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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; | ||
SMILES | C O)(=O)C1=CC=C(C2C3=NC=C(C4=C(C) | ||
化学名称 | |||
分子式 | C26H22N4O3 | 分子量 | 438.48 |
纯度 | 98% | 配送 | 惯例下常温包邮 |
产品描述 | 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). |
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