BO-264
作者：齊岳
發布時間：2023-08-25
08:58:42
點擊數：
產品名稱：BO-264
產品描述：
| 產品描述 | BO-264 is a highly potent and orally active inhibitor of transforming acidic coiled-coil 3 (TACC3, IC50 of 188 nM and a Kd of 1.5 nM). |
| 靶點活性 | Transforming acidic coiled-coil 3 (TACC3):188 nM (IC50), TACC3:1.5 nM (Kd) |
| 體外活性 | BO-264 demonstrated superior antiproliferative activity to the two currently reported TACC3 inhibitors, especially in aggressive breast cancer subtypes, basal and HER2+, via spindle assembly checkpoint-dependent mitotic arrest, DNA damage, and apoptosis, while the cytotoxicity against normal breast cells was negligible.?Furthermore, BO-264 significantly decreased centrosomal TACC3 during both mitosis and interphase.?BO-264 displayed potent antiproliferative activity ( 90% have less than 1 μmol/L GI50 value) in the NCI-60 cell line panel compromising of nine different cancer types.?Noteworthy, BO-264 significantly inhibited the growth of cells harboring FGFR3-TACC3 fusion, an oncogenic driver in diverse malignancies.?Importantly, its oral administration significantly impaired tumor growth in immunocompromised and immunocompetent breast and colon cancer mouse models, and increased survival without any major toxicity.?Finally, TACC3 expression has been identified as strong independent prognostic factor in breast cancer and strongly prognostic in several different cancers. |
| 分子量 | 353.382 |
| 分子式 | C18H19N5O3 |
| CAS No. | 2408648-20-2 |
存儲
Powder: -20°C for 3 years | In solvent: -80°C for 2 years
溶解度
DMSO: 50 mg/mL (141.49 mM),Need ultrasonic
( < 1 mg/mL refers to the product slightly soluble or insoluble )
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公司介紹：
西安齊岳生物科技有限公司是集化學科研和定制與一體的高科技化學公司。業務范圍包括化學試劑和產品的研發、生產、銷售等。涉及產品為通用試劑的分銷、非通用試劑的定制與研發，涵蓋生物科技、化學品、中間體和化工材料等領域。
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