In Vitro: IP2 (35 µM) shows immunomodulatory activity in murine MCA205 fibrosarcoma cells. IP2 (35 µM) increases in the intron-derived SL8 antigen presentation. IP2 (10 µM; 72 h) shows non-cytotoxic for cancer cells. IP2 (10 µM) shows selectivity against three G-protein coupled receptor ADRB1 (35%), HRH2 (40%), and OPRD1 (53%), and inhibits the three enzymes of COX1 (52.8%), PDE3A (84.8%), and PDE4D2 (87.2%). IP2 (10 µM) dose not induce immunogenic cell death hallmarks in human osteosarcoma U2OS cells.
In Vivo: IP2 (0.711 mg/kg for i.p. for mice; 9.103 mg/kg for i.v. for nice; 26.76 mg/kg for i.v. for dog) shows a high bioavailability in mice. IP2 (50, 100, 250, 500 mg/kg; i.p.) shows very well toleration in C57BL/6 mice. IP2 (2.5 mg/kg; i.v.) induces tumor growth defects in C57BL/6 mice. IP2 (5 mg/kg; intratumor injection; three times per week for 2 weeks) induces tumor growth defects in C57BL/6 mice. Pharmacokinetic Parameters of IP2 in Male C57BL/6J mice and male beagle dog.
Dose (mg/kg)
Cmax (ng/mL)
Tmax (h)
T1/2 (h)
CL (mL/min/kg)
F %
MRT0-t (h)
AUCtot (ng/mL·h)
AUCextra (%)
ip mice
9.103
2078
0.0833
0.8
154
86
0.7
982.3
1.3
iv mice
0.711
322.7
0.0833
1.1
133
0.9
88.8
15.2
iv dog
26.76
272 (µg/mL)
0.0833
3.8
0.69
3.8
654.7 (µg/mL·h)
0.9
Male C57BL/6J mice and male beagle dog; 0.711 mg/kg for i.p. for mice; 9.103 mg/kg for i.v. for mice; 26.76 mg/kg for i.v. for dog.