CF53 - BET 抑制劑 - 生命科學(xué)試劑 - MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemECF53Cat. No.: HY-112610CAS No.: 1808160-52-2分式: CHNO分量: 443.5作靶點(diǎn): Epigenetic Reader Domain; Histone Acetyltransferase作通路: Epigenetics儲(chǔ)存式: -20C, stored under nitrogen* In solvent : -80C, 6 months; -20C, 1 month (stored undernitro

2、gen)溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 110 mg/mL (248.03 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 2.2548 mL 11.2740 mL 22.5479 mL5 mM 0.4510 mL 2.2548 mL 4.5096 mL10 mM 0.2255 mL 1.1274 mL 2.2548 mL請(qǐng)根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。體內(nèi)實(shí)驗(yàn) 請(qǐng)根據(jù)您的實(shí)驗(yàn)動(dòng)物和給藥式選擇適當(dāng)?shù)娜芙獍?，配制前?qǐng)先配制澄清的儲(chǔ)備液，再依次添加

3、助溶劑(為保證實(shí)驗(yàn)結(jié)果的可靠性，體內(nèi)實(shí)驗(yàn)的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄清的儲(chǔ)備液可以根據(jù)儲(chǔ)存條件，適當(dāng)保存；以下溶劑前的百分 指該溶劑在您配制終溶液中的體積占)：1. 請(qǐng)依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 1.83 mg/mL (4.13 mM); Clear solution2. 請(qǐng)依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 1.83 mg/mL (4.13 mM); Clear solutionBIOLOGICAL ACTIVITY1/2 Master o

4、f Small Molecules 您邊的抑制劑師www.MedChemE物活性 CF53種效、選擇性、可服的 BET 抑制劑，對(duì) BRD4 BD1 的 Ki 值為 Kd 值為 2.2 nM，IC50 值為 2nM；CF53 對(duì) BRD2，BRD3，BRD4 和 BRDT BET 蛋的 BD1 和 BD2 兩個(gè)結(jié)構(gòu)域都有親和性，對(duì)其選擇性遠(yuǎn)于含溴結(jié)構(gòu)域 BET 蛋。CF53 在體外和體內(nèi)都具有顯著的抗腫瘤活性 1。IC50 & Target BRD4 (BD1) BRD4 (BD1) BRD4 (BD1) BRD4 (BD2)1 nM (Ki) 2 nM (IC50) 2.2 nM (Kd)

5、0.8 nM (Kd)BRD2 (BD2) BRD2 (BD1) BRD3 (BD2) BRD3 (BD1)0.6 nM (Kd) 1.1 nM (Kd) 0.49 nM (Kd) 0.52 nM (Kd)BRDT (BD2) BRDT (BD1) CREBBP EP3001 nM (Kd) 2 nM (Kd) 47 nM (Kd) 110 nM (Kd)CECR2570 nM (Kd)體外研究 CF53 (Compound 28) binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT BETproteins w

6、ith high affinities, Kds are 1.1 nM (BRD2 BD1), 0.6 nM (BRD2 BD2), 0.52 nM (BRD3 BD1), 0.49 nM(BRD3 BD2), 0.8 nM (BRD4 BD2), 2 nM (BRDT BD1), 2.1 nM (BRDT BD2), 47 nM (CREBBP), 570 nM(CECR2), 110 nM (EP300), respectively 1.CF53 exhibits IC50s of 7, 85 nM against MOLM-13 acute leukemia and MDA-MB-231

7、 breast cancer cell lines,respectively 1.體內(nèi)研究 CF53 (25, 50 mg/kg, p.o.) exhibits potent anti-tumor activity both in MDA-MB-231 xenograft tumor model and inRS4;11 model in mice 1.REFERENCES1. Zhao Y, et al. Structure-Based Discovery of CF53 as a Potent and Orally Bioavailable Bromodomain and Extra-Terminal (BET)Bromodomain Inhibitor. J Med Chem. 2018 Jul 26;61(14):6110-6120.McePdfHeightCaution: Product has not been fully validated for medical applications.For resear