产品
编 号:F755545
分子式:C28H36F3N7O7
分子量:639.62
产品类型
结构图
CAS No: 2759216-46-9
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产品详情
生物活性:
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.
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.