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CX-6258
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。
CX-6258图片
CAS NO:1202916-90-2
规格:98%
分子量:461.94
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议
50mg电议

产品介绍
Pan-Pim kinases Inhibitor
CAS:1202916-90-2
分子式:C26H24ClN3O3
分子量:461.94
纯度:98%
存储:Store at -20°C

Background:

Pim kinases (Provirus Integration site for Moloney murine leukemia virus) are a family of serine/threonine kinases that regulate cell survival. This family of kinases is composed of three different isoforms (Pim-1, Pim-2, and Pim-3). The simultaneous inhibition of Pim-1, Pim-2, and Pim-3 kinases is emerging as a promising strategy for anticancer drug development. CX-6258 is a potent, selective, and orally efficacious pan-Pim kinases inhibitor.


In vitro: CX-6258 exhibited in vitro synergy with chemotherapeutics. The antiproliferative activity of CX-6258 was examined against a panel of cell lines derived from human solid tumors and hematological malignancies. CX-6258 demonstrated robust antiproliferative potencies against all cell lines tested [1].


In vivo: CX-6258 was evaluated in two human tumor xenograft growth efficacy models, acute myeloid leukemia MV-4-11, and prostate adenocarcinoma PC3. The drug exhibited dose dependent efficacy, with a 50 mg/kg dose producing 45% tumor growth inhibition (TGI) and a 100 mg/kg dose producing 75% TGI. In addition, CX-6258 displayed significant efficacy in vivo in two xenograft models representing the diseases where Pim kinases had been shown to play an important role [1].


Clinical trial: No clinical data are available


Reference:
[1] Haddach M, Michaux J, Schwaebe MK, et al.  Discovery of CX-6258. A Potent, Selective, and Orally Efficacious pan-Pim Kinases Inhibitor. ACS Med Chem Lett. 2011;3(2):135-9.