Raptinal|cas:1176-09-6|西域试剂

Raptinal,98.60%

产品编号：Bellancom-121320| CAS NO：1176-09-6| 分子式：C₂₈H₁₈O₂| 分子量：386.44

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货号	包装	价格	库存与货期	购买量	操作
Bellancom-121320		￥1600.00	杭州北京（现货）
Bellancom-121320		￥2300.00	杭州北京（现货）

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Raptinal

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 activates caspase-3, initiates intrinsic pathway caspase-dependent apoptosis. Raptinal is able to rapidly induce cancer cell death by directly activating the effector caspase-3, bypassing the activation of initiator caspase-8 and caspase-9.

体外研究

H. pylori infection-induced apoptosis resistance in gastric epithelial cells triggered by Raptinal.
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.
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

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

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.
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.
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	C57BL/6 and BALB/c female mice (6-8 weeks old) bearing the B16-F10 model or 4T1 models
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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	C57BL/6 and BALB/c female mice (6-8 weeks old) bearing the B16-F10 model or 4T1 models
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.

体内研究

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	C57BL/6 and BALB/c female mice (6-8 weeks old) bearing the B16-F10 model or 4T1 models
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.

性状

Solid

溶解性数据

In Vitro:

DMSO : 20 mg/mL (51.75 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 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。