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BBT594
本产品不向个人销售,仅用作科学研究,不用于任何人体实验及非科研性质的动物实验。
BBT594图片
CAS NO:882405-89-2
包装与价格:
包装价格(元)
10mM (in 1mL DMSO)电议
5mg电议
10mg电议
50mg电议

产品介绍
BBT594 是一种有效的受体酪氨酸激酶 RET 抑制剂,用于癌症治疗。
Cas No.882405-89-2
别名NVP-BBT594
Canonical SMILESO=C(N1CCC2=C1C=CC(OC3=NC=NC(NC(C)=O)=C3)=C2)NC4=CC=C(CN5CCN(C)CC5)C(C(F)(F)F)=C4
分子式C28H30F3N7O3
分子量569.58
溶解度DMSO : ≥ 33 mg/mL (57.94 mM)
储存条件Store at -20°C
General tipsFor obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.
Shipping ConditionEvaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request
产品描述

BBT594 is a potent receptor tyrosine kinase RET inhibitor, used for cancer treatment.

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[1]. 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[2].

References:
[1]. Morandi A, et al. GDNF-RET signaling in ER-positive breast cancers is a key determinant of response and resistance to aromatase inhibitors. Cancer Res. 2013 Jun 15;73(12):3783-95.
[2]. Andreucci E, et al. Targeting the receptor tyrosine kinase RET in combination with aromatase inhibitors in ER positive breast cancer xenografts. Oncotarget. 2016 Sep 2. doi: 10.18632/oncotarget.11826. [Epub ahead of print]