DTP3-TFA-DataSheet-生命科學(xué)試劑-MedChemExpress

1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEDTP3 TFACat. No.: HY-100538A分式: CHFNO分量: 639.62作靶點: DNA/RNA Synthesis; JNK作通路: Cell Cycle/DNA Damage; MAPK/ERK Pathway儲存式: -20C, protect from light* In solvent : -80C, 6 months; -20C, 1 month (protect fromlight)溶解性數(shù)據(jù)體外實驗 H2O : 1

2、00 mg/mL (156.34 mM; Need ultrasonic)DMSO : 50 mg/mL (78.17 mM; Need ultrasonic)Mass Solvent1 mg 5 mg 10 mg Concentration制備儲備液1 mM 1.5634 mL 7.8171 mL 15.6343 mL5 mM 0.3127 mL 1.5634 mL 3.1269 mL10 mM 0.1563 mL 0.7817 mL 1.5634 mL請根據(jù)產(chǎn)品在不同溶劑中的溶解度，選擇合適的溶劑配制儲備液，并請注意儲備液的保存式和期限。體內(nèi)實驗 請根據(jù)您的實驗動物和給藥式選擇適當(dāng)?shù)娜芙獍?/p>

3、，配制前請先配制澄的儲備液，再依次添加助溶劑(為保證實驗結(jié)果的可靠性，體內(nèi)實驗的作液，建議您現(xiàn)現(xiàn)配，當(dāng)天使；澄的儲備液可以根據(jù)儲存條件，適當(dāng)保存；以下溶劑前的百分指該溶劑在您配制終溶液中的體積占)：1. 請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% salineSolubility: 2.5 mg/mL (3.91 mM); Clear solution2. 請依序添加每種溶劑： 10% DMSO 90% (20% SBE-CD in saline)Solubility: 2.5 mg/mL (3.91 mM); Clear solution3.

4、 請依序添加每種溶劑： 10% DMSO 90% corn oilSolubility: 2.5 mg/mL (3.91 mM); Clear solution1/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEBIOLOGICAL ACTIVITY物活性 DTP3 TFA種有效且選擇性的 GADD45/MKK7 (長停滯和 DNA 損傷誘導(dǎo) /促分裂原活化的蛋激酶激酶 7) 抑制劑。DTP3 TFA 靶向 NF-B 途徑下游的種重的癌癥選擇性細(xì)胞存活模塊。IC50 & Target GADD45/MKK7 1體外研究 DTP3 (10 M; 1-

5、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 2Cell Line: Multiple myeloma (MM) cell linesConcentration: 10 MIncubation Time: 1, 3, 5, 14, 21 daysResult: Caused t

6、he appearance of phosphorylated JNK, as early as 24 hours.體內(nèi)研究 DTP3 TFA (s.c.; 14.5 mg/kg/day; 28 days) has shown a dramatic shrinkage of the tumors, and virtuallyeradicates established subcutaneous myeloma xenografts in mice 2.DTP3 TFA (intravenous injection; 10 mg/kg/day) has t1/2 of 1.26 hours, C

7、L of 27.13 ML/min/kg, and Vd of2.80 L/kg 2.Animal Model: 6 to 8-week old male NOD/SCID mice (NOD.CB17-Prkdcscid/IcrCrl; Charles River) 2Dosage: 14.5 mg/kgAdministration: S.c.; daily; 28 daysResult: Had shown a dramatic shrinkage of the tumors.Animal Model: CD1 male mice of 25-30 g 2Dosage: 10 mg/kg

8、(Pharmacokinetic Study)Administration: Intravenous injectionResult: Had t1/2 of 1.26 hours, CL of 27.13 ML/min/kg, and Vd of 2.80 L/kg.REFERENCES1. Tornatore L, et al. Preclinical toxicology and safety pharmacology of the first-in-class GADD45/MKK7inhibitor and clinical candidate,DTP3. Toxicol Rep. 2019 Apr 19;6:369-379.2. Tornatore L, et al. Cancer-selective targeting of the NF-B survival pathway with GADD45/MKK7 inhibitors. Cancer Cell. 2014 Oct13;26(4):495-508.2/3 Master of Small Molecules 您邊的抑制劑師www.MedChemEMcePdfHeightCaution: Product has not been fully validated for medical a