KPT-330 |
Catalog No.GC12467
One-Click Copy Product Info
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KPT-330 (Selinexor) is an orally active selective inhibitor of nuclear export (SINE) compound that inhibits the nuclear export protein XPO1 (also known as CRM1).
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 1393477-72-9
Sample solution is provided at 25 µL, 10mM.
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KPT-330 (Selinexor) is an orally active selective inhibitor of nuclear export (SINE) compound that inhibits the nuclear export protein XPO1 (also known as CRM1) [1]. KPT-330 covalently binds to the Cys528 site of XPO1, resulting in its irreversible inactivation [2]. KPT-330 can induce apoptosis, has inhibitory activity against various types of cancer cells, and can also enhance the effects of other chemotherapeutic drugs [3].
In vitro, KPT-330 (0-1000 nM) treatment of non-small cell lung cancer (NSCLC) cell lines for 72 h dose-dependently induced growth inhibition, promoted G1 phase arrest and apoptosis, and stimulated the activation of caspase-3 and caspase-9 [4]. KPT-330 (0-1000 nM) treatment of prostate cancer (PCa) cell lines for 72 h dose-dependently induced cell growth inhibition with IC50 values ranging from 43-700nM [5].
In vivo, oral treatment of mice with non-small cell lung cancer with KPT-330 (10 mg/kg) for 4 weeks significantly reduced tumor volume, reduced Ki-67-positive cells, and increased the percentage of TUNEL-positive cells, and this therapy had a synergistic effect with cisplatin [4]. Oral treatment of mice with pancreatic cancer with KPT-330 (20 mg/kg) for 3 weeks significantly reduced the expression of CRM1 protein in tumor samples, induced p27 nuclear staining, and enhanced the expression of the pro-apoptotic protein Bax [6].
References:
[1] Wang A Y, Liu H. The past, present, and future of CRM1/XPO1 inhibitors[J]. Stem cell investigation, 2019.
[2]Houghton P J, Kang M, Reynolds C P, et al. Pediatric Preclinical Testing Program (PPTP) stage 1 evaluation of the XPO1/CRM1 inhibitor KPT-330[J]. AACR (abstract LB-354), 2013.
[3]Liu S, Qiao W, Sun Q, et al. Chromosome region maintenance 1 (XPO1/CRM1) as an anticancer target and discovery of its inhibitor[J]. Journal of Medicinal Chemistry, 2021, 64(21): 15534-15548.
[4]Sun H, Hattori N, Chien W, et al. KPT-330 has antitumour activity against non-small cell lung cancer[J]. British journal of cancer, 2014, 111(2): 281-291.
[5]Gravina G L, Mancini A, Sanita P, et al. KPT-330, a potent and selective exportin-1 (XPO-1) inhibitor, shows antitumor effects modulating the expression of cyclin D1 and survivin in prostate cancer models[J]. BMC cancer, 2015, 15: 1-19.
[6]Kazim S, Malafa M P, Coppola D, et al. Selective nuclear export inhibitor KPT-330 enhances the antitumor activity of gemcitabine in human pancreatic cancer[J]. Molecular cancer therapeutics, 2015, 14(7): 1570-1581.
Cell experiment [1]: | |
Cell lines | NSCLC cells |
Preparation method | NSCLC cells were seeded (3×103 cells per well) in 96-well plates, treated with different concentrations of KPT-330 (0, 0.1, 1, 10, 100, and 1000 nM, 72 h), and growth inhibition was measured by MTT assay. |
Reaction Conditions | 0-1000 nM ; 72 h |
Applications | KPT-330 (0.1-1000 nM) induced a dose-dependent growth inhibition after 72 h of exposure. |
Animal experiment [2]: | |
Animal models | Female athymic nude mice |
Preparation method | Female athymic nude mice were injected with luciferase-tagged L3.6pl human metastatic pancreatic cancer cells orthotopically into the pancreas. Mice were divided into four treatment groups of 5 animals each: group 1 was treated with vehicle; group 2 was treated with KPT-330 (20 mg/kg p.o., 3/week); group 3 was treated with gemcitabine (100mg/kg i.p., 2/week); and group 4 was treated with KPT-330 (10 mg/kg p.o., 3/week) + gemcitabine (50 mg/kg i.p., 2/week) for 4 weeks. The treatment was initiated 1 week after orthotopic injection of cell lines. |
Dosage form | 20mg/kg; p.o. |
Applications | CRM1 protein expression was significantly depleted after treatment with KPT-330 alone and in combination with gemcitabine, but was not changed with gemcitabine treatment alone. |
References: | |
| Cas No. | 1393477-72-9 | SDF | |
| Chemical Name | (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 | ||
| Formula | C17H11F6N7O | M.Wt | 443.31 |
| Solubility | ≥ 15.15mg/mL in DMSO | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.2558 mL | 11.2788 mL | 22.5576 mL |
| 5 mM | 451.2 μL | 2.2558 mL | 4.5115 mL |
| 10 mM | 225.6 μL | 1.1279 mL | 2.2558 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
g
μL
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL saline, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
- View current batch:
- Purity: >98.00% Appearance: A solid
- COA (Certificate of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 18 reference(s) in Google Scholar.)