XL495 is an potent, selective and orally active PKMYT1 inhibitor. XL495 inhibits CDK1 Thr14 phosphorylation and induces KAP1 Ser824 phosphorylation in xenograft tumors. XL495 reduces tumor growth in colorectal and breast cancer xenograft models, and achieves tumor regression with DNA-damaging agents in colorectal cancer xenograft models. XL495 can be used for the research of cancer, such as breast cancer and colorectal cancer [1] [2].
In Vivo, XL495 (p.o.) shows antitumor activity in a breast cancer cell line-derived xenograft (CDX) model.
References:
[1]. Zhu J, et al. Enantioselective Suzuki-Miyaura Chemistry: Route Evolution for the Synthesis of PKMYT1 Inhibitor XL495. J Org Chem. 2026 Apr 17;91(15):5379-5387.
[2]. Gwinn D, et al. XL495 is a potent, selective, and orally bioavailable inhibitor of PKMYT1[J]. Cancer Research, 2025, 85(8_Supplement_1): 1733-1733.
In Vivo, XL495 (p.o.) shows antitumor activity in a breast cancer cell line-derived xenograft (CDX) model.
References:
[1]. Zhu J, et al. Enantioselective Suzuki-Miyaura Chemistry: Route Evolution for the Synthesis of PKMYT1 Inhibitor XL495. J Org Chem. 2026 Apr 17;91(15):5379-5387.
[2]. Gwinn D, et al. XL495 is a potent, selective, and orally bioavailable inhibitor of PKMYT1[J]. Cancer Research, 2025, 85(8_Supplement_1): 1733-1733.