化合物FRAX597 T6014
品牌 | 厂商性质 | 产地 | 货期 |
---|---|---|---|
TargetMol | 生产商 | 美国 | 现货 |
性能特点
生化试剂,可用于动物细胞实验
规格 | CAS号 | 价格 | 操作 |
---|---|---|---|
2 mg | 1286739-19-2 | ¥413.00 | 询底价 |
5 mg | 1286739-19-2 | ¥828.00 | 询底价 |
1 mg | 1286739-19-2 | ¥289.00 | 询底价 |
10 mg | 1286739-19-2 | ¥1,390.00 | 询底价 |
1 mL | 1286739-19-2 | ¥987.00 | 询底价 |
50 mg | 1286739-19-2 | ¥3,570.00 | 询底价 |
500 mg | 1286739-19-2 | ¥10,800.00 | 询底价 |
25 mg | 1286739-19-2 | ¥2,390.00 | 询底价 |
100 mg | 1286739-19-2 | ¥5,160.00 | 询底价 |
Product Introduction
Bioactivity
英文名: FRAX597
描述: FRAX597 是一种有效的 ATP 竞争性 I 组 PAK 抑制剂,作用于PAK1、2和3,IC50分别为 8、13 和 19 nM。
细胞实验: 30,000 cells/well are plated in 12-well dishes in triplicate. Cell growth media with or without FRAX597 is replaced daily. At indicated time points, cells from individual wells are trypsinized and counted using a Coulter counter.(Only for Reference)
激酶实验: Determination of Enzyme IC50 Values: IC50 values are determined using a 10 concentration point, non-radioactive, functional assay that employs a fluorescence-based, coupled-enzyme format, according to the manufacturer's protocol (Z'-LYTE@biochemical assay). Kinase selectivity is determined using both the Z'-LYTE@ and Adapta@ kinase assay format.
体外活性: 负荷Nf2-/-SC4 Schwann细胞的NOD/SCID小鼠中,每天口服 FRAX597(100 mg/kg),对肿瘤生长有明显的抑制作用.患有原位脑膜瘤的SCID小鼠中,每天口服 FRAX597(90 mg/kg),明显抑制肿瘤生长.在KrasG12D小鼠中,每天口服 FRAX597(90 mg/kg),处理引起肿瘤消退以及Erk与Akt活性损失.
体内活性: FRAX597抗野生型PAK1(IC50=48 nM),而抗V342F PAK1突变型(IC50>3 μM)和V342Y PAK1突变型(IC50>2 μM)。FRAX597(100 nM )对YES1 (87%),RET (82%),CSF1R (91%),TEK (87%),PAK1 (82%),和PAK2 (93%)表现出明显的抑制作用。
存储条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year
溶解度: DMSO : 11.2 mg/mL (20 mM)
关键字: p21 activated kinases | FRAX 597 | Inhibitor | inhibit | PAK | FRAX-597 | FRAX597
相关产品: FRAX486 HCL(1232030-35-1 free base) | PF-3758309 hydrochloride | PAK4-IN-3 | ZMF-23 | FRAX1036 | KPT9274 | AZ13705339 | G-5555 | Fingolimod hydrochloride | PIR 3.5
相关库: Anti-Aging Compound Library | Bioactive Compounds Library Max | Inhibitor Library | Kinase Inhibitor Library | Cytoskeletal Signaling Pathway Compound Library | Target-Focused Phenotypic Screening Library | Bioactive Compound Library
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注:该产品未在中华人民共和国食品药品监督管理部门申请医疗器械注册和备案,不可用于临床诊断或治疗等相关用途