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.