Name: PROTAC EZH2 Degrader-1
Brand: TargetMol
SKU: T74602
Rating: 4.5 (1 reviews)

规格

价格

库存

数量

1 mg

¥ 2,150

5日内发货

5 mg

¥ 6,450

5日内发货

10 mg

¥ 9,750

5日内发货

产品介绍

生物活性

产品描述	PROTAC EZH2 Degrader-1 (Compound 150d) is a potent PROTAC molecule that effectively suppresses EZH2 methyltransferase activity, with a half-maximal IC50 of 2.7 nM. EZH2 is a histone methyltransferase crucial to tumorigenesis and cancer progression, and PROTAC EZH2 Degrader-1 represents an important chemical tool for probing its therapeutic relevance.
靶点活性	EZH2:2.7 nM
体外活性	方法：PROTAC EZH2 Degrader-1（2 nM）预处理H128细胞，然后用carboplatin，etoposide 和teniposide 处理72小时，使用CCK8法评估细胞活力。结果：PROTAC EZH2 Degrader-1显著降低了H128-LM细胞对carboplatin，etoposide 和teniposide的IC50值。[2]
体内活性	方法：PROTAC EZH2 Degrader-1（0.5 mg/kg，每周一次，共 3 次）腹腔注射给H128-LM 异种移植小鼠，评估肿瘤生长情况。结果：PROTAC EZH2 degrader-1与carboplatin，etoposide 和teniposide联合使用显著抑制了H128-LM肿瘤的生长，效果优于单独使用化疗药物。[2]

化学信息

分子量	942.15
分子式	C₅₄H₆₇N₇O₈
CAS No.	2641601-67-2
Smiles	O=C(NCC=1C(=O)NC(=CC1C)C)C2=CC(=CC(=C2C)N(CC)C3CCOCC3)C4=CC=C(C=C4)CN5CCN(CC5)CCCCCCCOC6=CC=CC=7C(=O)N(C(=O)C67)C8C(=O)NC(=O)CC8
颜色	White
物理性状	Solid

储存&溶解度

存储

keep away from moisture,store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

溶解度信息

DMSO: 80 mg/mL (84.91 mM), Sonication is recommended.

溶液配制表

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.0614 mL	5.3070 mL	10.6140 mL	53.0701 mL
5 mM	0.2123 mL	1.0614 mL	2.1228 mL	10.6140 mL
10 mM	0.1061 mL	0.5307 mL	1.0614 mL	5.3070 mL
20 mM	0.0531 mL	0.2654 mL	0.5307 mL	2.6535 mL
50 mM	0.0212 mL	0.1061 mL	0.2123 mL	1.0614 mL

体内实验配液计算器