OTX015
货号：
15947-1mg 基本售价：
686.0 元 规格：
1 mg
产品信息
概述| 货号 | 15947-1mg |
| 描述 | The bromodomain and extra terminal domain (BET) family of proteins, including BRD2, BRD3, and BRD4, play a key role in many cellular processes, including inflammatory gene expression, mitosis, and viral/host interaction by controlling the assembly of histone acetylation-dependent chromatin complexes. OTX015 is an orally bioavailable, small molecule inhibitor of BRD2, BRD3, and BRD4 (EC50s = 10-19 nM).1 It displays antiproliferative effects at a sub-micromolar range in vitro in a wide range of solid tumor types and leukemias, downregulating c-Myc expression and inducing cell cycle arrest and apoptosis.1,2,3 At 100 mg/kg, OTX015 has been shown to inhibit the growth of Ty82 BRD-NUT midline carcinoma tumors in nude mice by 79%.1 |
| 别名 | HY-15743;(−)-OTX015; |
性能| 供应商 | Cayman |
| 应用文献 |
1.Noel, J.K.,Iwata, K.,Ooike, S., et al. Development of the BET bromodomain inhibitor OTX015. Molecular Cancer Therapeutics 12, C244 (2013).
2.Braun, T.,Coude, M.M.,Berrou, J., et al. Preclinical study of the bromodomain inhibitor OTX015 in acute myeloid (AML) and lymphoid (ALL) leukemias. Blood 122, 4218 (2014).
3.Boi, M.,Todaro, M.,Vurchio, V., et al. OTX015, a bromodomain and extraterminal inhibitor, represents a novel agent for ALK positive anaplastic large cell lymphoma. Molecular Cancer Therapeutics 12, A219 (2013).
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| 运输条件 | Room temperature in continental US; may vary elsewhere |
| 存放说明 | -20 |
| 纯度 | ≥95% |
| 计算分子量 | 492 |
| 分子式 | C25H22ClN5O2S |
| CAS号 | 202590-98-5 |
| 稳定性 | ≥ 2 years |
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