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BET bromodomain inhibitor 1

CAS No. : 2411226-02-1

MCE 站：BET bromodomain inhibitor 1

产品活性：BET bromodomain inhibitor 1 是一种具有口服活性的，选择性 BET 溴结构域抑制剂，对 BRD4 的 IC₅₀ 为 2.6 nM。BET bromodomain inhibitor 1 与 BRD2(2)，BRD3(2)，BRD4(1)，BRD4(2) 和 BRDT(2) 高亲和力结合 (K_d 值分别为 1.3 nM、1.0 nM、3.0 nM、1.6 nM、2.1 nM)。BET bromodomain inhibitor 1 具有抗癌活性。

研究领域：Epigenetics

作用靶点：Epigenetic Reader Domain

In Vitro: BET bromodomain inhibitor 1 (compound 38; 31.25-125 nM; 24 hours) leads to more pronounced G1-phase cell cycle arrest.
BET bromodomain inhibitor 1 (31.25-500 nM; 6 or 24 hours) is highly effective in inducing dose-dependent inhibition on c-Myc expression and upregulation of p21 levels.
BET bromodomain inhibitor 1 (31.25-125 nM; 6 hours) robustly reduces the expressions of c-Myc, BCL-2, and CDK6.
BET bromodomain inhibitor 1 does not inhibit five cytochrome P450 enzymes (IC₅₀>20 μM).
BET bromodomain inhibitor 1 demonstrates an excellent selectivity for the BET bromodomain family over other bromodomains, with an ?1500-fold selectivity for BRD4(1) over EP300 (IC₅₀=3857 nM).
BET bromodomain inhibitor 1 strongly inhibited the growth of acute myeloid leukemia cell line MV4-11, acute leukemia cell lines Kasumi-1 and RS-4-11, and multiple myeloma cancer cell line MM1.S cells with IC₅₀ values of 2.4, 4.8, 17.6 and 15.1 nM, respectively.

In Vivo: BET bromodomain inhibitor 1 (compound 38; 6.25, 12.5 mg/kg; PO; daily ; for 28 days) exhibits stronger antitumor activities and completely inhibits the growth of tumor with a tumor growth inhibition (TGI) of 99.7% at 12.5 mg/kg.
BET bromodomain inhibitor 1 (1 mg/kg; IV) has a T_1/2 of 1.3 and 0.9 hours, a CL of 21.5 and 15.3 mL/min?kg, and a V_ss of 1464 and 782 mL/kg for rats and mouse, respectively.
BET bromodomain inhibitor 1 (3 mg/kg; PO) has a T_1/2 of 3.6 hours, a C_max of 159 ng/mL and an AUC of 884 ng?h/mL for rats.
BET bromodomain inhibitor 1 (1.3 mg/kg; PO) has a T_1/2 of 1.3 hours, a C_max of 399 ng/mL and an AUC of 1710 ng?h/mL for mouse.

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