CAS NO: | 2095732-06-0 |
包装 | 价格(元) |
100mg | 电议 |
250mg | 电议 |
500mg | 电议 |
生物活性 | Numidargistat (CB-1158) is a potent and orally active inhibitor ofarginase, withIC50s of 86 nM and 296 nM forrecombinant humanarginase1andrecombinant humanarginase2, respectively. Immuno-oncology agent[1]. |
IC50& Target | IC50: 86 nM (Arginase 1), 296 nM (Arginase 2)[1] |
体外研究 (In Vitro) | Numidargistat is a potent and orally-bioavailable inhibitor of arginase, with IC50s of 86 and 296 nM for recombinant human arginase 1 and 2, respectively. Numidargistat 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). Numidargistat 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. Numidargistat show no effect on NOS. In addition, Numidargistat is not directly cytotoxic to murine cancer cell lines[1]. |
体内研究 (In Vivo) | Numidargistat (100 mg/kg, p.o., twice per day) increases the number of tumor-infiltrating cytotoxic cells and decreases myeloid cells in mice. Numidargistat in combination with PD-L1 blockade or gemcitabine inhibits tumor growth in mice bearing CT26 cancer cells[1]. |
分子量 | 287.12 |
Formula | C11H22BN3O5 |
CAS 号 | 2095732-06-0 |
运输条件 | Room temperature in continental US; may vary elsewhere. |
储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |