CAN508

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CAN508  纯度: 99.91%

CAN508 是一种有效的、ATP 竞争性抑制 CDK9/cyclin T1，IC50为 0.35 μM。CAN508 对 CDK9/cyclin T1 比对其他的 CDK/cyclin 高出 38 倍的选择性。CAN508 具有抗肿瘤活性。

CAN508

CAN508 Chemical Structure

CAS No. : 140651-18-9

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ￥990 In-stock
5 mg ￥900 In-stock
10 mg ￥1700 In-stock
25 mg ￥3500 In-stock
50 mg ￥6000 In-stock
100 mg   询价  
200 mg   询价  

* Please select Quantity before adding items.

CAN508 相关产品

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生物活性

CAN508 is a potent, ATP-competitive CDK9/cyclin T1 inhibitor with an IC50 of 0.35 μM. CAN508 exhibits a 38-fold selectivity for CDK9/cyclin T over other CDK/cyclin complexes. Antitumor activity[1][2].

IC50 & Target[1]

CDK9/cyclinT1

0.35 μM (IC50)

CDK2/cyclinE

20 μM (IC50)

cdk2/cyclin A

69 μM (IC50)

Cdk4/cyclin D1

13.5 μM (IC50)

CDK7/cyclin H

26 μM (IC50)

Cdk1/cyclin B

44 μM (IC50)

体外研究
(In Vitro)

CAN508 reduces the frequency of S-phase cells of the cancer cell line HT-29 in antiproliferation assays[1].
CAN508 (20-40 μM; 72 hours) significantly reduces cell proliferation in a dose dependent manner in all three esophageal adenocarcinoma cell lines (SKGT4, OE33 and FLO-1 cells) with IC50s ranging from 34.99 to 91.09 μM[2].
CAN508 (40 μM; 72 hours) increases apoptosis in all three esophageal adenocarcinoma cells[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: SKGT4, OE33 and FLO-1 cells
Concentration: 40 μM
Incubation Time: 72 hours
Result: Increased apoptosis by 2 fold in all three esophageal adenocarcinoma cells compared to untreated controls.

体内研究
(In Vivo)

CAN508 (60 mg/kg; i.p.; daily for 10 days) has antitumor effects in esophageal adenocarcinoma xenografts[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: 4 weeks-old female nude mice (esophageal adenocarcinoma xenografts)[1]
Dosage: 60 mg/kg
Administration: I.p.; daily for 10 days
Result: Caused reduction of tumor growth starting from post-treatment day three with 50.83% reduction.

分子量

218.22

Formula

C9H10N6O
CAS 号

140651-18-9
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

4°C, protect from light

*In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
溶解性数据
In Vitro: 

DMSO : 250 mg/mL (1145.63 mM; Need ultrasonic)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 4.5825 mL 22.9127 mL 45.8253 mL
5 mM 0.9165 mL 4.5825 mL 9.1651 mL
10 mM 0.4583 mL 2.2913 mL 4.5825 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 (protect from light)。-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    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (9.53 mM); Clear solution

    此方案可获得 ≥ 2.08 mg/mL (9.53 mM，饱和度未知) 的澄清溶液。

    以 1 mL 工作液为例，取 100 μL 20.8 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。

    将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液

*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]. Krystof V, et al. 4-arylazo-3,5-diamino-1H-pyrazole CDK inhibitors: SAR study, crystal structure in complex with CDK2, selectivity, and cellular effects. J Med Chem. 2006;49(22):6500-6509.

    [2]. Tong Z, et al. Antitumor effects of cyclin dependent kinase 9 inhibition in esophageal adenocarcinoma. Oncotarget. 2017;8(17):28696-28710.

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