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MedKoo CAT#: 408094
CAS#: 2408648-20-2
Description: BO-264 is a highly potent and orally active transforming acidic coiled-coil 3 (TACC3) inhibitor with an IC50 of 188 nM and a Kd of 1.5 nM. BO-264 demonstrated superior anti-proliferative activity to the two currently reported TACC3 inhibitors, especially in aggressive breast cancer subtypes, basal and HER2+, via spindle assembly checkpoint (SAC)-dependent mitotic arrest, DNA damage and apoptosis, while the cytotoxicity against normal breast cells was negligible.
MedKoo Cat#: 408094
Name: BO-264
CAS#: 2408648-20-2
Chemical Formula: C18H19N5O3
Exact Mass: 353.1488
Molecular Weight: 353.382
Elemental Analysis: C, 61.18; H, 5.42; N, 19.82; O, 13.58
Synonym: BO-264; BO 264; BO264;
IUPAC/Chemical Name: 3-(4-methoxyphenyl)-N-(2-morpholinopyrimidin-4-yl)isoxazol-5-amine
InChi Key: WRCGBYNVBFVRTN-UHFFFAOYSA-N
InChi Code: InChI=1S/C18H19N5O3/c1-24-14-4-2-13(3-5-14)15-12-17(26-22-15)20-16-6-7-19-18(21-16)23-8-10-25-11-9-23/h2-7,12H,8-11H2,1H3,(H,19,20,21)
SMILES Code: COC1=CC=C(C2=NOC(NC3=NC(N4CCOCC4)=NC=C3)=C2)C=C1
TACC3, a TACC family member, is frequently upregulated in a broad spectrum of cancers, including breast cancer. It plays critical roles in protecting microtubule stability and centrosome integrity that is often dysregulated in cancers; therefore, making TACC3 a highly attractive therapeutic target.
BO-264 significantly decreased centrosomal TACC3 during both mitosis and interphase. BO-264 displayed potent anti-proliferative activity (~90% have less than 1 μM GI50 value) in the NCI-60 cell line panel compromising 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.
Akbulut O, Lengerli D, Saatci O, et al. A Highly Potent TACC3 Inhibitor as a Novel Anti-cancer Drug Candidate [published online ahead of print, 2020 Mar 26]. Mol Cancer Ther. 2020;molcanther.0957.2019. doi:10.1158/1535-7163.MCT-19-0957
