FRAX1036 |
Katalog-Nr.GC10251 |
FRAX1036 ist ein PAK-Inhibitor mit Kis von 23,3 nM, 72,4 nM und 2,4 μM fÜr PAK1, PAK2 bzw. PAK4.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1432908-05-8
Sample solution is provided at 25 µL, 10mM.
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.
References:
[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.
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