BBT594 is a potent receptor tyrosine kinase RET inhibitor , used for cancer treatment.
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. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Spécifications
Spécifications et pureté
10mM in DMSO
Mécanismes biochimiques et physiologiques
BBT594 is a potent receptor tyrosine kinase RET inhibitor , used for cancer treatment.
Conditions de stockage de stockage
Store at -80°C
Expédié en
Dry ice packs + Cold packs
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