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CAS No. : 882405-89-2
MCE 国际站:BBT594
产品活性:BBT594 是一种有效的受体酪氨酸激酶 RET 抑制剂,常用于癌症研究。
研究领域:Protein Tyrosine Kinase/RTK
作用靶点:RET
In Vitro: NVP-BBT594 blocks the GDNF-mediated enhancement of MCF7-LTED cell viability in 2D culture and 3D colony formation. The addition of 10 pM E2, to mimic the E2 level in post-menopausal patients that have relapsed on AI treatment and ceased AI therapy, increases 3D colony formation of both MCF7 and MCF7-LTED cells, and this effect is efficiently reverted by NVP-BBT594. Parental T47D cells cultured in presence of low level E2, GFRα1/GDNF stimulation results in increased 3D colony formation, which is significantly reverted by NVP-BBT594. NVP-BBT594 targets GDNF-RET signaling and sensitizes MCF7-2A cells to letrozole treatment. NVP-BBT594 impairs GDNF-mediated RET downstream signaling and significantly enhances the antiproliferative effects of letrozole. NVP-BBT594 shows the highest suppression of GDNF-induced RET signaling, as assessed by RET, ERK1/2, AKT and ER phosphorylation. NVP-AST487 and NVP-BBT594 have comparable RET inhibitory activity in wild-type MCF7 cells.
相关产品:Bioactive Compound Library Plus | Kinase Inhibitor Library | Protein Tyrosine Kinase Compound Library | Anti-Cancer Compound Library | Anti-Lung Cancer Compound Library | Anti-Liver Cancer Compound Library | Membrane Protein-targeted Compound Library | Membrane Receptor-targeted Compound Library | trans-Pralsetinib | RET-IN-24 | BT-13 | RET-IN-16 | WF-47-JS03 | Pyrazoloadenine | GSK3179106 | RET-IN-1 | Lenvatinib-d5 | Pz-1 | Regorafenib monohydrate | RET-IN-14 | AD57 | AD80 | FLT3/ITD-IN-4 | RET-IN-18 | Regorafenib-13C,d3 | RET V804M-IN-1 | RET-IN-19 | Enbezotinib | RET-IN-6 | BT44 | TG101209 | Regorafenib-d3 | Amuvatinib | WHI-P180 | RET-IN-10
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