ON1231320

目录号: HY-100789 纯度: 98.43%: FAQs
Data Sheet SDS COA 产品使用指南

摩尔计算器

ON1231320 是一种高度特异性的 polo 样激酶 2 (PLK2) 抑制剂，IC₅₀ 为 0.31 µM。ON1231320 在有丝分裂 G2/M 期阻断肿瘤细胞周期进程，导致细胞凋亡。ON1231320 是一种芳基磺酰基吡啶并嘧啶酮，具有抗肿瘤活性。

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ON1231320 Chemical Structure

CAS No. : 1312471-39-8

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25 mg	￥3500	In-stock
50 mg	￥5500	In-stock
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Customer Review

MCE 顾客使用本产品发表的 1 篇科研文献

•Comput Struct Biotec. 2023 Jan 16.

ON1231320 相关产品

•相关化合物库:

•同靶点产品:

•同靶点蛋白产品:

查看 Polo-like Kinase (PLK) 亚型特异性产品:

查看所有亚型

PLK1 PLK2 PLK3 PLK4

生物活性
纯度 & 产品资料
参考文献

生物活性

ON1231320 is a highly specific polo like kinase 2 (PLK2) inhibitor with an IC₅₀ of 0.31 µM. ON1231320 blocks tumor cell cycle progression in the G2/M phase in mitosis, causing apoptotic cell death. ON1231320, an arylsulfonyl pyrido-pyrimidinone, has antitumor activity^[1]^[2].

IC₅₀ & Target^[1]

PLK2

0.31 μM (IC₅₀)

PLK1

>10 μM (IC₅₀)

PLK3

>10 μM (IC₅₀)

PLK4

>10 μM (IC₅₀)

细胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
5637	GI₅₀	0.125 μM Compound: 7ao; ON1231320	Growth inhibition of human 5637 cells after 72 hrs by trypan blue assay Growth inhibition of human 5637 cells after 72 hrs by trypan blue assay	[PMID: 26762835]
A-431	GI₅₀	0.03 μM Compound: 7ao; ON1231320	Growth inhibition of human A431 cells after 72 hrs by trypan blue assay Growth inhibition of human A431 cells after 72 hrs by trypan blue assay	[PMID: 26762835]
A549	GI₅₀	0.075 μM Compound: 7ao; ON1231320	Growth inhibition of human A549 cells after 72 hrs by trypan blue assay Growth inhibition of human A549 cells after 72 hrs by trypan blue assay	[PMID: 26762835]
ASPC1	GI₅₀	0.3 μM Compound: 7ao; ON1231320	Growth inhibition of human AsPC1 cells after 72 hrs by trypan blue assay Growth inhibition of human AsPC1 cells after 72 hrs by trypan blue assay	[PMID: 26762835]
Bel-7402	GI₅₀	0.05 μM Compound: 7ao; ON1231320	Growth inhibition of human Bel7402 cells after 72 hrs by trypan blue assay Growth inhibition of human Bel7402 cells after 72 hrs by trypan blue assay	[PMID: 26762835]
BT-474	GI₅₀	0.1 μM Compound: 7ao; ON1231320	Growth inhibition of human BT474 cells after 72 hrs by trypan blue assay Growth inhibition of human BT474 cells after 72 hrs by trypan blue assay	[PMID: 26762835]
BT-549	GI₅₀	0.25 μM Compound: 7ao; ON1231320	Growth inhibition of human BT549 cells after 72 hrs by trypan blue assay Growth inhibition of human BT549 cells after 72 hrs by trypan blue assay	[PMID: 26762835]
BXPC-3	GI₅₀	0.075 μM Compound: 7ao; ON1231320	Growth inhibition of human BxPC3 cells after 72 hrs by trypan blue assay Growth inhibition of human BxPC3 cells after 72 hrs by trypan blue assay	[PMID: 26762835]
CAPAN-1	GI₅₀	0.075 μM Compound: 7ao; ON1231320	Growth inhibition of human Capan1 cells after 72 hrs by trypan blue assay Growth inhibition of human Capan1 cells after 72 hrs by trypan blue assay	[PMID: 26762835]
CCRF-CEM	GI₅₀	0.05 μM Compound: 7ao; ON1231320	Growth inhibition of human CEM cells after 72 hrs by trypan blue assay Growth inhibition of human CEM cells after 72 hrs by trypan blue assay	[PMID: 26762835]
COLO 205	GI₅₀	0.075 μM Compound: 7ao; ON1231320	Growth inhibition of human COLO205 cells after 72 hrs by trypan blue assay Growth inhibition of human COLO205 cells after 72 hrs by trypan blue assay	[PMID: 26762835]
Daudi	GI₅₀	0.075 μM Compound: 7ao; ON1231320	Growth inhibition of human Daudi cells after 72 hrs by trypan blue assay Growth inhibition of human Daudi cells after 72 hrs by trypan blue assay	[PMID: 26762835]
DU-145	IC₅₀	0.075 μM Compound: 7ao; ON1231320	Growth inhibition of human DU145 cells after 72 hrs by trypan blue assay Growth inhibition of human DU145 cells after 72 hrs by trypan blue assay	[PMID: 26762835]
Granta-519	GI₅₀	0.04 μM Compound: 7ao; ON1231320	Growth inhibition of human GRANTA-519 cells after 72 hrs by trypan blue assay Growth inhibition of human GRANTA-519 cells after 72 hrs by trypan blue assay	[PMID: 26762835]
HCC1806	GI₅₀	0.1 μM Compound: 7ao; ON1231320	Growth inhibition of human HCC1806 cells after 72 hrs by trypan blue assay Growth inhibition of human HCC1806 cells after 72 hrs by trypan blue assay	[PMID: 26762835]
HCT-116	GI₅₀	0.15 μM Compound: 7ao; ON1231320	Growth inhibition of human HCT116 cells after 72 hrs by trypan blue assay Growth inhibition of human HCT116 cells after 72 hrs by trypan blue assay	[PMID: 26762835]
HeLa	GI₅₀	0.05 μM Compound: 7ao; ON1231320	Growth inhibition of human HeLa cells after 72 hrs by trypan blue assay Growth inhibition of human HeLa cells after 72 hrs by trypan blue assay	[PMID: 26762835]
HepG2	GI₅₀	0.5 μM Compound: 7ao; ON1231320	Growth inhibition of human HepG2 cells after 72 hrs by trypan blue assay Growth inhibition of human HepG2 cells after 72 hrs by trypan blue assay	[PMID: 26762835]
HFL1	GI₅₀	> 2 μM Compound: 7ao; ON1231320	Growth inhibition of human HFL1 cells after 72 hrs by trypan blue assay Growth inhibition of human HFL1 cells after 72 hrs by trypan blue assay	[PMID: 26762835]
HL-60	GI₅₀	0.125 μM Compound: 7ao; ON1231320	Growth inhibition of human HL60 cells after 72 hrs by trypan blue assay Growth inhibition of human HL60 cells after 72 hrs by trypan blue assay	[PMID: 26762835]
Jurkat	GI₅₀	0.025 μM Compound: 7ao; ON1231320	Growth inhibition of human Jurkat cells after 72 hrs by trypan blue assay Growth inhibition of human Jurkat cells after 72 hrs by trypan blue assay	[PMID: 26762835]
K562	IC₅₀	0.075 μM Compound: 7ao; ON1231320	Growth inhibition of human K562 cells after 72 hrs by trypan blue assay Growth inhibition of human K562 cells after 72 hrs by trypan blue assay	[PMID: 26762835]
LNCaP	GI₅₀	0.04 μM Compound: 7ao; ON1231320	Growth inhibition of human LNCAP cells after 72 hrs by trypan blue assay Growth inhibition of human LNCAP cells after 72 hrs by trypan blue assay	[PMID: 26762835]
MCF7	GI₅₀	0.075 μM Compound: 7ao; ON1231320	Growth inhibition of human MCF7 cells after 72 hrs by trypan blue assay Growth inhibition of human MCF7 cells after 72 hrs by trypan blue assay	[PMID: 26762835]
MDA-MB-436	GI₅₀	0.15 μM Compound: 7ao; ON1231320	Growth inhibition of human MDA-MB-436 cells after 72 hrs by trypan blue assay Growth inhibition of human MDA-MB-436 cells after 72 hrs by trypan blue assay	[PMID: 26762835]
MDA-MB-453	GI₅₀	0.075 μM Compound: 7ao; ON1231320	Growth inhibition of human MDA-MB-453 cells after 72 hrs by trypan blue assay Growth inhibition of human MDA-MB-453 cells after 72 hrs by trypan blue assay	[PMID: 26762835]
MIA PaCa-2	GI₅₀	0.075 μM Compound: 7ao; ON1231320	Growth inhibition of human MIAPaCa2 cells after 72 hrs by trypan blue assay Growth inhibition of human MIAPaCa2 cells after 72 hrs by trypan blue assay	[PMID: 26762835]
NCI-H1650	GI₅₀	0.2 μM Compound: 7ao; ON1231320	Growth inhibition of human NCI-H1650 cells after 72 hrs by trypan blue assay Growth inhibition of human NCI-H1650 cells after 72 hrs by trypan blue assay	[PMID: 26762835]
NCI-H1734	GI₅₀	0.15 μM Compound: 7ao; ON1231320	Growth inhibition of human NCI-H1734 cells after 72 hrs by trypan blue assay Growth inhibition of human NCI-H1734 cells after 72 hrs by trypan blue assay	[PMID: 26762835]
NCI-H1975	GI₅₀	0.075 μM Compound: 7ao; ON1231320	Growth inhibition of human NCI-H1975 cells after 72 hrs by trypan blue assay Growth inhibition of human NCI-H1975 cells after 72 hrs by trypan blue assay	[PMID: 26762835]
NCI-H23	GI₅₀	0.2 μM Compound: 7ao; ON1231320	Growth inhibition of human H23 cells after 72 hrs by trypan blue assay Growth inhibition of human H23 cells after 72 hrs by trypan blue assay	[PMID: 26762835]
NCI-H292	GI₅₀	0.15 μM Compound: 7ao; ON1231320	Growth inhibition of human NCI-H292 cells after 72 hrs by trypan blue assay Growth inhibition of human NCI-H292 cells after 72 hrs by trypan blue assay	[PMID: 26762835]
NCI-H460	GI₅₀	0.1 μM Compound: 7ao; ON1231320	Growth inhibition of human H460 cells after 72 hrs by trypan blue assay Growth inhibition of human H460 cells after 72 hrs by trypan blue assay	[PMID: 26762835]
Panc1005	GI₅₀	0.4 μM Compound: 7ao; ON1231320	Growth inhibition of human Panc 10.05 cells after 72 hrs by trypan blue assay Growth inhibition of human Panc 10.05 cells after 72 hrs by trypan blue assay	[PMID: 26762835]
PC-3	GI₅₀	0.15 μM Compound: 7ao; ON1231320	Growth inhibition of human PC3 cells after 72 hrs by trypan blue assay Growth inhibition of human PC3 cells after 72 hrs by trypan blue assay	[PMID: 26762835]
PLC-PRF-5	GI₅₀	0.75 μM Compound: 7ao; ON1231320	Growth inhibition of human PLC/PRF/5 cells after 72 hrs by trypan blue assay Growth inhibition of human PLC/PRF/5 cells after 72 hrs by trypan blue assay	[PMID: 26762835]
Raji	GI₅₀	0.05 μM Compound: 7ao; ON1231320	Growth inhibition of human Raji cells after 72 hrs by trypan blue assay Growth inhibition of human Raji cells after 72 hrs by trypan blue assay	[PMID: 26762835]
RT-4	GI₅₀	0.5 μM Compound: 7ao; ON1231320	Growth inhibition of human RT4 cells after 72 hrs by trypan blue assay Growth inhibition of human RT4 cells after 72 hrs by trypan blue assay	[PMID: 26762835]
SK-HEP1	GI₅₀	0.1 μM Compound: 7ao; ON1231320	Growth inhibition of human SKHEP1 cells after 72 hrs by trypan blue assay Growth inhibition of human SKHEP1 cells after 72 hrs by trypan blue assay	[PMID: 26762835]
SK-MEL-28	GI₅₀	0.2 μM Compound: 7ao; ON1231320	Growth inhibition of human SK-MEL-28 cells after 72 hrs by trypan blue assay Growth inhibition of human SK-MEL-28 cells after 72 hrs by trypan blue assay	[PMID: 26762835]
SK-OV-3	GI₅₀	0.075 μM Compound: 7ao; ON1231320	Growth inhibition of human SKOV3 cells after 72 hrs by trypan blue assay Growth inhibition of human SKOV3 cells after 72 hrs by trypan blue assay	[PMID: 26762835]
SNU-398	GI₅₀	0.15 μM Compound: 7ao; ON1231320	Growth inhibition of human SNU398 cells after 72 hrs by trypan blue assay Growth inhibition of human SNU398 cells after 72 hrs by trypan blue assay	[PMID: 26762835]
SNU-449	GI₅₀	0.4 μM Compound: 7ao; ON1231320	Growth inhibition of human SNU449 cells after 72 hrs by trypan blue assay Growth inhibition of human SNU449 cells after 72 hrs by trypan blue assay	[PMID: 26762835]
SNU-475	GI₅₀	7.5 μM Compound: 7ao; ON1231320	Growth inhibition of human SNU475 cells after 72 hrs by trypan blue assay Growth inhibition of human SNU475 cells after 72 hrs by trypan blue assay	[PMID: 26762835]
SU.86.86	GI₅₀	0.4 μM Compound: 7ao; ON1231320	Growth inhibition of human SU8686 cells after 72 hrs by trypan blue assay Growth inhibition of human SU8686 cells after 72 hrs by trypan blue assay	[PMID: 26762835]
SW780	GI₅₀	0.15 μM Compound: 7ao; ON1231320	Growth inhibition of human SW780 cells after 72 hrs by trypan blue assay Growth inhibition of human SW780 cells after 72 hrs by trypan blue assay	[PMID: 26762835]
T-24	GI₅₀	0.15 μM Compound: 7ao; ON1231320	Growth inhibition of human T24 cells after 72 hrs by trypan blue assay Growth inhibition of human T24 cells after 72 hrs by trypan blue assay	[PMID: 26762835]
TCC-SUP	GI₅₀	0.25 μM Compound: 7ao; ON1231320	Growth inhibition of human TCCSUP cells after 72 hrs by trypan blue assay Growth inhibition of human TCCSUP cells after 72 hrs by trypan blue assay	[PMID: 26762835]
U2OS	GI₅₀	0.035 μM Compound: 7ao; ON1231320	Growth inhibition of human U2OS cells after 72 hrs by trypan blue assay Growth inhibition of human U2OS cells after 72 hrs by trypan blue assay	[PMID: 26762835]
U-87MG ATCC	GI₅₀	0.02 μM Compound: 7ao; ON1231320	Growth inhibition of human U87 cells after 72 hrs by trypan blue assay Growth inhibition of human U87 cells after 72 hrs by trypan blue assay	[PMID: 26762835]
U-937	GI₅₀	0.125 μM Compound: 7ao; ON1231320	Growth inhibition of human U937 cells after 72 hrs by trypan blue assay Growth inhibition of human U937 cells after 72 hrs by trypan blue assay	[PMID: 26762835]
UMUC3	GI₅₀	0.3 μM Compound: 7ao; ON1231320	Growth inhibition of human UM-UC-3 cells after 72 hrs by trypan blue assay Growth inhibition of human UM-UC-3 cells after 72 hrs by trypan blue assay	[PMID: 26762835]
WI-38	GI₅₀	> 5 μM Compound: 7ao; ON1231320	Growth inhibition of human WI38 cells after 72 hrs by trypan blue assay Growth inhibition of human WI38 cells after 72 hrs by trypan blue assay	[PMID: 26762835]
Z-138	GI₅₀	0.2 μM Compound: 7ao; ON1231320	Growth inhibition of human Z138 cells after 72 hrs by trypan blue assay Growth inhibition of human Z138 cells after 72 hrs by trypan blue assay	[PMID: 26762835]

体外研究
(In Vitro)

ON1231320 (化合物 7ao) 对 PLK1、PLK3 和 PLK4 没有抑制活性 (所有 IC₅₀>10 μM)^[1]。
ON1231320 (0-5 μM；24 小时) 激活人类肿瘤细胞的程序性细胞死亡^[1]。
ON1231320 抑制 16 种肿瘤细胞系 (DU145、MCF-7、BT474、SK-OV-3、MIA-PaCa-2、SK-MEL-28、A549、U87、COLO -205、HELA、H1975、RAJI、U205、K562、GRANTA-519；IC₅₀= 0.035-0.2 μM)^[1]。
ON1231320 不会明显抑制微管蛋白聚合^[1]。
ON1231320 不影响正常人成纤维细胞^[2]。

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

Apoptosis Analysis^[1]

Cell Line:	U2OS cells
Concentration:	0-5 µM
Incubation Time:	24 hours
Result:	Increased the activity of Caspases 3/7 in a dose-dependent manner. Induced apoptosis.

体内研究
(In Vivo)

ON1231320 (化合物 7ao；75 mg/kg；腹腔注射；隔日 (Q2D) 给药 20 天) 显著抑制肿瘤生长^[1]。

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

Animal Model:	6-8 week old NCR nu/nu female mice with MDAMB-231 triple negative breast cancer cells^[1]
Dosage:	75 mg/kg
Administration:	IP; alternate days (Q2D) for 20 days
Result:	Resulted in significant inhibition of tumor growth (86.5%)

分子量

467.45

Formula

C₂₂H₁₅F₂N₅O₃S

CAS 号

1312471-39-8

性状

固体

颜色

Light yellow to green yellow

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

细胞实验：

DMSO 中的溶解度 : 50 mg/mL (106.96 mM; 超声助溶; 吸湿的 DMSO 对产品的溶解度有显著影响，请使用新开封的 DMSO)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1393 mL	10.6963 mL	21.3927 mL
5 mM	0.4279 mL	2.1393 mL	4.2785 mL
10 mM	0.2139 mL	1.0696 mL	2.1393 mL

查看完整储备液配制表

* 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。

摩尔计算器
稀释计算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

浓度 _(start)

体积 _(start)

浓度 _(final)

体积 _(final)

动物实验：

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

方案一

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.35 mM); 悬浊液; 超声助溶

此方案可获得 2.5 mg/mL的均匀悬浊液，悬浊液可用于口服和腹腔注射。
以 1 mL 工作液为例，取 100 μL 25.0 mg/mL 的澄清 DMSO 储备液加到 900 μL 20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。
2 g SBE-β-CD（磺丁基醚 β-环糊精）粉末定容于 10 mL 的生理盐水中，完全溶解至澄清透明。

动物溶解方案计算器

请输入动物实验的基本信息：

给药剂量

mg/kg

动物的平均体重

每只动物的给药体积

μL

动物数量

只

由于实验过程有损耗，建议您多配一只动物的量

请输入您的动物体内配方组成：

DMSO +

Tween-80 +

Saline

如果您的动物是免疫缺陷鼠或者体弱鼠，建议 DMSO 中的在最后工作液体系中的占比尽量不超过 2%。

方案所需 助溶剂 包括：DMSO，，均可在 MCE 网站选购。，Tween 80，均可在 MCE 网站选购。

计算结果

工作液所需浓度 : mg/mL

储备液配制方法 : mg 药物溶于 μL DMSO（母液浓度为 mg/mL）。

您所需的储备液浓度超过该产品的实测溶解度，以下方案仅供参考，如有需要，请与 MCE 中国技术支持联系。

动物实验体内工作液的配制方法 : 取 μL DMSO 储备液，加入 μL 。 μL ，混合均匀至澄清，再加 μL Tween 80，混合均匀至澄清，再加 μL 生理盐水。

连续给药周期超过半月以上，请谨慎选择该方案。

请确保第一步储备液溶解至澄清状态，从左到右依次添加助溶剂。您可采用超声加热（超声清洗仪，建议频次 20-40 kHz），涡旋吹打等方式辅助溶解。

纯度 & 产品资料

纯度: 99.24%

选择批次：

Data Sheet (634 KB) SDS (252 KB)

COA (262 KB) HNMR (437 KB) LCMS (88 KB)

产品使用指南 (1538 KB)

参考文献

[1]. M V Ramana Reddy, et al. Discovery of 2-(1H-indol-5-ylamino)-6-(2,4-difluorophenylsulfonyl)-8-methylpyrido[2,3-d]pyrimidin-7(8H)-one (7ao) as a potent selective inhibitor of Polo like kinase 2 (PLK2). Bioorg Med Chem. 2016 Feb 15;24(4):521-44. [Content Brief]

[2]. Shashidhar S. Jatiani, et al. Abstract 643: Targeting cancer with a selective ATP-mimetic inhibitor of polo like kinase-2.

ON1231320 相关分类

完整储备液配制表

可选溶剂	浓度溶剂体积质量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	2.1393 mL	10.6963 mL	21.3927 mL	53.4817 mL
	5 mM	0.4279 mL	2.1393 mL	4.2785 mL	10.6963 mL
	10 mM	0.2139 mL	1.0696 mL	2.1393 mL	5.3482 mL
	15 mM	0.1426 mL	0.7131 mL	1.4262 mL	3.5654 mL
	20 mM	0.1070 mL	0.5348 mL	1.0696 mL	2.6741 mL
	25 mM	0.0856 mL	0.4279 mL	0.8557 mL	2.1393 mL
	30 mM	0.0713 mL	0.3565 mL	0.7131 mL	1.7827 mL
	40 mM	0.0535 mL	0.2674 mL	0.5348 mL	1.3370 mL
	50 mM	0.0428 mL	0.2139 mL	0.4279 mL	1.0696 mL
	60 mM	0.0357 mL	0.1783 mL	0.3565 mL	0.8914 mL
	80 mM	0.0267 mL	0.1337 mL	0.2674 mL	0.6685 mL
	100 mM	0.0214 mL	0.1070 mL	0.2139 mL	0.5348 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

ON12313201312471-39-8ON 1231320ON-1231320Polo-like Kinase (PLK)ApoptosisG2/MphasemitosisfibroblastsU2OSMDAMB-231triplenegativebreastInhibitorinhibitorinhibit

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ON1231320

Customer Review

MCE 顾客使用本产品发表的 1 篇科研文献

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