The PK and PD study of NR-V04. (A) PK parameters of NR-V04 in WT mice with three mice per group; one experiment. i.v. or IV, intraveneous injection; i.p. or IP, intraperitoneal injection; Tmax, time to drug peak comtration; Cmax, peak concentratin; AUC, area under the curve; T1/2, mean half-life; CL, clearance rate; MRT, mean residence time; Vss, steady state volume of distribution; F, fraction of bioavailability. (B) NR-V04 induces long-lasting degradation of NR4A1 in MC38 tumors. Mice bearing MC38 tumors were treated with two-dose administration of NR-V04 via i.p. (IP) injection at 1.8 mg/kg, and tumors were collected at indicated timepoints. Tumor lysates were analyzed by immunoblotting with each lane representing an individual tumor lysate; two experiments. (C) Immunoblotting showing NR4A1 degradation in MC38 tumors upon termination. MC38 tumor–bearing mice were treated with vehicle, 1.8 mg/kg NR-V04, or 0.75 mg/kg celastrol treatment (equivalent to 1.67 μmol/kg) every 4 days until experimental endpoints. Tumor tissues were collected for lysate collection and immunoblotting. Two to four biological samples per group, two experiments. Source data are available for this figure: SourceData F6.
Figure 6.

The PK and PD study of NR-V04. (A) PK parameters of NR-V04 in WT mice with three mice per group; one experiment. i.v. or IV, intraveneous injection; i.p. or IP, intraperitoneal injection; Tmax, time to drug peak comtration; Cmax, peak concentratin; AUC, area under the curve; T1/2, mean half-life; CL, clearance rate; MRT, mean residence time; Vss, steady state volume of distribution; F, fraction of bioavailability. (B) NR-V04 induces long-lasting degradation of NR4A1 in MC38 tumors. Mice bearing MC38 tumors were treated with two-dose administration of NR-V04 via i.p. (IP) injection at 1.8 mg/kg, and tumors were collected at indicated timepoints. Tumor lysates were analyzed by immunoblotting with each lane representing an individual tumor lysate; two experiments. (C) Immunoblotting showing NR4A1 degradation in MC38 tumors upon termination. MC38 tumor–bearing mice were treated with vehicle, 1.8 mg/kg NR-V04, or 0.75 mg/kg celastrol treatment (equivalent to 1.67 μmol/kg) every 4 days until experimental endpoints. Tumor tissues were collected for lysate collection and immunoblotting. Two to four biological samples per group, two experiments. Source data are available for this figure: SourceData F6.

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