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PROTAC B-Raf degrader 1
PROTAC B-Raf degrader 1
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货号：A1148709
PROTAC B-Raf degrader 2 is a PROTAC targeting on B-Raf, consist of B-Raf ligand RGS linked to CRBN ligand Pomalidomide.
PROTAC B-Raf degrader 1 化学结构
PROTAC B-Raf degrader 1 3D分子结构
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PROTAC B-Raf degrader 1 纯度/质量文件 产品仅供科研
货号：A1148709
标准纯度：
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产品说明书
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PROTAC B-Raf degrader 1 质控信息
Encorafenib
✔
99%+
GDC-0879
++++
99%+
SB-590885
++++
99%+
RAF265
99%+
Dabrafenib
++++
B-Raf, IC50: 5.2 nM
B-Raf (V600E), IC50: 0.7 nM
+++
98%
Lifirafenib
++++
++
BRAF(V600E), IC50: 23 nM
BRAF WT, IC50: 32 nM
+++
C-RAF (Y340/341D), IC50: 7 nM
EGFR
98%
ZM 336372
+
99%+
NVP-BHG 712
+
99%+
CCT196969
+
++
Src
98%
Vemurafenib
++
B-Raf, IC50: 100 nM
B-Raf (V600E), IC50: 31 nM
+
98+%
PLX4720
++
B-Raf, IC50: 160 nM
B-Raf (V600E), IC50: 13 nM
+++
C-Raf-1 (Y340D/Y341D), IC50: 6.7 nM
BRK
99+%
GW 5074
+++
99%+
Avutometinib
+++
BRAF V600E, IC50: 8.2 nM
BRAF, IC50: 19 nM
+
98%
LY3009120
++++
BRAF(V600E), IC50: 5.8 nM
BRAF WT, IC50: 15 nM
++++
99%+
Agerafenib
++
B-Raf (V600E), Kd: 14 nM
B-Raf, Kd: 36 nM
+
RET
99%+
TAK-632
+++
++++
99%+
AZ 628
+
B-Raf, IC50: 105 nM
B-Raf (V600E), IC50: 34 nM
++
99%
PLX7904
✔
98+%
Sorafenib
++
B-Raf, IC50: 22 nM
B-Raf (V599E), IC50: 38 nM
++++
++++
99%
Tovorafenib
✔
99%+
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1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多，抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用，但抑制强度暂时没有相关数据。
PROTAC B-Raf degrader 1 生物活性
描述
PROTAC B-Raf degrader 2 is a PROTAC targeting on B-Raf, consist of B-Raf ligand RGS linked to CRBN ligand Pomalidomide. PROTAC B-Raf degrader 2 led to a significant degradation of B-Raf at concentration of both 5μM and 10μM in MCF-7 cells post 24h, accompanied with a downregulation of its downstream Mcl-1. PROTAC B-Raf degrader 2 at concentration of 20μM achieved an apoptosis rate of 76.70% (64.00% early apoptosis, 12.70% late apoptosis) and arrested cell cycle at the same G2/M phase in MCF-7 cells post 24h. PROTAC B-Raf degrader 2 exhibited cytotoxicity to MCF-7, MDA-MB-231, HepG2, LO2 and B16 cell lines with IC50 values of 2.70, 21.21, 18.70, 41.11 and 22.68μM, respectively, post 72-hour treatment[1]
PROTAC B-Raf degrader 1 参考文献
PROTAC B-Raf degrader 1 实验方案
计算器
摩尔计算器
总药量计算器
工作液计算器
存储液制备
1mg
5mg
10mg
1 mM
5 mM
10 mM
1.31mL
0.26mL
0.13mL
6.55mL
1.31mL
0.65mL
13.09mL
2.62mL
1.31mL
PROTAC B-Raf degrader 1 技术信息
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