ZT-12-037-01

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ZT-12-037-01  纯度: 98.21%

ZT-12-037-01 是靶向选择性丝氨酸/苏氨酸激酶 STK19 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。

ZT-12-037-01

ZT-12-037-01 Chemical Structure

CAS No. : 2328073-61-4

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生物活性

ZT-12-037-01 is a STK19-targeted inhibitor, has a high-affinity interaction with STK19 protein and inhibits oncogenic NRAS-driven melanocyte malignant transformation. ZT-12-037-01 is an ATP-competitive inhibitor, inhibiting phosphorylation of NRAS (major isoform of Ras family) with an IC50 of 24 nM[1].

体外研究
(In Vitro)

ZT-12-037-01 (3 μM; 14 days) significantly inhibits mutant NRAS-STK19-driven melanocyte colony formation and proliferation[1].
ZT-12-037-01 (0-3 μM) has an inhibitory effects of ZT-12-037-01 on STK19WT and STK19D89N-activated NRAS phosphorylation in HPMs[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay[1]

Cell Line: CDK4 (R24C) melanocyte cells; hTERT melanocyte cells; p53DD melanocyte cells
Concentration: 3 μM
Incubation Time: 14 days
Result: Inhibited melanocyte proliferation.

Western Blot Analysis[1]

Cell Line: STK19WT and STK19D89N
Concentration: 0 μM, 0.1 μM, 0.3 μM, 1 μM, 3 μM
Incubation Time:
Result: Inhibited NRAS phosphorylation.

体内研究
(In Vivo)

ZT-12-037-01 (intraperitoneally injection; 25-50 mg/kg; once daily; 21 days) inhibits growth of SK-MEL-2 xenograft melanoma and the sections of tumors indicates induction of apoptosis by increasing cleaved caspase-3[1].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: SK-MEL-2 xenograft melanoma nude mice with hTERT/p53DD/CDK4(R24C) melanocytes[1]
Dosage: 25 mg/kg; 50 mg/kg
Administration: Intraperitoneally injection; 21 days; once a day
Result: Inhibited growth of SK-MEL-2 xenograft melanoma.

分子量

385.50

Formula

C21H31N5O2
CAS 号

2328073-61-4
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 8.33 mg/mL (21.61 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.5940 mL 12.9702 mL 25.9403 mL
5 mM 0.5188 mL 2.5940 mL 5.1881 mL
10 mM 0.2594 mL 1.2970 mL 2.5940 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。
储备液的保存方式和期限：-80°C, 6 months; -20°C, 1 month。-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用； 以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

  • 1.

    请依序添加每种溶剂： 50% PEG300    50% saline

    Solubility: 5 mg/mL (12.97 mM); Suspended solution; Need ultrasonic

*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
参考文献

  • [1]. Yin C, et al. Pharmacological Targeting of STK19 Inhibits Oncogenic NRAS-Driven Melanomagenesis. Cell. 2019 Feb 21;176(5):1113-1127.e16.

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