ChemicalBook CAS DataBase List 2745060-92-6

2745060-92-6

Name	INX-315
CAS	2745060-92-6
Molecular Formula	C19H21N7O3S
Molecular Weight	427.48
MOL File	2745060-92-6.mol

Chemical Properties

density	1.712±0.14 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted)
form	Solid
pka	9.847±0.12(predicted)
color	White to off-white

Safety Data

Symbol(GHS)	GHS07
Signal word	Warning
Hazard statements	H302-H315-H319
Precautionary statements	P501-P270-P264-P280-P302+P352-P337+P313-P305+P351+P338-P362+P364-P332+P313-P301+P312+P330

Hazard Information

Uses

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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