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CAS No.: 2328073-61-4

ZT-12-037-01 Catalog No. CSN24738

Synonyms: ZT-12-037-01

ZT-12-037-01 is a potent and selective STK19 inhibitor with an IC50 value of 24.04nM

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技术信息

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 STK19^WT 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].
动物研究
剂量
C57BL/6J mice: 25 mg/kg^[1] (i.p., BID)

给药途径
i.p.
参考文献

动物研究
剂量	C57BL/6J mice: 25 mg/kg^[1] (i.p., BID)
给药途径	i.p.

[1] Yin C, Zhu B, Zhang T, Liu T, Chen S, Liu Y, Li X, Miao X, Li S, Mi X, Zhang J, Li L, Wei G, Xu ZX, Gao X, Huang C, Wei Z, Goding CR, Wang P, Deng X, Cui R. Pharmacological Targeting of STK19 Inhibits Oncogenic NRAS-Driven Melanomagenesis. Cell. 2019 Feb 21;176(5):1113-1127.e16.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5940 mL
- 12.9701 mL
- 25.9401 mL
- 5 mM
- 0.5188 mL
- 2.5940 mL
- 5.1880 mL
- 10 mM
- 0.2594 mL
- 1.2970 mL
- 2.5940 mL

技术信息

CAS号

2328073-61-4

储存条件

粉末: Inert atmosphere,Room Temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C21H31N5O2

运输

蓝冰

分子量

385.50

别名

ZT-12-037-01

溶解度

DMSO	insoluble
Water	insoluble

动物实验配方

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