Tazemetostat - CAS:1403254-99-8

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Tazemetostat (Synonyms:EPZ-6438; E-7438)

目录号 : KM6272 CAS No. : 1403254-99-8 纯度 : 98%

Tazemetostat (EPZ-6438) 是一种有效，选择性，口服的 EZH2 抑制剂。Tazemetostat (EPZ-6438) 抑制含有 PRC2 复合体的野生型 EZH2 的活性， K_i 值为 2.5±0.5 nM。Tazemetostat (EPZ-6438) 抑制 EZH2，在肽测定和核小体测定中 IC₅₀ 分别为 11 和 16 nM。Tazemetostat (EPZ-6438) 抑制大鼠 EZH2，IC₅₀ 为 4 nM。Tazemetostat (EPZ-6438) 还抑制 EZH1，IC₅₀ 为 392 nM。

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5mg		In-stock
10mg		In-stock
50mg		In-stock
100mg		In-stock
200mg		In-stock
500mg	询价	In-stock
1g	询价	In-stock

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生物活性

Tazemetostat (EPZ-6438) is a potent, selective and orally available EZH2 inhibitor. Tazemetostat (EPZ-6438) inhibits the activity of human polycomb repressive complex 2 (PRC2)-containing wild-type EZH2 with a K_i value of 2.5 nM. Tazemetostat (EPZ-6438) inhibits EZH2 with IC₅₀s of 11 and 16 nM in peptide assay and nucleosome assay, respectively. Tazemetostat (EPZ-6438) inhibits rat EZH2 with an IC₅₀ of 4 nM. Tazemetostat (EPZ-6438) also inhibits EZH1 with an IC₅₀ of 392 nM.

体外研究

Tazemetostat (EPZ-6438) inhibits multi wild-type and mutant lymphoma cell lines proliferation with IC₅₀s of 0.49 nM-7.6 μM.

Cell Proliferation Assay

Cell Line:	Wild-type and mutant lymphoma cell lines: DOHH-2 cell (EZH2 wild-type), Farage cell (EZH2 wild-type), OCI-LY19 cell (EZH2 wild-type), Toledo cell (EZH2 wild-type), KARPAS-422 (EZH2 Y646N), Pfeiffer (EZH2 A682G), RL cell line (EZH2 Y646N), SU-DHL-10 (EZH2 Y646F), SU-DHL-6 (EZH2 Y646N), WSU-DLCL2 (EZH2 Y646F)
Concentration:	0.49 nM-7.6 μM
Incubation Time:	11 days
Result:	Inhibited DOHH-2 cell (EZH2 wild-type; IC₅₀=1.7 μM), Farage cell (EZH2 wild-type; IC₅₀=99 nM), OCI-LY19 cell (EZH2 wild-type; IC₅₀=6.2 μM), Toledo cell (EZH2 wild-type; IC₅₀=7.6 μM), KARPAS-422 (EZH2 Y646N; IC₅₀=1.8 nM), Pfeiffer (EZH2 A682G; IC₅₀=0.49 nM), RL cell line (EZH2 Y646N; IC₅₀=5.8 μM), SU-DHL-10 (EZH2 Y646F; IC₅₀=5.8 nM), SU-DHL-6 (EZH2 Y646N; IC₅₀=4.7 nM), WSU-DLCL2 (EZH2 Y646F; IC₅₀=8.6 nM) proliferation.

体内研究

Tazemetostat (EPZ-6438; 250 or 500 mg/kg twice daily for 21-28 days) practically eliminates the fast-growing G401 tumors.

Animal Model:	SCID mice bearing s.c. G401 xenografts
Dosage:	125 mg/kg, 250 mg/kg, 500 mg/kg
Administration:	Oral; twice daily; 28 days
Result:	Practically eliminated the fast-growing G401 tumors at 250 or 500 mg/kg.

分子式

C₃₄H₄₄N₄O₄

分子量

572.74

CAS号

1403254-99-8

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 : 31.25 mg/mL (54.56 mM; ultrasonic and warming and heat to 60°C)

0.1 M HCL : 14.29 mg/mL (24.95 mM; ultrasonic and adjust pH to 5 with HCl)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.7460 mL	8.7300 mL	17.4599 mL
5 mM	0.3492 mL	1.7460 mL	3.4920 mL
10 mM	0.1746 mL	0.8730 mL	1.7460 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。

临床试验

科研文献

纯度： 98%

Data Sheet

产品使用指南

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Other Forms of Rapamycin:

KKL 顾客使用本产品发表的 31 篇科研文献

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