1414455-21-2

IBL-302 (AMU302) is an orally available dual-signaling inhibitor of PIM and PI3K/AKT/mTOR with activity against breast cancer and neuroblastoma. IBL-302 demonstrated in vivo efficacy in a nude mouse xenograft model, inhibiting trastuzumab (HY-P9907) resistance challenges. IBL-302 also enhances the effects of common cytotoxic chemotherapy drugs cisplatin (HY-17394), doxorubicin (HY-15142A), and etoposide (HY-13629)[1][2][3].

[1] Kennedy SP et al. Preclinical evaluation of a novel triple-acting PIM/PI3K/mTOR inhibitor, IBL-302, in breast cancer. Oncogene. 2020 Apr;39(14):3028-3040. DOI:10.1038/s41388-020-1202-y
[2] Kennedy S P, et al. Evaluation of dual-acting PIM/PI3K inhibitor IBL-302 in preclinical breast cancer models[J]. Cancer Research, 2018, 78(13_Supplement): 2932-2932.
[3] Martínez-González S, et al. Macrocyclization as a Source of Desired Polypharmacology. Discovery of Triple PI3K/mTOR/PIM Inhibitors. ACS Med Chem Lett. 2021 Nov 2;12(11):1794-1801. DOI:10.1021/acsmedchemlett.1c00412