ZT-12-037-01 是一种选择性丝氨酸/苏氨酸激酶 STK19 的抑制剂,与 STK19 蛋白具有高亲和力相互作用,抑制 NRAS 驱动的黑素细胞恶性转化。ZT-12-037-01 是 ATP 竞争性抑制剂,可以抑制 NRAS 的磷酸化,IC50 为 24 nM。
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描述 | The serine/threonine-protein kinase 19 (STK19) is a critical regulator of NRAS, one of the major isoforms of the RAS family. The oncogenic mutation of NRAS is a critical driver for the proliferation of melanocyte and eventually the transformation to melanoma. ZT-12-037-01 is a potent and selective STK19 inhibitor with an IC50 value of 24.04nM. ZT-12-037-01 at the doses of 0.01–3μM efficiently inhibited the phosphorylation of NRAS in vitro at a dose- and time-dependent manner. It also showed STK19-targeted inhibition in the presence of ATP (10, 30, 100, and 300μM) with increasing IC50 values (35.46, 95.6, 169.3 and 680.7nM, respectively). The inhibitory effect of ZT-12-037-01 (0.1–3μM) on STK19WT and STK19D89N-activated NRAS phosphorylation was observed in human primary melanocytes. Treatment with 3μM ZT-12-037-01 significantly suppressed NRAS-STK19-driven colony formation in mutant melanocytes. In nude mice inoculated with SK-MEL-2 cells, ZT-12-037-01 treatment (at 25 and 50mg/kg) inhibited tumor growth in a dose-dependent manner. Mice treated by ZT-12-037-01 also presented a markedly lower level of Ki67 and a higher expression of cleaved caspase-3 in tumors. The survival rate of SK-MEL-2 xenografts showed significantly prolonged survival rate compared with control group[1]. |
作用机制 | ZT-12-037-01 is an ATP-competitive inhibitor for STK19[1]. |
Dose | C57BL/6J mice: 25 mg/kg[1] (i.p., BID) |
Administration | i.p. |
计算器 | ||||
存储液制备 | ![]() |
1mg | 5mg | 10mg |
1 mM 5 mM 10 mM |
2.59mL 0.52mL 0.26mL |
12.97mL 2.59mL 1.30mL |
25.94mL 5.19mL 2.59mL |
CAS号 | 2328073-61-4 |
分子式 | C21H31N5O2 |
分子量 | 385.503 |
别名 | |
运输 | 蓝冰 |
存储条件 |
粉末 Inert atmosphere,Room Temperature 液体 -20°C:3-6个月-80°C:12个月 |
溶解度 |
DMSO: 50 mg/mL(129.7 mM),配合低频超声,并调节pH至2,注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO 1M HCl: 100 mg/mL(259.4 mM),配合低频超声助溶 |
动物实验配方 |