EPZ-011989 trifluoroacetate 是一种有效且代谢稳定的Zeste Homolog 2 (EZH2)抑制剂，具有口服活性。EPZ-011989 trifluoroacetate 对 EZH2 具有抑制性抑制作用，Ki值<3 nM。EPZ-011989 trifluoroacetate 具有出强大的甲基标记抑制和抗肿瘤活性。EPZ-011989 trifluoroacetate 可用于多种癌症的研究。
| 生物活性 | EPZ-011989 trifluoroacetate is a potent and orally activeZeste Homolog 2 (EZH2)inhibitor with metabolic stability. EPZ-011989 trifluoroacetate has inhibitory inhibition forEZH2with aKivalue of<3 nm. epz-011989 trifluoroacetate shows robust methyl mark inhibition and anti-tumor activity. can be used for the research of various cancers[1]. |
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体外研究
(In Vitro) | EPZ-011989 trifluoroacetate inhibits mutant and wild-type EZH2 with an Kivalue of<3 nm[1].
EPZ-011989 trifluoroacetate reduces cellular H3K27 methylation with an IC50value of 94 nM[1].
EPZ-011989 trifluoroacetate (0-10 μM; 11 days) has anti-proliferation effect in WSU-DLCL2 cells[1].
Cell Proliferation Assay[1] | Cell Line: | WSU-DLCL2 cells | | Concentration: | 0-10 μM | | Incubation Time: | 11 days | | Result: | Demonstrated an average lowest cytotoxic concentration (LCC) in WSU-DLCL2 cells of 208 nM. |
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体内研究
(In Vivo) | EPZ-011989 trifluoroacetate (oral; 30-1000 mg/kg; single or bid; for 7 days or 21 days) can elicit robust methyl mark inhibition and antitumor activity[1].
| Animal Model: | SCID mice[1] | | Dosage: | 125, 250, 500, and 1000 mg/kg | | Administration: | Oral; single, twice-daily (BID)for 7 days or twice-daily (BID)for 21 days | | Result: | Provided coverage over the LCC for 24 h (1000 mg/kg ), while the 250 and 500 mg/kg doses provided coverage over this value for approximately 8 h.
Observed complete ablation of the methyl mark by the end of day 7.
Showed robust tumor growth inhibition, methyl mark reduction and extended total and free plasma exposure time. |
| Animal Model: | Rat[1] | | Dosage: | 30, 100, and 300 mg/kg | | Administration: | Oral, single | | Result: | | dose (mg/kg) | route | t1/2(h) | tmax(h) | Cmax(ng/mL) | AUCinf(h*ng/mL) | time above LCC (h) | | 30 | p.o. | 4.7 | 2 | 240 | 970 | 4 | | 100 | p.o. | 3.9 | 2.7 | 1600 | 5600 | 8 | | 300 | p.o. | 3.7 | 2.7 | 2900 | 10000 | 10 |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | 4°C, sealed storage, away from moisture *In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture) |
| 溶解性数据 | In Vitro: DMSO : 100 mg/mL(138.92 mM;Need ultrasonic) 配制储备液 | 1 mM | 1.3892 mL | 6.9461 mL | 13.8922 mL | | 5 mM | 0.2778 mL | 1.3892 mL | 2.7784 mL | | 10 mM | 0.1389 mL | 0.6946 mL | 1.3892 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 (sealed storage, away from moisture)。-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: ≥ 2.5 mg/mL (3.47 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (3.47 mM，饱和度未知) 的澄清溶液。 以 1 mL 工作液为例，取 100 μL 25.0 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。 2. 请依序添加每种溶剂： 10% DMSO 90% (20%SBE-β-CDin saline) Solubility: ≥ 2.5 mg/mL (3.47 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (3.47 mM，饱和度未知) 的澄清溶液。 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 μL20% 的 SBE-β-CD 生理盐水水溶液中，混合均匀。 3. 请依序添加每种溶剂： 10% DMSO 90%corn oil Solubility: ≥ 2.5 mg/mL (3.47 mM); Clear solution
此方案可获得 ≥ 2.5 mg/mL (3.47 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。 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玉米油中，混合均匀。 *以上所有助溶剂都可在本网站选购。
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