PROTAC B-Raf degrader 1 - CAS:2364367-27-9

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PROTAC B-Raf degrader 1

目录号 : KM10272 CAS No. : 2364367-27-9

Data Sheet 产品使用指南

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

规格	价格	是否有货
5mg		In-stock
10mg		In-stock
50mg	询价	In-stock
100mg	询价	In-stock

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Isoginkgetin In-stock
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生物活性

PROTAC B-Raf degrader 1 (compound 2) is a proteolysis targeting chimera (PROTAC) for the degradation of B-Raf based on Cereblon ligand with anti-cancer activity.

体外研究

The IC₅₀ values 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.
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.
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.
PROTAC B-Raf degrader 1 arrests cell cycle at the G2/M phase.

Cell Cytotoxicity Assay

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 IC₅₀ values 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

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

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

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

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 mg	5 mg	10 mg

1 mM	1.3093 mL	6.5465 mL	13.0929 mL
5 mM	0.2619 mL	1.3093 mL	2.6186 mL
10 mM	0.1309 mL	0.6546 mL	1.3093 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°C, 6 months; -20°C, 1 month (stored under nitrogen)。-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 (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。
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。