Discovery of XNW9015, a potent, selective, and CNS-penetrating covalent inhibitor of CDK7 with excellent in vivo antitumor activities (AACR 2023)
In the Palbociclib-resistant breast cancer cell line MCF-7, XNW9015 exhibited antiproliferative activity, with an IC50 of 81nM, while neither Palbociclib nor Fulvestrant can inhibit the cell viability...XNW9015 exhibited superior rodent pharmacokinetic characteristics when compared to LY3405105 (Eli Lilly and Company, WO2019099298)...In summary, XNW9015 has demonstrated potent in vitro and in vivo antitumor effects, favorable pharmacokinetic and toxicological properties. XNW9015 has become a potential clinical candidate for cancer therapeutics, both as monotherapies and in combination settings.