1. MAPK/ERK Pathway
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PROTAC B-Raf degrader 1 

目录号: HY-111758
产品使用指南

PROTAC B-Raf degrader 1 (compound 2) 是基于PROTAC技术的一种 B-Raf 降解剂。有抗肿瘤活性。

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PROTAC B-Raf degrader 1 Chemical Structure

PROTAC B-Raf degrader 1 Chemical Structure

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Description

PROTAC B-Raf degrader 1 (compound 2) is a proteolysis targeting chimera (PROTAC) for the degradation of B-Raf. With anti-cancer activity[1].

IC50 & Target[1]

B-Raf

 

In Vitro

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[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 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[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.
References
Molecular Weight

763.77

Formula

C₃₆H₃₇N₅O₁₂S

SMILES

O=C(NC1=CC=CC(C(N2C(CC3)C(NC3=O)=O)=O)=C1C2=O)CNC(CNC4=CC(CS(=O)(/C=C/C5=C(OC)C=C(OC)C=C5OC)=O)=CC=C4OC)=O

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2

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产品名称:
PROTAC B-Raf degrader 1
目录号:
HY-111758
需求量:

PROTAC B-Raf degrader 1

Cat. No.: HY-111758