BRAF V600E/CRAF-IN-2

• 常用名: BRAF V600E/CRAF-IN-2
• 英文名: BRAF V600E/CRAF-IN-2
• CAS号: 2499499-62-4
• 分子量: 549.59
• 密度: N/A
• 沸点: N/A
• 分子式: C₃₀H₃₀F₃N₅O₂
• 熔点: N/A
• 闪点: N/A

BRAF V600E/CRAF-IN-2用途

BRAF V600E/CRAF-IN-2(化合物9c)是BRAF V600E/CRAF的有效抑制剂,IC50s分别为0.888和0.229μM。BRAF V600E/CRAF-IN-2触发HCT-116结肠癌细胞G0/G1期凋亡和细胞周期阻滞。BRAF V600E/CRAF-IN-2具有研究癌症疾病的潜力【1】。

BRAF V600E/CRAF-IN-2名称

• 英文名: BRAF V600E/CRAF-IN-2

BRAF V600E/CRAF-IN-2生物活性

• 描述: BRAF V600E/CRAF-IN-2(化合物9c)是BRAF V600E/CRAF的有效抑制剂,IC50s分别为0.888和0.229μM。BRAF V600E/CRAF-IN-2触发HCT-116结肠癌细胞G0/G1期凋亡和细胞周期阻滞。BRAF V600E/CRAF-IN-2具有研究癌症疾病的潜力【1】。
• 相关类别:
  研究领域 >> 癌症
  信号通路 >> MAPK/ERK信号通路 >> 拉夫
• 参考文献:

  [1]. El-Damasy AK,et al. 2-Anilinoquinoline based arylamides as broad spectrum anticancer agents with B-RAFV600E/C-RAF kinase inhibitory effects: Design, synthesis, in vitro cell-based and oncogenic kinase assessments. Eur J Med Chem. 2020 Dec 15;208:112756.

BRAF V600E/CRAF-IN-2物理化学性质

• 分子式: C₃₀H₃₀F₃N₅O₂
• 分子量: 549.59
• InChIKey: OTASYYGEHSXRJI-UHFFFAOYSA-N
• SMILES: CCN1CCN(c2cc(C(=O)Nc3cccc(Nc4ccc5c(OC)cccc5n4)c3)cc(C(F)(F)F)c2)CC1

BRAF V600E/CRAF-IN-2靶点实验

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实验名称：Selectivity ratio of IC50 for inhibition of human BRAF V600E mutant to IC50 for inhib... 来源：ChEMBL 靶标：N/A External Id：CHEMBL4711000

实验名称：Inhibition of human DDR1 at 10 uM using KKSRGDYMTMQIG as substrate in presence of [ga... 来源：ChEMBL 靶标：Epithelial discoidin domain-containing receptor 1 External Id：CHEMBL4710990

实验名称：Inhibition of human CRAF at 10 uM using MEK1 (K97R) as substrate in presence of [gamm... 来源：ChEMBL 靶标：RAF proto-oncogene serine/threonine-protein kinase External Id：CHEMBL4710991

实验名称：Inhibition of human BRAF at 10 uM using MEK1 (K97R) as substrate in presence of [gamm... 来源：ChEMBL 靶标：Serine/threonine-protein kinase B-raf External Id：CHEMBL4710988

实验名称：Inhibition of human BRAF V600E mutant at 10 uM using MEK1 (K97R) as substrate in pres... 来源：ChEMBL 靶标：Serine/threonine-protein kinase B-raf External Id：CHEMBL4710989

实验名称：Inhibition of human FMS at 10 uM using poly[Glu:Tyr] (4:1) as substrate in presence o... 来源：ChEMBL 靶标：Macrophage colony-stimulating factor 1 receptor External Id：CHEMBL4710994

实验名称：Growth inhibition of human LOX IMVI cells at 10 uM measured after 48 hrs by SRB assay... 来源：ChEMBL 靶标：LOX IMVI External Id：CHEMBL4710867

实验名称：Inhibition of human TRKA at 10 uM using poly[Glu:Tyr] (4:1) as substrate in presence ... 来源：ChEMBL 靶标：High affinity nerve growth factor receptor External Id：CHEMBL4710992

实验名称：Inhibition of human DDR2 at 10 uM using KKSRGDYMTMQIG as substrate in presence of [ga... 来源：ChEMBL 靶标：Discoidin domain-containing receptor 2 External Id：CHEMBL4710993

实验名称：Induction of apoptosis in human HCT-116 cells assessed as necrotic cells at 2.5 uM me... 来源：ChEMBL 靶标：HCT-116 External Id：CHEMBL4710982

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