A TACC3 inhibitor
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BO-264

Item No. 36611

Technical Information
Formal Name
N-[3-(4-methoxyphenyl)-5-isoxazolyl]-2-(4-morpholinyl)-4-pyrimidinamine
CAS Number
2408648-20-2
Molecular Formula
C18H19N5O3
Formula Weight
Purity
≥98%
A solid
DMF: 10 mg/mlDMSO: 1 mg/mlEthanol: insolPBS (pH 7.2): insol
λmax
252, 312 nm
SMILES
COC(C=C1)=CC=C1C2=NOC(NC3=NC(N4CCOCC4)=NC=C3)=C2
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)
InChi Key
WRCGBYNVBFVRTN-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    Product Description

    BO-264 is a transforming acidic coiled-coil containing protein 3 (TACC3) inhibitor.1 It binds to TACC3 in thermal shift and drug affinity responsive target stability (DARTS) assays and inhibits the growth of JIMT-1, HCC1954, MDA-MB-231, MDA-MB-436, and CAL-51 cancer cells (IC50s = 0.19, 0.16, 0.12, 0.13, and 0.36 µM, respectively). BO-264 is cytotoxic to RT4 cells that endogenously express TACC3-FGFR3 fusion proteins (IC50 = 3.66 µM). It induces mitotic arrest, apoptosis, and aberrant spindle formation and reduces centrosomal localization of TACC3 in JIMT-1 cells. BO-264 (25 mg/kg) reduces tumor volume and increases median survival in an EMT6 mouse xenograft model.

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Akbulut, O., Lengerli, D., Saatci, O., et alA highly potent TACC3 inhibitor as a novel anticancer drug candidate. Mol. Cancer Ther. 19(6), 1243-1254 (2020).