产品说明书
ZT-12-037-01
 |
同义名 : | - |
| CAS号 : | 2328073-61-4 | |
| 货号 : | A1177125 | |
| 分子式 : | C21H31N5O2 | |
| 纯度 : | 99%+ | |
| 分子量 : | 385.503 | |
| MDL号 : | MFCD32197197 | |
| 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： |
| 生物活性 | |||
|---|---|---|---|
| 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]. | ||
| 实验方案 | |||
|---|---|---|---|
| 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 |
| 参考文献 |
|---|