INX-315 is an orally active and selective CDK2 inhibitor that induces cell cycle arrest in the G1 phase. INX-315 reduces CDK2 substrate phosphorylation and inhibits tumor growth in a dose-dependent manner in xenograft mouse models. INX-315 may be used in cancer research.
INX-315 (30-300 nM, 24 hours) inhibits cell cycle progression in OVCAR3 and MKN1 cells by reducing retinoblastoma protein (Rb) phosphorylation[1].INX-315 (0.3 nM to 10 μM, 6 days) inhibits cell proliferation in CCNE1-amplified ovarian carcinoma cell line[1].
INX-315 (100 mg/kg, p.o., twice daily for 56 days) effectively inhibits tumor growth in a gastric adenocarcinoma BALB/c nude mouse model[1].INX-315 (100 mg/kg twice daily or 200 mg/kg once daily, i.p.) demonstrates significant tumor inhibition in the OVCAR3 ovarian cancer CDX model with good tolerance[2].INX-315 (100 mg/kg twice daily, i.p.) demonstrates significant antitumor activity in the GA0103 gastric cancer PDX model with good tolerance[2].
References:
[1]. Dietrich C, et al. INX-315, a selective CDK2 inhibitor, induces cell cycle arrest and senescence in solid tumors. Cancer Discov. 2023 Dec 4.
[2]. Trub A G, et al. INX-315, a potent and selective CDK2 inhibitor, demonstrates robust antitumor activity in CCNE1-amplified cancers[J]. Cancer Research, 2023, 83(7_Supplement): 5994-5994.