BBT594(Synonyms: NVP-BBT594)

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BBT594 (Synonyms: NVP-BBT594) 纯度: 99.94%

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。

BBT594(Synonyms: NVP-BBT594)

BBT594 Chemical Structure

CAS No. : 882405-89-2

规格 价格 是否有货 数量
10 mM * 1 mL in DMSO ¥2757 In-stock
5 mg ¥2200 In-stock
10 mg ¥3600 In-stock
50 mg ¥9900 In-stock
100 mg 询价

* Please select Quantity before adding items.

BBT594 相关产品

相关化合物库:

  • 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

生物活性

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

体外研究
(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[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].

上海金畔生物科技有限公司 has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

569.58

Formula

C28H30F3N7O3

CAS 号

882405-89-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : ≥ 33 mg/mL (57.94 mM)

* “≥” means soluble, but saturation unknown.

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 1.7557 mL 8.7784 mL 17.5568 mL
5 mM 0.3511 mL 1.7557 mL 3.5114 mL
10 mM 0.1756 mL 0.8778 mL 1.7557 mL

*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

参考文献
  • [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]

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