包装 | 价格(元) |
1mg | 电议 |
5mg | 电议 |
10mg | 电议 |
25mg | 电议 |
50mg | 电议 |
100mg | 电议 |
分子式 | C28H36F3N7O7 |
分子量 | 639.62 |
溶解度 | Water: 100 mg/mL (156.34 mM); DMSO: 50 mg/mL (78.17 mM) |
储存条件 | -20°C, protect from light |
General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while. |
Shipping Condition | Evaluation sample solution : ship with blue ice All other available size: ship with RT , or blue ice upon request |
产品描述 | 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[1]. 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]. Western Blot Analysis[2] Cell Line: Multiple myeloma (MM) cell lines 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] [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. |