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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Cited by 7 Publications

4 Customer Reviews

  • 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.

    Whole cell lysates from THP-1, OCI-AML3, and MV4-11 cells treated with ABT-199 or KPT-330, alone or in combination, for 24 hours, were subjected to Western blotting and probed with the indicated antibodies.

    J Cell Mol Med, 2018, doi:10.1111/jcmm.13886. Selinexor (KPT-330) purchased from Selleck.

  • Inhibitors of nuclear export reduce cell proliferation and induce apoptosis of SI-NET cell lines CNDT2.5 and KRJ-I. b, Treatments with KPT-330/selinexor. *, p < 0.05.

    BMC Cancer, 2018, 18(1):764. Selinexor (KPT-330) purchased from Selleck.

    Localization of NF-κB p65 in the cytoplasm and nuclear was detected by immunofluorescence. Confocal images were taken after cells were stained with the anti-p65 Ab and Alexa Flour 594-conjugated secondary Ab. Cell nuclei were stained with DAPI (blue).

    Biochem Biophys Res Commun, 2018, 503(3):1773-1779. 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]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
BT474 cells NUnSOo9NTnWwY4Tpc44h[XO|YYm= NGf1RoMxNjFizszN NHvHPZMzPCCqIH;yJFQ5KGh? NXS2VWRlcW6mdXPld{BlcW[oZYLlcpRq[WxiQXv0JJNq\26jbHnu[{0h[W6mIH3leIFjd2yrc32tZZN{d2OrYYTl[EBo\W6nIHX4dJJme3Orb36gdJJw\mmuZYOu NI\lWGQ{ODl6N{O4NC=>
MCF-7 M2fON2Z2dmO2aX;uJIF{e2G7 MlvvNE4yKM7:TR?= MmKwNlQhcCCxcjC0PEBp MkHabY5lfWOnczDkbYZn\XKnboTpZYwhSWu2IIPp[45idGmwZz2gZY5lKG2ndHHic4xqe21vYYPzc4Nq[XSnZDDn[Y5mKGW6cILld5Nqd25icILv[olt\XNw M1vlWVMxQTh5M{iw
THP-1 NXPLblRbTnWwY4Tpc44h[XO|YYm= MUOyOEBp MlLQR4xm[X[jZ3Wgc4YhWEGUUDDhcoQh[2G|cHHz[UA{KHencnWgd5Rzd26pbImg[Y5p[W6lZXSgbY4hfGinIHPvcYJqdmG2aX;uJJRz\WG2bXXueEB4cGWwIHPvcZBiemWmIITvJGFDXC1zOUmgc5IhU1CWLUOzNEBidG:wZR?= MnWwN|A2QTZ|OUi=
OCI-AML3 MlywSpVv[3Srb36gZZN{[Xl? NGXTSYMzPCCq MXXDcIVifmGpZTDv[kBRSVKSIHHu[EBk[XOyYYPlJFMhf2W{ZTDzeJJwdmeueTDlcohidmOnZDDpckB1cGViY3;tZolv[XSrb36geJJm[XSvZX70JJdp\W5iY3;tdIFz\WRidH:gRWJVNTF7OTDvdkBMWFRvM{OwJIFtd26n MUGzNFU6PjN7OB?=
MV4-11 NIjZfYZHfW6ldHnvckBie3OjeR?= NVnxcGpPOjRiaB?= NHnpTHBEdGWjdnHn[UBw\iCSQWLQJIFv\CClYYPwZZNmKDNid3Xy[UB{fHKxbnfsfUBmdmijbnPl[EBqdiC2aHWgZ49u[mmwYYTpc44hfHKnYYTt[Y51KHeqZX6gZ49ueGG{ZXSgeI8hSUKWLUG5PUBweiCNUGStN|MxKGGub37l NGmyV4o{ODV7NkO5PC=>
T24 M3PrOGNmdGxidnnhZoltcXS7IHHzd4F6 MXmwMEAxNjBzLDCwMlEtKDFizszN NVjFbXgzPzJiaB?= MX;j[YxtKH[rYXLpcIl1gSCmZXPy[YF{\WRiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NIPyO4c{ODN2OU[1NC=>
J82 NFTFfHJE\WyuII\pZYJqdGm2eTDhd5NigQ>? NWHycYZIOCxiMD6wNUwhOC5zLDCxJO69VQ>? M4nYfFczKGh? MWnj[YxtKH[rYXLpcIl1gSCmZXPy[YF{\WRiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NWPmTottOzB|NEm2OVA>
TCCSUP Mn;uR4VtdCC4aXHibYxqfHliYYPzZZk> NYD4VVBVOCxiMD6wNUwhOC5zLDCxJO69VQ>? NV30ZZI{PzJiaB?= MoPiZ4VtdCC4aXHibYxqfHliZHXjdoVie2WmIHnuJIEh\G:|ZTDk[ZBmdmSnboSgcYFvdmW{ M{Hz[|MxOzR7NkWw
UM-UC-3 NV[zXXlFS2WubDD2bYFjcWyrdImgZZN{[Xl? Mmr6NEwhOC5yMTygNE4yNCBzIN88US=> NGS5PJo4OiCq M1TXfYNmdGxidnnhZoltcXS7IHTlZ5Jm[XOnZDDpckBiKGSxc3Wg[IVx\W6mZX70JI1idm6nch?= M2nZb|MxOzR7NkWw

... Click to View More Cell Line Experimental Data

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

Molarity Calculator

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Calculate the mass, volume or concentration required for a solution. The Selleck molarity 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
NCT02471911 Recruiting Diffuse Large B-Cell Lymphoma Weill Medical College of Cornell University|Karyopharm Therapeutics Inc November 2015 Phase 1
NCT02471911 Recruiting Diffuse Large B-Cell Lymphoma Weill Medical College of Cornell University|Karyopharm Therapeutics Inc November 2015 Phase 1
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
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
NCT02213133 Terminated Squamous Cell Carcinoma Karyopharm Therapeutics Inc July 2014 Phase 2
NCT02213133 Terminated Squamous Cell Carcinoma Karyopharm Therapeutics Inc July 2014 Phase 2

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

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID