Selinexor (KPT-330)

Catalog No.S7252

Selinexor (KPT-330) Chemical Structure

Molecular Weight(MW): 443.31

Selinexor (KPT-330) is an orally bioavailable selective CRM1 inhibitor. Phase 2.

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1 Customer Review

  • Bortezomib and KPT330 enhance apoptosis in HCT116 and RKO cells. A, HCT116 and RKO cells were treated with bortezomib, KPT330, or their combination for 48 hours at the indicated concentrations. The cells were subsequently stained with Annexin V, apoptotic cells were distinguished by flow cytometric analysis. B, Measurement of caspase-3 and -7 by means of a luminometric assay was performed in cells receiving the same treatment.

    Mol Cancer Ther, 2017, 16(4):717-728. Selinexor (KPT-330) purchased from Selleck.

Purity & Quality Control

Choose Selective CRM1 Inhibitors

Biological Activity

Description Selinexor (KPT-330) is an orally bioavailable selective CRM1 inhibitor. Phase 2.
Targets
CRM1 [1]
(Cell-free assay)
In vitro

As the clinical candidate analog of KPT-185, KPT-330 exhibits similar effects on the viability of T-ALL cells and elicits rapid apoptotic response. KPT-330 also reduces cell growth in MOLT-4, Jurkat, HBP-ALL, KOPTK-1, SKW-3, and DND-41 cell lines, with IC50 values of 34-203 nM. [1]

In vivo KPT-330 dramatically suppresses the growth of T-ALL cells (MOLT-4) and AML cells (MV4–11) in vivo, with little toxicity to normal haematopoietic cells. [1] In SCID mice with diffuse human MM bone lesions, KPT-330 inhibits MM-induced bone lysis and prolongs survival. Moreover, KPT-330 directly impairs osteoclastogenesis and bone resorption by blocking RANKL-induced NF-κB and NFATc1, with minimal impact on osteoblasts and BMSCs. [2]

Protocol

Cell Research:[1]
+ Expand
  • Cell lines: MOLT-4, Jurkat, HBP-ALL, KOPTK-1, SKW-3, and DND-41 cell lines
  • Concentrations: ~1 μM
  • Incubation Time: 72 hours
  • Method: Cell lines are cultured in RPMI 1640 medium, supplemented with 10% fetal bovine serum and penicillin/streptomycin. Cell Titer Glo assay is used to assess cell viability upon treatment with either dimethyl sulfoxide (DMSO) or KPT-330. Cells are plated at a density of 10 000 cells per well in a 96-well plate and incubated with DMSO or increasing concentrations of KPT-330. The cell viability is measured after 72 h exposure to KPT-330 and reported as a percentage of DMSO control cells. Jurkat cells that overexpress BCL2 are generated using MSCV-IRES-GFP retroviral expression system. Jurkat cells infected with BCL2 or control vector viruses are sorted by flow cytometry and the expression of BCL2 confirmed by Western blot analysis using BCL2 antibody.
    (Only for Reference)
Animal Research:[1]
+ Expand
  • Animal Models: T-ALL and AML orthograft mouse model
  • Formulation: Pluronic F-68/PVP-K29/32
  • Dosages: 20 -25 mg/kg
  • Administration: p.o.
    (Only for Reference)

Solubility (25°C)

In vitro DMSO 88 mg/mL (198.5 mM)
Ethanol 40 mg/mL (90.23 mM)
Water Insoluble
In vivo Add solvents to the product individually and in order(Data is from Selleck tests instead of citations):
2% DMSO+49% PEG 300+ddH2O
For best results, use promptly after mixing.
5mg/mL

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 443.31
Formula

C17H11F6N7O

CAS No. 1393477-72-9
Storage powder
in solvent
Synonyms N/A

Bio Calculators

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Calculate the mass, volume or concentration required for a solution. The Selleck molarity calculator is based on the following equation:

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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*When preparing stock solutions, please always use the batch-specific molecular weight of the product found on the via label and MSDS / COA (available on product pages).

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Dilution Calculator

Calculate the dilution required to prepare a stock solution. The Selleck dilution calculator is based on the following equation:

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This equation is commonly abbreviated as: C1V1 = C2V2 ( Input Output )

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Clinical Trial Information

NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT02530476 Active not recruiting Leukemia|Acute Myeloid Leukemia M.D. Anderson Cancer Center|Karyopharm Therapeutics Inc|National Cancer Institute (NCI) December 8 2015 Phase 1|Phase 2
NCT02402764 Active not recruiting Breast Cancer H. Lee Moffitt Cancer Center and Research Institute|Karyopharm Therapeutics Inc July 8 2015 Phase 2
NCT02228525 Active not recruiting Myelodysplastic Syndromes Memorial Sloan Kettering Cancer Center|M.D. Anderson Cancer Center|Columbia University|Karyopharm Therapeutics Inc August 27 2014 Phase 2
NCT02120222 Recruiting Recurrent Melanoma Kari Kendra|Karyopharm Therapeutics Inc|Ohio State University Comprehensive Cancer Center May 27 2014 Phase 1
NCT03095612 Recruiting Non-small Cell Lung Cancer University of Texas Southwestern Medical Center|Karyopharm Therapeutics Inc March 22 2018 Phase 1|Phase 2
NCT02831686 Recruiting Multiple Myeloma|Relapsed and/or Refractory Multiple Myeloma Memorial Sloan Kettering Cancer Center|Karyopharm Therapeutics Inc|Millennium Pharmaceuticals Inc. July 2016 Phase 1

Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

Tel: +1-832-582-8158 Ext:3

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID