SYC-435

• 常用名: SYC-435
• 英文名: TC-E 5008
• CAS号: 50405-58-8
• 分子量: 215.248
• 密度: 1.3±0.1 g/cm3
• 沸点: 384.0±35.0 °C at 760 mmHg
• 分子式: C₁₃H₁₃NO₂
• 熔点: N/A
• 闪点: 186.0±25.9 °C

SYC-435用途

SYC-435(SYC435)是突变IDH1的有效抑制剂,在突变IDH1的异柠檬酸盐口袋处结合,对IDH1 R132H的Ki值为190nM,对IDH1 R132C的Ki值为120nM；SYC-435具有细胞活性并且能够显着降低表达IDH1 R132C的HT1080纤维肉瘤细胞系中的D-2-HG产生(IC50=2.4uM)。

SYC-435名称

• 英文名: SYC-435

SYC-435生物活性

• 描述: SYC-435(SYC435)是突变IDH1的有效抑制剂,在突变IDH1的异柠檬酸盐口袋处结合,对IDH1 R132H的Ki值为190nM,对IDH1 R132C的Ki值为120nM；SYC-435具有细胞活性并且能够显着降低表达IDH1 R132C的HT1080纤维肉瘤细胞系中的D-2-HG产生(IC50=2.4uM)。
• 参考文献: References 1. Liu Z, et al. J Med Chem. 2014 Oct 23;57(20):8307-18. 2. Ma T, et al. J Med Chem. 2018 Jun 18. doi: 10.1021/acs.jmedchem.8b00159. View Related Products by Target Isocitrate Dehydrogenase (IDH)

SYC-435物理化学性质

• 密度: 1.3±0.1 g/cm3
• 沸点: 384.0±35.0 °C at 760 mmHg
• 分子式: C₁₃H₁₃NO₂
• 分子量: 215.248
• 闪点: 186.0±25.9 °C
• 精确质量: 215.094635
• LogP: 2.18
• InChIKey: AVLZAVSZOAQKRC-UHFFFAOYSA-N
• SMILES: Cc1cc(Cc2ccccc2)n(O)c(=O)c1
• 蒸汽压: 0.0±0.9 mmHg at 25°C
• 折射率: 1.634

SYC-435靶点实验

查看更多实验

实验名称：Inhibition of recombinant IDH1 R132H mutant (unknown origin) expressed in Escherichia... 来源：ChEMBL 靶标：Isocitrate dehydrogenase [NADP] cytoplasmic External Id：CHEMBL5356485

实验名称：Selectivity ratio of Ki for wild type IDH1 (unknown origin) to Ki for recombinant IDH... 来源：ChEMBL 靶标：N/A External Id：CHEMBL2390490

实验名称：Inhibition of recombinant wildtype IDH1 (unknown origin) expressed in Escherichia col... 来源：ChEMBL 靶标：Isocitrate dehydrogenase [NADP] cytoplasmic External Id：CHEMBL5356484

实验名称：Apparent permeability of the compound across apical to basolateral side in human Caco... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5139995

实验名称：Efflux ratio of apparent permeability across basolateral to apical side over apical t... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5139996

实验名称：Half life in mouse liver microsomes at 2 uM in presence of NADPH by LC/MS/MS analysis 来源：ChEMBL 靶标：N/A External Id：CHEMBL5139993

实验名称：Half life in human liver microsomes at 2 uM in presence of NADPH by LC/MS/MS analysis 来源：ChEMBL 靶标：N/A External Id：CHEMBL5139994

实验名称：Selectivity ratio of Ki for wild type IDH1 (unknown origin) to Ki for recombinant IDH... 来源：ChEMBL 靶标：N/A External Id：CHEMBL2390487

实验名称：Cytotoxicity against human HepDES19 cells assessed as reduction in cell viability inc... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5139987

实验名称：Selectivity index, ratio of CC50 for cytotoxicity against African green monkey Vero c... 来源：ChEMBL 靶标：N/A External Id：CHEMBL5139988

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SYC-435英文别名

• 6-benzyl-1-hydroxy-4-methylpyridin-2(1H)-one
• 6-Benzyl-1-hydroxy-4-methyl-2(1H)-pyridinone
• SYC-435