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ON123300

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

ON123300  纯度: 99.34%

ON123300 是一种强效的，可透过血脑屏障的多激酶抑制剂，可抑制 CDK4 (IC50=3.9 nM），Ark5 (IC50=5 nM)，PDGFRβ (IC50=26 nM)，FGFR1 (IC50=26 nM)，RET (IC50=9.2 nM) 和 FYN (IC50=11 nM)。ON123300 在脑肿瘤中抑制 Akt 磷酸化及激活 Erk。ON123300 抑制 CDK6，IC50 为 9.82 nM。

ON123300

ON123300 Chemical Structure

CAS No. : 1357470-29-1

规格 价格 是否有货 数量
Free Sample (0.1-0.5 mg)   Apply now  
10 mM * 1 mL in DMSO ￥1134 In-stock
2 mg ￥800 In-stock
5 mg ￥1200 In-stock
10 mg ￥1800 In-stock
50 mg ￥6600 In-stock
100 mg ￥9950 In-stock
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生物活性

ON123300, a strong and brain-penetrant[1] multi-kinase inhibitor, inhibits CDK4 (IC50=3.9 nM), Ark5 (IC50=5 nM), PDGFRβ (IC50=26 nM), FGFR1 (IC50=26 nM), RET (IC50=9.2 nM), and FYN (IC50=11 nM). Single agent ON123300 causes a dose-dependent suppression of phosphorylation of Akt as well as activation of Erk in brain tumors[2]. ON123300 inhibits CDK6 with an IC50 of 9.82 nM[3].

IC50 & Target[2][3]

Cdk4/cyclin D1

3.9 nM (IC50)

ARK5

5 nM (IC50)

CDK6/cyclinD1

9.82 nM (IC50)

RET

9.2 nM (IC50)

FYN

11 nM (IC50)

FGFR1

26 nM (IC50)

PDGFRβ

26 nM (IC50)

PI3K-δ

144 nM (IC50)

体外研究
(In Vitro)

ON123300 inhibits U87 glioma cell proliferation with an IC50 of 3.4±0.1 μM[2]. ON123300 (1 and 10 μM) inhibits cell proliferation in a panel of 11 glioma models including a patient-derived model (GBM10)[2].
ON123300 (6.3 μM; 1 h) reduces phosphorylation of Akt and its downstream signaling components, P70S6K, 40S rpS6 and Rb S780, yet ON123300 induces Erk activation in U87 cells; both in a dose- and time-dependent manner[2]. ON123300 inhibits PI3Kδ with the IC50 of 144nM[3].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Cytotoxicity Assay[2]

Cell Line: U87 glioma cells
Concentration: 0, 4, 8, 12, 16 μM
Incubation Time: 72 hour
Result: Had an IC50 equal to 3.4±0.1 μM.

Western Blot Analysis[2]

Cell Line: U87 cells
Concentration: 6.3 μM
Incubation Time: 1 h
Result: Inhibited phosphorylation of Akt (at S473 site) and its downstream signaling components, P70S6K, 40S ribosomal protein S6 (rpS6) and Rb S780 (decreased to 40.1%; 31.8 %; 60.5%; 54.5% relatively to control), yet increased p-Erk (increased to 120% relative to control).

体内研究
(In Vivo)

ON123300 decreases p-Akt expression and increases p-Erk activity in brain tumors upon administration at both IV doses of 5 mg/kg and 25 mg/kg in U87 brain tumor-bearing mouse. The half-life (T1/2) is 1.5 h for 5 mg/kg and 25 mg/kg in plasma[2].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: NIH Swiss nude mice bearing U87 glioma model[2].
Dosage: 5 mg/kg or 25 mg/kg
Administration: IV bolus at a dose of either 5 mg/kg or 25 mg/kg via a tail vein.
Result: The p-Akt rapidly declined and reached nadir values of 73% and 60% of control within 30 min after 5 mg/kg and 25 mg/kg dose levels, respectively.

Clinical Trial

分子量

429.52

Formula

C24H27N7O
CAS 号

1357470-29-1
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 : 16.67 mg/mL (38.81 mM; ultrasonic and warming and heat to 60°C)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.3282 mL 11.6409 mL 23.2818 mL
5 mM 0.4656 mL 2.3282 mL 4.6564 mL
10 mM 0.2328 mL 1.1641 mL 2.3282 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。
参考文献

  • [1]. Hua Lv, et al. Integrated pharmacokinetic-driven approach to screen candidate anticancer drugs for brain tumor chemotherapy. AAPS J. 2013 Jan;15(1):250-7.

    [2]. Xiaoping Zhang, et al. Preclinical pharmacological evaluation of a novel multiple kinase inhibitor, ON123300, in brain tumor models. Mol Cancer Ther. 2014 May;13(5):1105-16.

    [3]. S K A Divakar, et al. Dual inhibition of CDK4/Rb and PI3K/AKT/mTOR pathways by ON123300 induces synthetic lethality in mantle cell lymphomas. Leukemia. 2016 Jan;30(1):86-93.

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ON1231320

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上海金畔生物科技有限公司为生命科学和医药研发人员提供生物活性分子抑制剂、激动剂、特异性抑制剂、化合物库、重组蛋白，专注于信号通路和疾病研究领域。

ON1231320  纯度: 99.24%

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。

ON1231320

ON1231320 Chemical Structure

CAS No. : 1312471-39-8

规格 价格 是否有货 数量
5 mg ￥1000 In-stock
10 mg ￥1700 In-stock
25 mg ￥3500 In-stock
50 mg ￥5500 In-stock
100 mg ￥9500 In-stock
200 mg   询价  
500 mg   询价  

* Please select Quantity before adding items.

ON1231320 相关产品

•相关化合物库:

  • Bioactive Compound Library Plus

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)

体外研究
(In Vitro)

ON1231320 (Compound 7ao) has no inhibitory activity against PLK1, PLK3 and PLK4 (all IC50>10 µM)[1].
ON1231320 (0-5 µM; 24 hours) activates programmed cell death in human tumor cells[1].
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)[1].
ON1231320 does not appreciably inhibit tubulin polymerization[1]. ON1231320 does not affect normal human fibroblasts[2].

上海金畔生物科技有限公司 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 (Compound 7ao; 75 mg/kg; IP; alternate days (Q2D) for 20 days) results in significant inhibition of tumor growth[1].

上海金畔生物科技有限公司 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
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 : 25 mg/mL (53.48 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。

    将 2 g 磺丁基醚 β-环糊精加入 5 mL 生理盐水中，再用生理盐水定容至 10 mL，完全溶解，澄清透明
*以上所有助溶剂都可在 上海金畔生物科技有限公司 网站选购。
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.

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

所有产品仅用作科学研究或药证申报，我们不为任何个人用途提供产品和服务