首页工具

ARQ 069

产品编号 T10372 CAS 1314021-57-2

ARQ 069 (3.8-60 μM; for 2 hours) reduces the degree of phosphorylation of FGFR (predominantly FGFR2) in a concentration-dependent manner, without decreasing β-actin. ARQ 069 shows an affinity for FGFR2 of 5.2 μM. ARQ 069 inhibits FGFR phosphorylation in Kato III cells (IC50: 9.7 μM). ARQ 069 targets the inactive forms of FGFR1 and FGFR2 kinases and inhibits their enzymatic activity. When ARQ 069 is preincubated with either phosphorylated FGFR1 or FGFR2, the potency of ARQ 069 in inhibiting Pyk2 phosphorylation is markedly reduced, with IC50 values determined to be greater than 30 and 24.8 μM for FGFR1 and FGFR2, respectively. ARQ 069 exhibits at least a 20-fold preference for binding to the unphosphorylated, inactive forms of FGFR1 and FGFR2.

TargetMol的所有产品和服务仅用于科学研究，不能被用于人体，我们也不向个人提供产品和服务。

ARQ 069, CAS 1314021-57-2

规格	价格/CNY	货期
25 mg	￥ 10,600	6-8周
50 mg	￥ 13,800	6-8周
100 mg	￥ 17,500	6-8周

大包装超大折扣，点击咨询

该分子属于定制产品。陶术拥有优秀的合成团队，经验和能力，可以为您提供高性价比的产品。但由于客观因素，研发中会存在小概率合成不成功的情况，还请理解，如您有任何问题，欢迎咨询，我们将竭诚为您服务。

更多批次查询请联系客服

生物活性

化学信息

存储 & 溶解度

参考文献

产品描述	ARQ 069 (3.8-60 μM; for 2 hours) reduces the degree of phosphorylation of FGFR (predominantly FGFR2) in a concentration-dependent manner, without decreasing β-actin. ARQ 069 shows an affinity for FGFR2 of 5.2 μM. ARQ 069 inhibits FGFR phosphorylation in Kato III cells (IC50: 9.7 μM). ARQ 069 targets the inactive forms of FGFR1 and FGFR2 kinases and inhibits their enzymatic activity. When ARQ 069 is preincubated with either phosphorylated FGFR1 or FGFR2, the potency of ARQ 069 in inhibiting Pyk2 phosphorylation is markedly reduced, with IC50 values determined to be greater than 30 and 24.8 μM for FGFR1 and FGFR2, respectively. ARQ 069 exhibits at least a 20-fold preference for binding to the unphosphorylated, inactive forms of FGFR1 and FGFR2.
靶点活性	FGFR1 unphosphorylated:0.84 μM, FGFR1 autophosphorylation:2.8 μM, FGFR2 autophosphorylation:1.9 μM, FGFR2 unphosphorylated:1.23 μM
体外活性	ARQ 069 (3.8-60 μM; for 2 hours) reduces the degree of phosphorylation of FGFR (predominantly FGFR2) in a concentration-dependent manner, without decreasing β-actin[1]. ARQ 069 shows an affinity for FGFR2 of 5.2 μM[1]. ARQ 069 inhibits FGFR phosphorylation in Kato III cells with an IC50 of 9.7 μM[1]. ARQ 069 targets the inactive forms of FGFR1 and FGFR2 kinases and inhibits their enzymatic activity. When ARQ 069 is preincubated with either phosphorylated FGFR1 or FGFR2, the potency of ARQ 069 in inhibiting Pyk2 phosphorylation is markedly reduced, with IC50 values determined to be greater than 30 and 24.8 μM for FGFR1 and FGFR2, respectively. ARQ 069 exhibits at least a 20-fold preference for binding to the unphosphorylated, inactive forms of FGFR1 and FGFR2[1]. ARQ 068 is the R-enantiomer, and ARQ 069 is the S-enantiomer[1].

分子量	273.33
分子式	C18H15N3
CAS No.	1314021-57-2

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

计算器

摩尔浓度计算器

稀释计算器

配液计算器

分子量计算器

质量

浓度

容积

分子量

浓度 (起始)

容积 (起始)

浓度 (终)

容积 (终)

溶液体积

质量

配液浓度

参考文献

1. Eathiraj S, et al. A novel mode of protein kinase inhibition exploiting hydrophobic motifs of autoinhibited kinases: discovery of ATP-independent inhibitors of fibroblast growth factor receptor. J Biol Chem. 2011 Jun 10;286(23):20677-87.

剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

剂量

mg/kg

每只动物体重

给药体积

μL

动物数量

第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

% DMSO+

% +