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。
| 生物活性 | CAN508 is a potent, ATP-competitiveCDK9/cyclin T1inhibitor with anIC50of 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) |
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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].
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. |
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体内研究
(In Vivo) | CAN508 (60 mg/kg; i.p.; daily for 10 days) has antitumor effects in esophageal adenocarcinoma xenografts[1].
| 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. |
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| 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 | 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℃, 6 months; -20℃, 1 month (protect from light)。-80℃ 储存时，请在 6 个月内使用，-20℃ 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。 *以上所有助溶剂都可在本网站选购。
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