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KPT-330 目录号 GC12467

CRM1 inhibitor, orally bioavailable and selective

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥714.00
现货
5mg
¥462.00
现货
50mg
¥2,982.00
现货

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Sample solution is provided at 25 µL, 10mM.

质量管理

Quality Control & SDS

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实验参考方法

Cell experiment [1, 2]:

Cell lines

NSCLC cells lines (A549, H460, H1975, PC14, H1299, and H23); MiaPaCa-2 and L3.6pl cells

Preparation method

The solubility of this compound in DMSO is >10 mM. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months.

Reacting condition

1.0 μmol/L for 24h; or 0.1-1.0 μmol/L

Applications

KPT-330 inhibited proliferation, induced cell cycle arrest and apoptosis-related proteins in 11 NSCLC cells lines (A549, H460, H1975, PC14, H1299, and H23). Moreover, KPT-330 (0.1-1.0 μmol/L) dose-dependently inhibited the growth of MiaPaCa-2 and L3.6pl cells.

Animal experiment [1, 2]:

Animal models

Human NSCLC H1975 tumor xenograft model; human metastatic pancreatic cancer cells are orthotopically injected into the pancreas of mice model

Dosage form

10 mg/kg, oral treatment, thrice weekly for 4 weeks; or 10, 20 mg/kg p.o., 3/week

Applications

KPT-330(10 mg/kg) showed antitumour activity against human non-small cell lung cancer. Moreover, KPT-330 potentiated the antitumor activity of gemcitabine in human pancreatic cancer through inhibition of tumor growth, induction of apoptosis, and depletion of the antiapoptotic proteins.

Other notes

Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal.

References:

1. Sun, H., Hattori, N., Chien, W., Sun, Q., Sudo, M., GL, E. L., Ding, L., Lim, S. L., Shacham, S., Kauffman, M., Nakamaki, T. and Koeffler, H. P. (2014) KPT-330 has antitumour activity against non-small cell lung cancer. Br J Cancer. 111, 281-291

2. Kazim, S., Malafa, M. P., Coppola, D., Husain, K., Zibadi, S., Kashyap, T., Crochiere, M., Landesman, Y., Rashal, T., Sullivan, D. M. and Mahipal, A. (2015) Selective Nuclear Export Inhibitor KPT-330 Enhances the Antitumor Activity of Gemcitabine in Human Pancreatic Cancer. Mol Cancer Ther. 14, 1570-1581

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Chemical Properties

Cas No. 1393477-72-9 SDF
别名 N/A
化学名 (Z)-3-[3-[3,5-bis(trifluoromethyl)phenyl]-1,2,4-triazol-1-yl]-N'-pyrazin-2-ylprop-2-enehydrazide
Canonical SMILES C1=CN=C(C=N1)NNC(=O)C=CN2C=NC(=N2)C3=CC(=CC(=C3)C(F)(F)F)C(F)(F)F
分子式 C17H11F6N7O 分子量 443.31
溶解度 ≥15.15mg/mL in DMSO 储存条件 Store at -20°C
General tips For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months.
Shipping Condition Evaluation sample solution : ship with blue ice
All other available size: ship with RT , or blue ice upon request

产品描述

KPT-330, analog of KPT-185, is a selective inhibitor of CRM1 [1].

Chromosomemaintenance protein 1 (CRM1) is a nuclear export receptor involved in the active transport of transcription factors, cell-cycle regulators, tumor suppressors and RNA molecules. In cancer, CRM1 is overexpression and overactive transport [1].

KPT-330 is an orally bioavailable and selective CRM1 inhibitor. In kidney cancer (RCC) cells, KPT-330 inhibited CRM1 and increased nuclear localization of p21. Then, KPT-330 induced apoptosis and inhibited cells growth [2]. In human non-small cell lung cancer (NSCLC) cells, KPT-330 inhibited cell proliferation and induced the expression of apoptosis-related proteins and cell cycle arrest [3].

In mice bearing MiaPaCa-2 xenograft model, KPT-330 (20 mg/kg) significantly inhibited tumor growth without significant toxicity or body weight loss. Also, KPT-330 increased PAR-4, pro-apoptotic Bax, cleaved PARP and caspase-3. These results suggested that KPT-330 induced apoptosis by the activation of PAR-4 signaling [1]. In mice bearing human NSCLC xenografts, KPT-330 significantly inhibited tumor growth [3].

References:
[1].  Azmi AS, Aboukameel A, Bao B, et al. Selective inhibitors of nuclear export block pancreatic cancer cell proliferation and reduce tumor growth in mice. Gastroenterology, 2013, 144(2): 447-456.
[2].  Wettersten HI, Landesman Y, Friedlander S, et al. Specific inhibition of the nuclear exporter exportin-1 attenuates kidney cancer growth. PLoS One, 2014, 9(12): e113867.
[3].  Sun H, Hattori N, Chien W, et al. KPT-330 has antitumour activity against non-small cell lung cancer. Br J Cancer, 2014, 111(2): 281-291.