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(+)-JQ-1

CAS No. : 1268524-70-4

MCE 國際站：(+)-JQ-1

產(chǎn)品活性：(+)-JQ-1 (JQ1) 是一種有效特異性的可逆 BET bromodomain 抑制劑，抑制 BRD4(1/2) 的 IC₅₀ 分別為 77 nM 和 33 nM。(+)-JQ-1 激活自噬 (autophagy)。

研究領(lǐng)域：Epigenetics  |  Autophagy  |  PROTAC

作用靶點(diǎn)：Epigenetic Reader Domain  |  Autophagy  |  Ligands for Target Protein for PROTAC

In Vitro: (+)-JQ-1 represents a potent, highly specific and Kac competitive inhibitor for the BET family of bromodomains. (+)-JQ-1 (100 nM, 48 h) prompts squamous differentiation exhibited by cell spindling, flattening and increased expression of keratin. (+)-JQ-1 (250 nM) induces rapid expression of keratin in treated NMC 797 cells compared to (-)-JQ1 (250 nM) and vehicle controls, as determined by quantitative immunohistochemistry.(+)-JQ-1 (250 nM) elicits a time-dependent induction of strong (3+) keratin staining of treated NMC 797 cells, compared to (-)-JQ1 (250 nM). De-repression of autophagy genes is observed almost immediately after (+)-JQ-1 addition. (+)-JQ-1 is a potent thienodiazepine inhibitor (K_d=90 nM) of the BET family coactivator protein BRD4, which is implicated in the pathogenesis of cancer via transcriptional control of the MYC oncogene. Dose-ranging studies of (+)-JQ-1 demonstrates potent inhibition of H4Kac4 binding with a IC₅₀ value of 10 nM for murine BRDT(1) and 11 nM for human BRDT(1).

In Vivo: Matched cohorts of mice with established tumors are randomized to treatment with (+)-JQ1 (50 mg/kg) or vehicle, administered by daily intraperitoneal injection. Prior to randomization, and after four days of therapy, mice are evaluated by FDG-PET imaging. A marked reduction in FDG uptake is observed with (+)-JQ1 treatment. Tumor-volume measurements confirm a reduction in tumor growth with JQ1 treatment. Pharmacokinetic studies of (+)-JQ1 are performed in CD1 mice following intravenous and oral administration. Mean plasma concentration-time profiles of (+)-JQ1 after intravenous dosing (5 mg/kg). The pharmacokinetic parameters for intravenous (+)-JQ1 demonstrate excellent drug exposure (AUC=2090 hr*ng/mL) and an approximately one hour half-life (T1/2). Mean plasma concentration-time profiles of (+)-JQ1 after oral dosing (10 mg/kg). The pharmacokinetic parameters for oral (+)-JQ1 demonstrate excellent oral bioavailability (F=49%), peak plasma concentration (C_max=1180 ng/mL) and drug exposure (AUC=2090 hr*ng/mL).

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