(+)-JQ-1

中文名稱：(+)-JQ-1

英文名稱：(+)-JQ-1

產(chǎn)品規(guī)格：1mL(10mM)|2mg|5mg|10mg|50mg|100mg|200mg|500m

(+)-JQ-1是一種BET bromodomain抑制劑，抑制BRD4(1)和BRD4(2)的IC50分別為77 nM和33 nM。(+)-JQ-1激活自噬。在DMSO中的溶解度≥ 45 mg/mL (98.47 mM)。
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CAS號：1268524-70-4
別名：JQ1
純度：99.90%
分子式：C₂₃H₂₅ClN₄O₂S
分子量：456.99
結(jié)構(gòu)式：

保存條件：4℃，有效期2年。溶入溶劑后-20℃請盡量在一個月內(nèi)使用。

體外研究
(+)-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 (Kd=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).

貯存液制備(溶劑為DMSO)：

體內(nèi)研究
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 (Cmax=1180 ng/mL) and drug exposure (AUC=2090 hr*ng/mL).

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