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Raptinal
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
Raptinal图片
CAS NO:1176-09-6
包装与价格:
包装价格(元)
10 mM * 1 mL in DMSO电议
5mg电议
10mg电议
50mg电议
100mg电议

产品介绍
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].

IC50& Target[1]

Caspase 3

 

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.
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.
分子量

386.44

性状

Solid

Formula

C28H18O2

CAS 号

1176-09-6

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder-20°C3 years
4°C2 years
In solvent-80°C6 months
-20°C1 month
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
浓度溶剂体积质量1 mg5 mg10 mg
1 mM2.5877 mL12.9386 mL25.8772 mL
5 mM0.5175 mL2.5877 mL5.1754 mL
10 mM0.2588 mL1.2939 mL2.5877 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。

    将 0.9 g 氯化钠,完全溶解于 100 mL ddH2O 中,得到澄清透明的生理盐水溶液
  • 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。