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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[1]. | [in vivo]
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]. | Animal Model: | OVCAR3 ovarian cancer CDX model constructed by injecting OVCAR3 ovarian cancer cell line into immunodeficient mice[2] | | Dosage: | 100 or 200 mg/kg | | Administration: | Intraperitoneal injection (i.p.), 100 mg/kg twice daily or 200 mg/kg once daily for up to 42 days | | Result: | Resulted in tumor stasis (100 mg/kg twice daily), achieved 89% tumor growth inhibition (TGI), and did not cause significant weight loss (200 mg/kg once daily). |
| Animal Model: | GA0103 gastric cancer PDX model constructed by injecting patient-derived GA0103 gastric cancer tumor into immunodeficient mice[2] | | Dosage: | 100 mg/kg | | Administration: | Intraperitoneal injection (i.p.), twice daily for 56 days | | Result: | Resulted in tumor stasis and did not cause significant weight loss. |
| Animal Model: | CCNE1-amplified gastric adenocarcinoma PDX (GA0103) in BALB/c nude mice model[1] | | Dosage: | 25, 50 或 100 mg/kg | | Administration: | Oral gavage (p.o.), twice daily, for 56 days | | Result: | inhibited the growth of tumor in a dose-dependent manner, with 100 mg/kg group showing tumor regression. |
| [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. DOI:10.1158/2159-8290.CD-23-0954
[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. |
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