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| 产品名称 | ERK ↓ ↑ | ERK1 ↓ ↑ | ERK2 ↓ ↑ | ERK5 ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
| DEL-22379 |
+
ERK, IC50: 0.5 μM |
+
ERK, IC50: 0.5 μM |
98% | ||||||||||||||||
| Pluripotin |
++
ERK1, Kd: 98 nM |
RasGAP | 98+% | ||||||||||||||||
| FR 180204 |
+
ERK1, Ki: 0.31 μM |
++
ERK2, Ki: 0.14 μM |
98% | ||||||||||||||||
| Ravoxertinib |
+++
ERK1, IC50: 1.1 nM |
++++
ERK2, IC50: 0.3 nM |
99%+ | ||||||||||||||||
| SCH772984 |
+++
ERK1, IC50: 4 nM |
++++
ERK2, IC50: 1 nM |
99%+ | ||||||||||||||||
| Temuterkib |
+++
ERK1, IC50: 5 nM |
+++
ERK2, IC50: 5 nM |
99%+ | ||||||||||||||||
| VX-11e |
+++
ERK2, Ki: <2 nM |
99%+ | |||||||||||||||||
| Ulixertinib |
++++
ERK2, IC50: <0.3 nM |
99%+ | |||||||||||||||||
| XMD17-109 |
++
ERK5, IC50: 162 nM |
99%+ | |||||||||||||||||
| 1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 | |||||||||||||||||||
| 描述 | KO-947 is a potent and selective inhibitor of ERK1/2 kinases with potential clinical utility in MAPK pathway dysregulated tumors. |
| Concentration | Treated Time | Description | References | |
| U118MG-R cells | 10 μM | Investigate the inhibitory effect of KO-947 on ERK phosphorylation | CNS Neurosci Ther. 2022 Dec;28(12):2104-2115. | |
| T98G-R cells | 10 μM | Investigate the inhibitory effect of KO-947 on ERK phosphorylation | CNS Neurosci Ther. 2022 Dec;28(12):2104-2115. |
| Administration | Dosage | Frequency | Description | References | ||
| J:NU mice | Subcutaneous tumor model | Intraperitoneal injection | 50 mg/kg | Single dose, imaging after 2 hours | Evaluate the inhibitory effect of KO-947 on ERK in subcutaneous tumor model, results showed significant signal increase | ACS Cent Sci. 2023 Mar 20;9(4):719-732 |
| NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
| NCT03051035 | Advanced Malignant Neoplasm | Phase 1 | Recruiting | April 15, 2020 | United States, Minnesota ... 展开 >> Mayo Clinic Not yet recruiting Rochester, Minnesota, United States, 55902 United States, Pennsylvania Fox Chase Cancer Center Recruiting Philadelphia, Pennsylvania, United States, 19111-2497 收起 << |
| 计算器 | ||||
| 存储液制备 | ![]() |
1mg | 5mg | 10mg |
|
1 mM 5 mM 10 mM |
2.81mL 0.56mL 0.28mL |
14.07mL 2.81mL 1.41mL |
28.14mL 5.63mL 2.81mL |
|
| CAS号 | 1695533-89-1 |
| 分子式 | C21H17N5O |
| 分子量 | 355.39 |
| SMILES Code | O=C(NC1=C(C=C2C(NN=C2C3=CC=NC=C3)=C1)C4)N4CC5=CC=CC=C5 |
| MDL No. | MFCD31657422 |
| 别名 | |
| 运输 | 蓝冰 |
| InChI Key | ODIUJYZERXVGEI-UHFFFAOYSA-N |
| Pubchem ID | 136653617 |
| 存储条件 |
In solvent -20°C: 3-6个月 -80°C: 12个月 Pure form Sealed in dry, 2-8°C |
| 溶解方案 |
DMSO: 60 mg/mL(168.83 mM),配合低频超声助溶,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 以下溶解方案都请先按照体外实验的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
|
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