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抑制剂描述:

产品名称:TPX-0005

产品别名:见爱必信官网

英文别名:TPX-0005

靶点:ALK

CAS:1802220-02-5

纯度:>98%

外观:见爱必信官网

保存方法:Store at -20℃ for one year(Powder);Store at 2-4℃ for two weeks;Store at -20℃ for six months after dissolution.

描述:

 TPX-0005是一种新型的ALK/ROS1/TRK抑制剂,对WT ALK、ALK(G1202R)、ALK(L1196M)的IC₅₀分别为1.01 nM、1.26 nM、1.08 nM;同时也是一种有效的SRC抑制剂,IC₅₀为5.3 nM。

溶解性:DMSO:70 mg/mL (196.97 mM)
Ethanol:10 mg/mL (28.13 mM)

体外研究:

TPX-0005 is an orally available and potent ATP-competitive inhibitor against ALK, ROS1, TRKA, TRKB and TRKC recombinant kinases and their corresponding clinical resistant mutants. TPX-0005 demonstrates potent anti-proliferative activity in the range of sub-nanomolar to low nanomolar in a number of human cancer cell lines and engineered stable cell lines expressing the targeted oncogenes or their solvent front mutants, accompanied by inhibition of target phosphorylation and concomitant inactivation of downstream effectors such as ERK, AKT and STAT3. TPX-0005 inhibits H2228 cell migration in a wound healing assay with similar activity to saracatinib. TPX-0005 is able to not only inhibit the wild-type and a broad spectrum of mutant ALKs, but also overcome primary resistance and suppress metastatic features by inhibiting SRC.

体内研究:In patient derived xenograft tumor models, TPX-0005 treatment results in significant regression of tumors harboring the oncogenic ALK, ROS1 and TRKC fusions. Moreover, in a series of mouse xenograft tumor models, TPX-0005 exhibits marked anti-tumor activity not only in tumors harboring the wildtype oncogenic targets but also in tumors harboring the oncogenes with the solvent front mutations via inhibition of the target phosphorylation.

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