Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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).
パッケージサイズ | 在庫状況 | 単価(税別) | |||
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1 mg | 在庫あり | ¥ 10,000 | |||
5 mg | 在庫あり | ¥ 22,500 | |||
10 mg | 在庫あり | ¥ 41,000 | |||
25 mg | 在庫あり | ¥ 64,000 | |||
50 mg | 在庫あり | ¥ 85,500 | |||
100 mg | 在庫あり | ¥ 137,000 | |||
1 mL * 10 mM (in DMSO) | 在庫あり | ¥ 27,000 |
説明 | 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). |
ターゲット&IC50 | TACC3:188 nM (IC50), TACC3:1.5 nM (Kd) |
In vitro | 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 | 353.38 |
分子式 | C18H19N5O3 |
CAS No. | 2408648-20-2 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 50 mg/mL (141.49 mM), Sonication is recommended.
You can also refer to dose conversion for different animals. 詳細
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BO-264 2408648-20-2 Angiogenesis Apoptosis Tyrosine Kinase/Adaptors FGFR inhibit cytotoxicity antitumor Fibroblast growth factor receptor Inhibitor TACC3 spindle abnormalities ERK1/2 DNA phosphorylation BO 264 FGFR3-TACC3 mitotic damage anti-proliferative BO264 inhibitor