ARQ 069

发表于由

上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

ARQ 069 

ARQ 069 是 ARQ 523 的类似物，以对映体特异的方式抑制 FGFR 活性。ARQ 069 靶向非磷酸化，非活性形式的 FGFR1/FGFR2 激酶，IC50 分别为 0.84 μM 和 1.23 μM。ARQ 069 通过非 ATP 竞争的方式抑制 FGFR1/FGFR2 自磷酸化，IC50 分别为 2.8 μM 和 1.9 μM。

ARQ 069

ARQ 069 Chemical Structure

CAS No. : 1314021-57-2

规格 是否有货
100 mg   询价  
250 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

生物活性

ARQ 069, an analog of ARQ 523, inhibits FGFR in an enantiospecific manner. ARQ 069 targets the unphosphorylated, inactive forms of FGFR1/FGFR2 kinases (IC50s of 0.84 μM and 1.23 μM, respectively). ARQ 069 inhibits FGFR1/FGFR2 autophosphorylation (IC50s of 2.8 and 1.9 μM, respectively) through a mechanism in a non-ATP competitive dependent manner[1].

IC50 & Target

unphosphorylated FGFR1

0.84 μM (IC50)

unphosphorylated FGFR2

1.23 μM (IC50)

FGFR1 autophosphorylation

2.8 μM (IC50)

FGFR2 autophosphorylation

1.9 μM (IC50)

体外研究
(In Vitro)

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].

Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only.

Western Blot Analysis[1]

Cell Line: Kato III human gastric carcinoma cells
Concentration: 3.8, 7.5, 15, 30, 60 μM
Incubation Time: For 2 hours
Result: Reduced the degree of phosphorylation of FGFR (predominantly FGFR2) in a concentration-dependent manner, without decreasing β-actin.

分子量

273.33

Formula

C18H15N3
CAS 号

1314021-57-2
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
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.

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务