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PROTAC B-Raf degrader 1
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。
PROTAC B-Raf degrader 1图片
CAS NO:2364367-27-9

PROTAC B-Raf degrader 1 (compound 2) 是基于Cereblon配体的一种B-RafPROTAC。有抗肿瘤活性。
生物活性

PROTACB-Raf degrader 1 (compound 2) is a proteolysis targeting chimera (PROTAC) for the degradation ofB-Rafbased onCereblonligand with anti-cancer activity[1].

IC50& Target[1]

B-Raf

 

体外研究
(In Vitro)

The IC50values of PROTAC B-Raf degrader 1 (compound 2) towards MCF-7, MDA-MB-231, HepG2, LO2 and B16 cells are 2.7 μM, 21.21 μM, 18.70 μM, 41.11μM and 22.68 μM, respectively[1].
PROTAC B-Raf degrader 1 (5 or 10 μM) can accelerate the degradation of B-Raf by recruiting ubiquitin-proteasome system, and further affects the expression of Mcl-1, a downstream protein of B-Raf[1].
MCF-7 cells achieve an apoptosis rate of 76.70% (64.00% early apoptosis, 12.70% late apoptosis) after 24 h incubation of PROTAC B-Raf degrader 1 with the concentration of 20 μM[1].
PROTAC B-Raf degrader 1 arrests cell cycle at the G2/M phase[1].

Cell Cytotoxicity Assay[1]

Cell Line:Human MCF-7 breast cancer cell line, MDA-MB-231 breast cancer cells, human HepG2 hepatoma cells, human normal LO2 liver cells, B16 cells.
Concentration:0-200 μM.
Incubation Time:72 hours.
Result:The IC50values are 2.7 μM, 21.21 μM, 18.70 μM, 41.11μM and 22.68 μM in MCF-7, MDA-MB-231, HepG2, LO2 and B16 cells, respectively.

Western Blot Analysis[1]

Cell Line:Human MCF-7 breast cancer cell line.
Concentration:5 or 10 μM.
Incubation Time:24 hours.
Result:Effectively induced the degradation of B-Raf and impacted the expression of Mcl-1.

Apoptosis Analysis[1]

Cell Line:Human MCF-7 breast cancer cell line.
Concentration:2.7-20 μM.
Incubation Time:24 hours.
Result:Achieved an apoptosis rate of 76.70% (64.00% early apoptosis, 12.70% late apoptosis) after 24 h incubation with the concentration of 20 μM.

Cell Cycle Analysis[1]

Cell Line:Human MCF-7 breast cancer cell line.
Concentration:20 μM.
Incubation Time:24 hours.
Result:1.94% cells were arrested at G1 phase, 8.20% at S phase, and 89.86% at G2/M phase.
分子量

763.77

性状

Solid

Formula

C36H37N5O12S

CAS 号

2364367-27-9

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

-20°C, stored under nitrogen

*In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

溶解性数据
In Vitro: 

DMSO : 25 mg/mL(32.73 mM;Need ultrasonic)

配制储备液
浓度溶剂体积质量1 mg5 mg10 mg
1 mM1.3093 mL6.5465 mL13.0929 mL
5 mM0.2619 mL1.3093 mL2.6186 mL
10 mM0.1309 mL0.6546 mL1.3093 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 (stored under nitrogen)。-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 (3.27 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.27 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 (3.27 mM); Clear solution

    此方案可获得 ≥ 2.5 mg/mL (3.27 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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