中文名 | Inobrodib |
英文名 | (S)-1-(3,4-difluorophenyl)-6-(5-(3,5-dimethylisoxazol-4-yl)-1-((1r,4S)-4-methoxycyclohexyl)-1H-benzo[d]imidazol-2-yl)piperidin-2-one |
别名 | 化合物CBP-IN-1 |
英文别名 | CCS147 CCS1477 CBP-IN-1 CCS-1477 Inobrodib CBP inhibitor 1 CBP-IN-1 (CCS1477) CCS-1477(CBP-IN-1) 2-Piperidinone, 1-(3,4-difluorophenyl)-6-[5-(3,5-dimethyl-4-isoxazolyl)-1-(trans-4-methoxycyclohexyl)-1H-benzimidazol-2-yl]-, (6S)- (S)-1-(3,4-difluorophenyl)-6-(5-(3,5-dimethylisoxazol-4-yl)-1-((1r,4S)-4-methoxycyclohexyl)-1H-benzo[d]imidazol-2-yl)piperidin-2-one |
CAS | 2222941-37-7 |
化学式 | C30H32F2N4O3 |
分子量 | 534.6 |
密度 | 1.37±0.1 g/cm3(Predicted) |
沸点 | 761.0±60.0 °C(Predicted) |
溶解度 | DMSO : 80 mg/mL母液保存:分装冻存,避免反复冻融;-20℃,1个月;-80℃,6个月(稀释后溶液温度低保存可能会析出,尽量现用现配) |
酸度系数 | 4.40±0.10(Predicted) |
存储条件 | -20℃ |
产品用途 | Inobrodib (CCS1477) 是一种口服活性的、有效且选择性强的 p300/CBP 抑制剂。Inobrodib 与 p300 和 CBP 结合,Kd 值为 1.3 和 1.7 nM,与 Kd 为 222 nM 的 BRD4 相比,具有 170/130 倍的选择性。Inobrodib 抑制前列腺癌细胞系的细胞增殖并降低雄激素受体 (AR) 和 C-MYC 调节的基因表达。 |
靶点 | p300/CBP |
参考资料 展开查看 | 1: Rasool RU, Natesan R, Asangani IA. Toppling the HAT to Treat Lethal Prostate Cancer. Cancer Discov. 2021 May;11(5):1011-1013. doi: 10.1158/2159-8290.CD-21-0184. PMID: 33947717. 2: Welti J, Sharp A, Brooks N, Yuan W, McNair C, Chand SN, Pal A, Figueiredo I, Riisnaes R, Gurel B, Rekowski J, Bogdan D, West W, Young B, Raja M, Prosser A, Lane J, Thomson S, Worthington J, Onions S, Shannon J, Paoletta S, Brown R, Smyth D, Harbottle GW, Gil VS, Miranda S, Crespo M, Ferreira A, Pereira R, Tunariu N, Carreira S, Neeb AJ, Ning J, Swain A, Taddei D; SU2C/PCF International Prostate Cancer Dream Team, Schiewer MJ, Knudsen KE, Pegg N, de Bono JS. Targeting the p300/CBP Axis in Lethal Prostate Cancer. Cancer Discov. 2021 May;11(5):1118-1137. doi: 10.1158/2159-8290.CD-20-0751. Epub 2021 Jan 11. PMID: 33431496; PMCID: PMC8102310. 3: He ZX, Wei BF, Zhang X, Gong YP, Ma LY, Zhao W. Current development of CBP/p300 inhibitors in the last decade. Eur J Med Chem. 2021 Jan 1;209:112861. doi: 10.1016/j.ejmech.2020.112861. Epub 2020 Oct 1. PMID: 33045661. |
1mg | 5mg | 10mg | |
---|---|---|---|
1 mM | 1.871 ml | 9.353 ml | 18.705 ml |
5 mM | 0.374 ml | 1.871 ml | 3.741 ml |
10 mM | 0.187 ml | 0.935 ml | 1.871 ml |
5 mM | 0.037 ml | 0.187 ml | 0.374 ml |
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