CF53 |
| カタログ番号GC33028 |
CF53 は BRD4 BD1 の Ki が 1 nM 未満、Kd が 2.2 nM、IC50 が 2 nM の、BET タンパク質の非常に強力で選択的な経口活性阻害剤です。 CF53 は、BRD2、BRD3、BRD4、および BRDT BET タンパク質の BD1 および BD2 ドメインの両方に高い親和性で結合し、BET ブロモドメインを含まないタンパク質よりも非常に選択的です。 CF53 は、in vitro と in vivo の両方で強力な抗腫瘍活性を示します。
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Cas No.: 1808160-52-2
Sample solution is provided at 25 µL, 10mM.
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CF53 is a highly potent, selective and orally active inhibitor of BET protein, with a Ki of <1 nM, Kd of 2.2 nM and an IC50 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[1].
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[1].CF53 exhibits IC50s of 7, 85 nM against MOLM-13 acute leukemia and MDA-MB-231 breast cancer cell lines, respectively[1].
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[1].
[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.
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