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FRAX1036
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
FRAX1036图片
CAS NO:1432908-05-8
包装:25mg
规格:98%
市场价:3663元
分子量:518.05

产品介绍
p21-activated kinase I (PAK1) inhibitor
CAS:1432908-05-8
分子式:C28H32ClN7O
分子量:518.05
纯度:98%
存储:Store at -20°C

Background:

IC50: N/A


FRAX1036 is a p21-activated kinase I (PAK1) inhibitor.


Breast cancer is a clinically and molecularly heterogeneous disease and plenty of genetic and epigenetic studies of breast tumors has revealed novel putative driver genes, such as p21-activated kinase (PAK)1. As a serine/threonine kinase downstream of small GTP-binding proteins including Rac1 and Cdc42, PAK1 is an critical component of growth factor signaling networks and cellular functions important to tumorigenesis.


In vitro: Previous study demonstrated that the administration of docetaxel with either FRAX1036 or PAK1 small interfering RNA oligonucleotides was able to alter signaling to cytoskeletal-associated proteins dramatically, such as stathmin, and also able to induce microtubule disorganization and cellular apoptosis. In addition, the live-cell imaging data showed that the duration of mitotic arrest mediated by docetaxel could be significantly reduced by the treatment of FRAX1036, which was associated with increased kinetics of apoptosis [1].


In vivo: In previous animal study, the untreated mice bearing KT21 transplants showed ventricular invasion, whereas Ben-Men grew at the injection site. Efficacy results found that the treatment with Frax1036 could lead to a slower tumor growth, with reduction in body mass index (BMI) signals of 37% when compared to vehicle cohort [2].


Clinical trial: Up to now, FRAX1036 is still in the preclinical development stage.


参考文献:
[1] Ong CC et al.  Small molecule inhibition of group I p21-activated kinases in breast cancer induces apoptosis and potentiates the activity of microtubule stabilizing agents. Breast Cancer Res.2015 Apr 23;17:59.
[2] Chow HY et al.  Group I Paks as therapeutic targets in NF2-deficient meningioma. Oncotarget.2015 Feb 10;6(4):1981-94.