YM458 是一种有效的EZH2和BRD4双重抑制剂，对 EZH2 和 BRD4 的IC50分别为490 nM 和 34 nM。YM458 可抑制实体癌细胞增殖和集落形成，诱导细胞周期阻滞与细胞凋亡 (apoptosis)。YM458 可用于抗癌研究。
| 生物活性 | YM458 is a potentEZH2andBRD4dual inhibitor withIC50s of 490 nM and 34 nM, respectively. YM458 inhibits cell proliferation and colony formation and induces cell cycle arrest andapoptosisin solidcancercells. YM458 can be used for researching anticancer[1]. |
| IC50& Target[1] | EZH2 490 nM (IC50) | BRD4 34 nM (IC50) |
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体外研究
(In Vitro) | YM458 (compound D7) (0-30 μM; 6 days) has antiproliferative activities against AsPC-1 cells with an IC50of 0.69 ± 0.16 μM; and (1 μM; 72 hours) significantly decreases the degree of H3K27me3 and c-Myc in AsPC-1[1].
YM458 (0-30 μM; 4 or 6 days) inhibits cell proliferation on a broad range of solid cancer cells, and significantly suppresses proliferation of A549 lung cancer cells and HCT116 colorectal cancer cells at 1 μM[1].
YM458 (0.05-0.4 μM; 12-20 days) inhibits colony formation of AsPC-1, HCT116, and A549 cancer cells in a dose-dependent manner[1].
Western Blot Analysis | Cell Line: | AsPC-1[1] | | Concentration: | 1 μM | | Incubation Time: | 72 hours | | Result: | Decreased the degree of H3K27me3 and c-Myc significantly. |
Cell Proliferation Assay | Cell Line: | AsPC-1, SW1990, CFPAC-1, A549, HCC827, H1650, H292, H460, DLD1, HCT116, and RKO[1] | | Concentration: | 0-30 μM | | Incubation Time: | 4 or 6 days | | Result: | Inhibited cell proliferation on a broad range of solid cancer cells, and significantly suppressed proliferation of A549 lung cancer cells and HCT116 colorectal cancer cells at 1 μM. |
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体内研究
(In Vivo) | YM458 (60 mg/kg; IP; every other day, for 38 days) prevents tumor growth with inhibitory rates of 38.6% in AsPC-1 cells and 62.3% in A549 cells[1].
Pharmacokinetic Parameters of YM458 in Female BALB/c mice[1].
| IP (80 mg/kg) | PO (80 mg/kg) | | t1/2(h) | 3.81 | 4.16 | | Tmax(h) | 1 | 1 | | Cmax(ng/mL) | 27126.3 | 4383.6 | | AUC0-24(ng/mL·h) | 273220.1 | 13509.1 | | CL (mL/min/kg) | 4.88 | | | F (%) | | 4.94 |
| Animal Model: | BALB/c nude mice (injected with A549 or AsPC-1)[1] | | Dosage: | 60 mg/kg | | Administration: | IP; every other day, for 38 days | | Result: | Prevented tumor growth with inhibitory rates of 38.6% in AsPC-1 cells and 62.3% in A549 cells. |
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| 运输条件 | Room temperature in continental US; may vary elsewhere. |
| 储存方式 | Please store the product under the recommended conditions in the Certificate of Analysis. |
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