ON1231320 - CAS:1312471-39-8

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ON1231320

目录号 : KM9511 CAS No. : 1312471-39-8

Data Sheet 产品使用指南

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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10mg		In-stock
25mg		In-stock
50mg		In-stock
100mg		In-stock
200mg	询价	In-stock
500mg	询价	In-stock

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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.

体外研究

ON1231320 (Compound 7ao) has no inhibitory activity against PLK1, PLK3 and PLK4 (all IC₅₀>10 µM).
ON1231320 (0-5 µM; 24 hours) activates programmed cell death in human tumor cells.
ON1231320 inhibits cell proliferation in 16 tumor cell lines (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).
ON1231320 does not appreciably inhibit tubulin polymerization. ON1231320 does not affect normal human fibroblasts.

Apoptosis Analysis

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

ON1231320 (Compound 7ao; 75 mg/kg; IP; alternate days (Q2D) for 20 days) results in significant inhibition of tumor growth.

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

分子式

C₂₂H₁₅F₂N₅O₃S

分子量

467.45

CAS号

1312471-39-8

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 : 50 mg/mL (106.96 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	2.1393 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

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： 10% DMSO → 90% (20% SBE-β-CD in saline)

Solubility: 2.5 mg/mL (5.35 mM); Suspended solution; Need ultrasonic

此方案可获得 2.5 mg/mL (5.35 mM) 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。