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产品名称 | PLK1 ↓ ↑ | PLK2 ↓ ↑ | PLK3 ↓ ↑ | PLK4 ↓ ↑ | 其他靶点 | 纯度 | |||||||||||||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
HMN-214 | ✔ | 99%+ | |||||||||||||||||
SBE13 HCl |
++++
PLK1, IC50: 200 pM |
98% | |||||||||||||||||
Onvansertib |
+++
PLK1, IC50: 2 nM |
99%+ | |||||||||||||||||
Volasertib |
++++
PLK1, IC50: 0.87 nM |
97% | |||||||||||||||||
GSK461364 |
+++
PLK1, Ki: 2.2 nM |
99%+ | |||||||||||||||||
MLN0905 |
+++
PLK1, IC50: 2 nM |
99%+ | |||||||||||||||||
Ro3280 |
++
PLK1, IC50: 3 nM |
99% | |||||||||||||||||
(E/Z)-Rigosertib sodium |
+
PLK1, IC50: 9 nM |
+
PLK2, IC50: 260 nM |
Bcr-Abl | 99%+ | |||||||||||||||
BI 2536 |
++++
PLK1, IC50: 0.83 nM |
++
PLK2, IC50: 3.5 nM |
+
PLK3, IC50: 9.0 nM |
99%+ | |||||||||||||||
CFI-400945 |
++
PLK4, IC50: 2.8 nM |
Tie-2 | 98% | ||||||||||||||||
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 | ON1231320, a selective inhibitor of PLK2, exhibits an IC50 of 0.31 µM. It impedes the progression of the tumor cell cycle at the G2/M phase during mitosis, leading to apoptosis. As an arylsulfonyl pyrido-pyrimidinone compound, ON1231320 possesses antitumor properties[1][2]. ON1231320 effectively curbs the proliferation of a spectrum of 16 tumor cell lines, including DU145, MCF-7, BT474, SK-OV-3, MIA-PaCa-2, SK-MEL-28, A549, U87, COLO-205, HELA, H1975, RAJI, U205, K562, and GRANTA-519, with IC50 values ranging from 0.035 to 0.2 µM. Additionally, ON1231320 is not known to significantly affect tubulin polymerization[1]. |
Animal study | The administration of ON1231320, at a dose of 75 mg/kg via intraperitoneal injection every other day for a period of 20 days, led to a marked reduction in tumor growth. The treatment achieved an 86.5% decrease in tumor size in an animal model comprising 6-8 week old NCR nu/nu female mice implanted with MDA-MB-231 triple negative breast cancer cells[1]. |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.14mL 0.43mL 0.21mL |
10.70mL 2.14mL 1.07mL |
21.39mL 4.28mL 2.14mL |
CAS号 | 1312471-39-8 |
分子式 | C22H15F2N5O3S |
分子量 | 467.448 |
别名 | 7ao |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Inert atmosphere,2-8°C |
溶解度 |
DMSO: 50 mg/mL(106.96 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 |
动物实验配方 |