1、Hotline: 400-820-3792Inhibitors Agonists Screening Librarieswww.MedChemEBBT594Cat. No.: HY-18840CAS No.: 882405-89-2Synonyms: NVP-BBT594分式: CHFNO分量: 569.58作靶點(diǎn): RET作通路: Protein Tyrosine Kinase/RTK儲(chǔ)存式: Powder -20C 3 years4C 2 yearsIn solvent -80C 6 months-20C 1 month溶解性數(shù)據(jù)體外實(shí)驗(yàn) DMSO : 33 mg/mL (57.94 mM

2、)* means soluble, but saturation unknown.Mass Solvent1 mg 5 mg 10 mg Concentration制備儲(chǔ)備液1 mM 1.7557 mL 8.7784 mL 17.5568 mL5 mM 0.3511 mL 1.7557 mL 3.5114 mL10 mM 0.1756 mL 0.8778 mL 1.7557 mL請(qǐng)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(chǔ)備液，并請(qǐng)注意儲(chǔ)備液的保存式和期限。BIOLOGICAL ACTIVITY物活性 BBT594種有效的受體酪氨酸激酶 RET 抑制劑，常于癌癥研究。體外研究NVP-B

3、BT594 blocks the GDNF-mediated enhancement of MCF7-LTED cell viability in 2D culture and 3Dcolony formation. The addition of 10 pM E2, to mimic the E2 level in post-menopausal patients that haverelapsed on AI treatment and ceased AI therapy, increases 3D colony formation of both MCF7 and MCF7-1/2 Ma

4、ster of Small Molecules 您邊的抑制劑師www.MedChemELTED cells, and this effect is efficiently reverted by NVP-BBT594. Parental T47D cells cultured in presence oflow level E2, GFR1/GDNF stimulation results in increased 3D colony formation, which is significantlyreverted by NVP-BBT594. NVP-BBT594 targets GDNF

5、-RET signaling and sensitizes MCF7-2A cells toletrozole treatment. NVP-BBT594 impairs GDNF-mediated RET downstream signaling and significantlyenhances the antiproliferative effects of letrozole 1. NVP-BBT594 shows the highest suppression of GDNF-induced RET signaling, as assessed by RET, ERK1/2, AKT

6、 and ER phosphorylation. NVP-AST487 andNVP-BBT594 have comparable RET inhibitory activity in wild-type MCF7 cells 2.REFERENCES1. Morandi A, et al. GDNF-RET signaling in ER-positive breast cancers is a key determinant of response and resistance to aromataseinhibitors. Cancer Res. 2013 Jun 15;73(12):3

7、783-952. Andreucci E, et al. Targeting the receptor tyrosine kinase RET in combination with aromatase inhibitors in ER positive breast cancerxenografts. Oncotarget. 2016 Sep 2. doi: 10.18632/oncotarget.11826. Epub ahead of printMcePdfHeightCaution: Product has not been fully validated for medical applications.For research use