CF53|1808160-52-2|-陌孚医药/Medlife

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CF53

目录号: PL13409 纯度: ≥99%

CAS No. :1808160-52-2

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中文名称	CF53
英文名称	CF53
英文别名	CF53;N-(3-cyclopropyl-1-methyl-1H-pyrazol-5-yl)-7-(3,5-dimethyl-1,2-oxazol-4-yl)-6-methoxy-2-methyl-9H-pyrimido[4,5-b]indol-4-amine;BET inhibitor CF53;N-(5-Cyclopropyl-2-methylpyrazol-3-yl)-7-(3,5-dimethyl-1,2-oxazol-4-yl)-6-methoxy-2-methyl-9H-pyrimi
Cas No.	1808160-52-2
分子式	C₂₄H₂₅N₇O₂
分子量	443.50
包装储存	-20°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

产品详情	CF53 是一种高效、选择性、可口服的 BET 抑制剂，对 BRD4 BD1 的 K_i 值为 <1 nM，K_d 值为 2.2 nM，IC₅₀ 值为 2 nM；CF53 对 BRD2，BRD3，BRD4 和 BRDT BET 蛋白的 BD1 和 BD2 两个结构域都有高亲和性，对其选择性远高于非含溴结构域 BET 蛋白。CF53 在体外和体内都具有显著的抗肿瘤活性。
生物活性	CF53 is a highly potent, selective and orally active inhibitor of BET protein, with a K i of <1 nM, K d of 2.2 nM and an IC 50 of 2 nM for BRD4 BD1. CF53 binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT BET proteins with high affinities, very selective over non-BET bromodomain-containing proteins. CF53 shows potent anti-tumor activity both in vitro and in vivo.
性状	Solid
IC50 & Target[1][2]	BRD4 (BD1) <1 nM (Ki) BRD4 (BD1) 2 nM (IC50
体外研究(In Vitro)	CF53 (Compound 28) binds to both the BD1 and BD2 domains of BRD2, BRD3, BRD4, and BRDT BET proteins with 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. CF53 exhibits IC50s of 7, 85 nM against MOLM-13 acute leukemia and MDA-MB-231 breast cancer cell lines, respectively. has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	CF53 (25, 50 mg/kg, p.o.) exhibits potent anti-tumor activity both in MDA-MB-231 xenograft tumor model and in RS4;11 model in mice. has not independently confirmed the accuracy of these methods. They are for reference only.
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	-20°C, stored under nitrogen In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
参考文献	[1]. 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.

溶解度数据	In Vitro: DMSO : 110 mg/mL (248.03 mM; Need ultrasonic)配制储备液

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