47 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.47 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%corn oil Solubility: ≥ 2.5 mg/mL (6.47 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (6.47 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。
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