DTP3 TFA is a potent and selective GADD45β/MKK7 (growth arrest and DNA-damage-inducible β/mitogen-activated protein kinase kinase 7) inhibitor. DTP3 TFA targets an essential, cancer-selective cell-survival module downstream of the NF-κB pathway.
体外研究
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.
Western Blot Analysis
Cell Line:
Multiple myeloma (MM) cell lines
Concentration:
10 μM
Incubation Time:
1, 3, 5, 14, 21 days
Result:
Caused the appearance of phosphorylated JNK, as early as 24 hours.
体内研究
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.
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.
Animal Model:
6 to 8-week old male NOD/SCID mice (NOD.CB17-Prkdcscid/IcrCrl; Charles River)
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
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.
运输条件
Room temperature in continental US; may vary elsewhere.