ZT-12-037-01|cas:2328073-61-4|西域试剂

ZT-12-037-01,98.67%

产品编号：Bellancom-122866| CAS NO：2328073-61-4| 分子式：C₂₁H₃₁N₅O₂| 分子量：385.50

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货号	价格	库存与货期
Bellancom-122866	￥800.00	杭州北京（现货）
Bellancom-122866	￥1400.00	杭州北京（现货）
Bellancom-122866	￥5600.00	杭州北京（现货）
Bellancom-122866	￥9800.00	杭州北京（现货）

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ZT-12-037-01

产品介绍

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。

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.

体外研究

ZT-12-037-01 (3 μM; 14 days) significantly inhibits mutant NRAS-STK19-driven melanocyte colony formation and proliferation.
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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

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

Cell Line:	STK19^WT and STK19^D89N
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.

西域 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
Dosage:	25 mg/kg; 50 mg/kg
Administration:	Intraperitoneally injection; 21 days; once a day
Result:	Inhibited growth of SK-MEL-2 xenograft melanoma.

体内研究

西域 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
Dosage:	25 mg/kg; 50 mg/kg
Administration:	Intraperitoneally injection; 21 days; once a day
Result:	Inhibited growth of SK-MEL-2 xenograft melanoma.

体内研究

西域 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
Dosage:	25 mg/kg; 50 mg/kg
Administration:	Intraperitoneally injection; 21 days; once a day
Result:	Inhibited growth of SK-MEL-2 xenograft melanoma.

性状

Solid

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