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PXL51107 结构式

PXL51107

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货号 :BCP28928CAS号 :1627929-55-8纯度:98%
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  • 基本信息与产品描述
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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