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CAS No.: 1185763-69-2

NVP-BVU972 Catalog No. CSN17159

Synonyms: BVN-972;BVU-972

NVP-BVU972 is a potent and selective c-Met inhibitor with IC50 of 14 nM with antitumor effects.

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技术信息

生物活性

描述Receptor tyrosine kinases (RTKs) has been implicated in the development and progression of many types of cancer. The hepatocyte growth factor (HGF) RTK, as known as MET, is required for various morphogenetic events in both embryonic and adult organisms. c-Met is a receptor-type tyrosine kinase, which is involved in a wide range of cellular responses such as proliferation, motility, migration and invasion. c-MET RTK and its ligand, hepatocyte growth factor (HGF), exist in most solid tumors and c-MET signaling has been documented in a wide range of human malignancies^[3]. NVP-BVU972 is a novel selective c-MET kinase inhibitor with an IC₅₀ of 14 nM which better than 10 μM in kinase RON. Cell lines were seeded with viral supernatants for 14 to 16h in the presence of 6 μg/mL polybrene and cell lines replaced with growth medium subsequently to obtain cell lysates for protein expression levels and activation status of Met. The result showed that NVP-BVU972 potently prevents the growth of the MET gene amplified cell lines GTL-16, MKN-45 and EBC-1 with IC₅₀ values of 66 nM, 82 nM and 32 nM, respectively, which indicate that NVP-BVU972 possessed great sensitivity to MET. Moreover, after BaF3 cell line was induced with N-ethyl-N-nitrosourea (ENU) for 16h, NVP-BVU972 was added to a final concentration of 600, 1,200, 2,400, 4,800, or 9,600 nM, suggesting that Y1230 and D1228 mutations give rise to both shifts to greater than 129 nM of the measured IC₅₀ values^[4].
作用机制The π-stacking of the core imidazo-pyridazine moiety of NVP-BVU972 with the aromatic side chain of Y1230 binds to the c-MET kinase.
参考文献

[1] Shin JS, Hong SW, et al. NPS-1034, a novel MET inhibitor, inhibits the activated MET receptor and its constitutively active mutants. Invest New Drugs. 2014 Jun;32(3):389-99.
[2] Tiedt R, Degenkolbe E, et al. A drug resistance screen using a selective MET inhibitor reveals a spectrum of mutations that partially overlap with activating mutations found in cancer patients. Cancer Res. 2011 Aug 1;71(15):5255-64.
[3] Organ SL, Tsao MS. An overview of the c-MET signaling pathway. Ther Adv Med Oncol. 2011 Nov;3(1 Suppl):S7-S19. doi: 10.1177/1758834011422556. PMID: 22128289; PMCID: PMC3225017.
[4] Lutterbach B, Zeng Q, Davis LJ, Hatch H, Hang G, Kohl NE, Gibbs JB, Pan BS. Lung cancer cell lines harboring MET gene amplification are dependent on Met for growth and survival. Cancer Res. 2007 Mar 1;67(5):2081-8. doi: 10.1158/0008-5472.CAN-06-3495. Erratum in: Cancer Res. 2007 Apr 15;67(8):3987. PMID: 17332337.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.9379 mL
- 14.6895 mL
- 29.3789 mL
- 5 mM
- 0.5876 mL
- 2.9379 mL
- 5.8758 mL
- 10 mM
- 0.2938 mL
- 1.4689 mL
- 2.9379 mL

技术信息

CAS号

1185763-69-2

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C20H16N6

运输

蓝冰

分子量

340.38

别名

BVN-972;BVU-972

溶解度

DMSO	50.0 mg/mL (146.9 mM)
Water	insoluble

动物实验配方

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