DTP3 TFA (s.c.; 14.5 mg/kg/day; 28 days) has shown a dramatic shrinkage of the tumors, and virtually eradicates established subcutaneous myeloma xenografts in mice[2]. DTP3 TFA (intravenous injection; 10 mg/kg/day) has t1/2 of 1.26 hours, CL of 27.13 ML/min/kg, and Vd of 2.80 L/kg[2]. Animal Model: 6 to 8-week old male NOD/SCID mice (NOD.CB17-Prkdcscid/IcrCrl; Charles River)[2] Dosage: 14.5 mg/kg Administration: S.c.; daily; 28 days Result: Had shown a dramatic shrinkage of the tumors. Animal Model: CD1 male mice of 25-30 g[2] Dosage: 10 mg/kg (Pharmacokinetic Study) Administration: Intravenous injection Result: Had t1/2 of 1.26 hours, CL of 27.13 ML/min/kg, and Vd of 2.80 L/kg.
In Vitro
DTP3 (10 μM; 1-21 days) causes the potent and tumor-selective induction of JNK activation and apoptosis, as shown by the appearance of phosphorylated JNK, as early as 24 hours[2].
Kinase Assay
Cell Assay
Animal Administration
References
[1]. Tornatore L, et al. Preclinical toxicology and safety pharmacology of the first-in-class GADD45β/MKK7inhibitor and clinical candidate, DTP3. Toxicol Rep. 2019 Apr 19;6:369-379.
[2]. Tornatore L, et al. Cancer-selective targeting of the NF-κB survival pathway with GADD45β/MKK7 inhibitors. Cancer Cell. 2014 Oct 13;26(4):495-508.
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