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CB-1158(INCB01158)
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。
CB-1158(INCB01158)图片
CAS NO:2095732-06-0
规格:98%
分子量:287.12
包装与价格:
包装价格(元)
5mg电议
10mg电议
25mg电议

产品介绍
CB-1158是一种有效的,可口服的精氨酸酶(arginase)抑制剂,对重组人arginase1/2的IC50值分别为86和296nM。
CAS:2095732-06-0
分子式:C11H22BN3O5
分子量:287.12
纯度:98%
存储:Store at -20°C

Background:

CB-1158 is a potent and orally bioavailable inhibitor of arginase, with IC50s of 86 and 296 nM for recombinant human arginase 1 and 2, respectively.


CB-1158 is a potent and orally-bioavailable inhibitor of arginase, with IC50s of 86 and 296 nM for recombinant human arginase 1 and 2, respectively. CB-1158 inhibits native rginase 1 (Arg1) in human granulocyte, erythrocyte, and hepatocyte lysate with IC50s of 178 nM, 116 nM and 158 nM, respectively, and blocks Arg1 in cancer patient plasma (IC50, 122 nM). CB-1158 also exhibits potent inhibitory activity against arginase in human HepG2, K562 cell lines and primary human hepatocytes with IC50s of 32, 139, 210 μM, respectively. CB-1158 show no effect on NOS. In addition, CB-1158 is not directly cytotoxic to murine cancer cell lines[1].


CB-1158 (100 mg/kg, p.o., twice per day) increases the number of tumor-infiltrating cytotoxic cells and decreases myeloid cells in mice. CB-1158 in combination with PD-L1 blockade or gemcitabine inhibits tumor growth in mice bearing CT26 cancer cells[1].


[1]. Steggerda SM, et al. Inhibition of arginase by CB-1158 blocks myeloid cell-mediated immune suppression in the tumor microenvironment. J Immunother Cancer. 2017 Dec 19;5(1):101.