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首页-小分子抑制剂&激动剂-Epigenetics-Bromodomain-PLX51107
PLX51107

Chemical Structure : PLX51107

CAS No.: 1627929-55-8

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PLX51107 (PLX-51107, OPN-51107, OPN5)

货号: PC-50010Not For Human Use, Lab Use Only.

PLX51107 (OPN-51107, OPN5) is a novel structurally distinct BET bromodomain inhibitor that inhibits all four BET family proteins BRD2, BRD3, BRD4, and BRDT with low nanomolar potency.

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5 mg ￥980 In stock
10 mg ￥1580 In stock
25 mg ￥2780 In stock
50 mg ￥4580 In stock
100 mg Get quote
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

PLX51107 (OPN-51107, OPN5) is a novel structurally distinct BET bromodomain inhibitor that inhibits all four BET family proteins BRD2, BRD3, BRD4, and BRDT with low nanomolar potency.
PLX51107 exhibits modest preference for BD1 versus BD2 within each BET protein (Kd=1.6, 2.1, 1.7, and 5 nM for BD1 and 5.9, 6.2, 6.1 and 120 nM for BD2 of BRD2, BRD3, BRD4, and BRDT, respectively).
PLX51107 potently reduces viability and proliferation of the human AML cell lines MV4-11, MOLM-13, OCI-AML3, and Kasumi-1 with IC50 of 0.17, 1.8, 0.2 and 0.2 uM, respectively.
PLX51107 has sufficient potency and oral bioavailability to demonstrate in vivo efficacy in animal models of a variety of tumor types.

物理化学性质&存储条件

分子量 438.487
分子式 C26H22N4O3
外观性状 Solid
CAS No.
储存条件
固体粉末
-20 °C 12 个月; 4°C 6 个月
配置液
-80 °C 6 个月; -20°C 6 个月
Shipping Room temperature in continental US; may vary elsewhere
Solubility

10 mM in DMSO
Chemical Name/SMILES

(S)-4-(6-(3,5-dimethylisoxazol-4-yl)-1-(1-(pyridin-2-yl)ethyl)-1H-pyrrolo[3,2-b]pyridin-3-yl)benzoic acid

参考文献

1. Ozer HG, et al. Cancer Discov. 2018 Jan 31. pii: CD-17-0902.

2. Nicole R. Grieselhuber, et al. Blood 2016 128:3941.

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