PXL51107
| CAS号 | 1627929-55-8 | 货号 | BCP28928 |
| 中文名 | PXL51107 | ||
| 英文名 | PXL51107 | ||
| 中文别名 | |||
| 英文别名 | PXL 51107 ; PXL-51107; | ||
| 分子式 | C26H22N4O3 | 分子量 | 438.48 |
| 生物活性 | PLX51107 is a novel structurally distinct BET bromodomain inhibitor that inhibits all four BET family proteins BRD2, BRD3, BRD4, and BRDT with low nanomolar potency; exhibits modest preference for BD1 versus BD2 within each BET protein (Kd=1.6, 2.1, 1.7, and 5 nM for BD1 and 5.9, 6.2, 6.1 and 120 nM for BD2 of BRD2, BRD3, BRD4, and BRDT, respectively).potently reduces viability and proliferation of the human AML cell lines MV4-11, MOLM-13, OCI-AML3, and Kasumi-1 with IC50 of 0.17, 1.8, 0.2 and 0.2 uM, respectively; has sufficient potency and oral bioavailability to demonstrate in vivo efficacy in animal models of a variety of tumor types.PLX51107 shows significant interactions only with the bromodomains of CBP and EP300 (p300) (Kd in the 100 nM range). | ||
| 信号通路 | Epigenetics | ||
| 靶 点 | Epigenetic Reader Domain | ||
结构式
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