EPZ011989 trifluoroacetate EPZ-011989 trifluoroacetate|cas:1598383-41-5|西域试剂

EPZ011989 trifluoroacetate EPZ-011989 trifluoroacetate

产品编号：Bellancom-16986A| CAS NO：1598383-41-5| 分子式：C₃₇H₅₂F₃N₅O₆| 分子量：719.83

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货号	价格	库存与货期
Bellancom-16986A	￥1120.00	杭州北京（现货）
Bellancom-16986A	￥1960.00	杭州北京（现货）
Bellancom-16986A	￥6860.00	杭州北京（现货）

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EPZ011989 trifluoroacetate EPZ-011989 trifluoroacetate

产品介绍

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，K_i 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 active Zeste Homolog 2 (EZH2) inhibitor with metabolic stability. EPZ-011989 trifluoroacetate has inhibitory inhibition for EZH2 with a K_i value of <3 nM. EPZ-011989 trifluoroacetate shows robust methyl mark inhibition and anti-tumor activity. EPZ-011989 trifluoroacetate can be used for the research of various cancers.

体外研究

EPZ-011989 trifluoroacetate inhibits mutant and wild-type EZH2 with an K_i value of <3 nM.
EPZ-011989 trifluoroacetate reduces cellular H3K27 methylation with an IC₅₀ value of 94 nM.
EPZ-011989 trifluoroacetate (0-10 μM; 11 days) has anti-proliferation effect in WSU-DLCL2 cells.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Proliferation Assay

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.

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	SCID mice
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

Dosage:

30, 100, and 300 mg/kg

Administration:

Oral, single

Result:

dose (mg/kg)	route	t_1/2 (h)	t_max (h)	C_max (ng/mL)	AUC_inf (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

体内研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	SCID mice
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

Dosage:

30, 100, and 300 mg/kg

Administration:

Oral, single

Result:

dose (mg/kg)	route	t_1/2 (h)	t_max (h)	C_max (ng/mL)	AUC_inf (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

体内研究

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.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	SCID mice
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

Dosage:

30, 100, and 300 mg/kg

Administration:

Oral, single

Result:

dose (mg/kg)	route	t_1/2 (h)	t_max (h)	C_max (ng/mL)	AUC_inf (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

性状

Solid

溶解性数据

In Vitro:

DMSO : 100 mg/mL (138.92 mM; Need ultrasonic)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

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°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)。-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: ≥ 2.5 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。
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
2.

请依序添加每种溶剂： 10% DMSO 90% (20% SBE-β-CD in 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 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
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。