Name: EZH2-IN-4
Brand: TargetMol
SKU: T39497
Rating: 4.5 (1 reviews)

规格

价格

库存

数量

25 mg

¥ 10,600

6-8周

生物活性

产品描述	EZH2-IN-4 is a highly potent EZH2 inhibitor that can be taken orally. It exhibits inhibitory effects against wild type (WT) 5-membered (5-mer) EZH2 and mutant 5-mer EZH2, with IC 50 values of 0.923 nM and 2.65 nM, respectively. Moreover, EZH2-IN-4 has demonstrated significant anti-cancer activity.
靶点活性	EZH2 (mutant 5-mer):2.65 nM (IC50), EZH2 (WT 5-mer):0.923 nM (IC50)
体外活性	EZH2-IN-4 (example 38) shows a cell H3K27me3 IC 50 of 0.00973 nM in Karpas-422 (EZH2 Y641N) cells[1]. EZH2-IN-4 shows an IC 50 of 10.1 nM in Plate Kj?pas-422 cells[1]. EZH2-IN-4 inhibits the proliferation of ovarian cancer cell lines (COV-434, TOV-21G, TOV-112D, A2780, Caov-3, OVCAR3; IC 50 s=0.02-8.6 μM) and has no effect on SKOV3, HeyA8, HEC59 cell (IC 50 >20 μM)[1].
体内活性	EZH2-IN-4 (example 38; oral gavage; 15 mpk; BID) results in 73% inhibition of tumor methylation in the Karpas-422 xenograft model[1]. EZH2-IN-4 (po; 50 mpk; twice a day; pretreatment for 5 days; followed by co-administration with gemcitabine plus cisplatin for at least 23 additional days) significant inhibits A2780 tumor growth in A2780 xenograft model[1].
别名	EZH2-IN-4

化学信息

分子量	511.73
分子式	C₂₉H₄₁N₃O₃S
CAS No.	2088132-99-2
Smiles	[H][C@@]1(CC[C@@H](CC1)N1CC(C1)OC)[C@@H](C)c1sc2CCCN(Cc3c(C)cc(C)[nH]c3=O)C(=O)c2c1C \|wU:13.15,1.14,wD:4.7,1.0,(-2.14,-2.64,;-3.68,-2.64,;-2.91,-3.98,;-3.68,-5.31,;-5.22,-5.31,;-5.99,-3.98,;-5.22,-2.64,;-5.99,-6.64,;-5.59,-8.13,;-7.08,-8.53,;-7.48,-7.04,;-7.85,-9.86,;-9.39,-9.86,;-2.91,-1.31,;-3.68,.03,;-1.37,-1.31,;-.46,-.06,;1,-.54,;2.21,.42,;3.71,.08,;4.37,-1.31,;3.71,-2.7,;4.67,-3.9,;6.19,-3.67,;6.75,-2.24,;5.79,-1.03,;8.27,-2.01,;9.23,-3.21,;10.76,-2.98,;8.67,-4.65,;7.15,-4.87,;6.59,-6.31,;2.21,-3.04,;1.86,-4.54,;1,-2.08,;-.46,-2.55,;-.94,-4.02,)\|