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 12 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 NFTsb|NHfW6ldHnvckBie3OjeR?= M3rwclAvOSEQvF2= M3i2flI1KGhib4KgOFghcA>? NX\4Tnk6cW6mdXPld{BlcW[oZYLlcpRq[WxiQXv0JJNq\26jbHnu[{0h[W6mIH3leIFjd2yrc32tZZN{d2OrYYTl[EBo\W6nIHX4dJJme3Orb36gdJJw\mmuZYOu NHvmdFE{ODl6N{O4NC=>
MCF-7 MXvGeY5kfGmxbjDhd5NigQ>? MnPMNE4yKM7:TR?= MVGyOEBpKG:{IES4JIg> NUTmRXdbcW6mdXPld{BlcW[oZYLlcpRq[WxiQXv0JJNq\26jbHnu[{0h[W6mIH3leIFjd2yrc32tZZN{d2OrYYTl[EBo\W6nIHX4dJJme3Orb36gdJJw\mmuZYOu NFzU[mw{ODl6N{O4NC=>
THP-1 NHPMNnlHfW6ldHnvckBie3OjeR?= MYGyOEBp M2\rPWNt\WG4YXflJI9nKFCDUmCgZY5lKGOjc4Dhd4UhOyC5ZYLlJJN1em:wZ3z5JIVvcGGwY3XkJIlvKHSqZTDjc41jcW6jdHnvckB1emWjdH3lcpQhf2inbjDjc41x[XKnZDD0c{BCSlRvMUm5JI9zKEuSVD2zN|Ah[WyxbnW= MXSzNFU6PjN7OB?=
OCI-AML3 M2jobGZ2dmO2aX;uJIF{e2G7 MV6yOEBp NY\6Ro9tS2ynYY\h[4Uhd2ZiUFHSVEBidmRiY3HzdIF{\SB|IIfldoUhe3S{b37ncJkh\W6qYX7j[YQhcW5idHjlJINwdWKrbnH0bY9vKHS{ZXH0cYVvfCC5aHXuJINwdXCjcnXkJJRwKEGEVD2xPVkhd3JiS2DUMVM{OCCjbH;u[S=> Ml;QN|A2QTZ|OUi=
MV4-11 M1fsNmZ2dmO2aX;uJIF{e2G7 NGDxPZozPCCq MYfDcIVifmGpZTDv[kBRSVKSIHHu[EBk[XOyYYPlJFMhf2W{ZTDzeJJwdmeueTDlcohidmOnZDDpckB1cGViY3;tZolv[XSrb36geJJm[XSvZX70JJdp\W5iY3;tdIFz\WRidH:gRWJVNTF7OTDvdkBMWFRvM{OwJIFtd26n NFTEUoY{ODV7NkO5PC=>
T24 MUfD[YxtKH[rYXLpcIl1gSCjc4PhfS=> NWTQeGp2OCxiMD6wNUwhOC5zLDCxJO69VQ>? NHTD[oI4OiCq MUXj[YxtKH[rYXLpcIl1gSCmZXPy[YF{\WRiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MnTzN|A{PDl4NUC=
J82 M4XqdGNmdGxidnnhZoltcXS7IHHzd4F6 MUOwMEAxNjBzLDCwMlEtKDFizszN NWDhcoZ4PzJiaB?= MYXj[YxtKH[rYXLpcIl1gSCmZXPy[YF{\WRiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? MWqzNFM1QTZ3MB?=
TCCSUP MXXD[YxtKH[rYXLpcIl1gSCjc4PhfS=> Ml;FNEwhOC5yMTygNE4yNCBzIN88US=> M17RVFczKGh? MYLj[YxtKH[rYXLpcIl1gSCmZXPy[YF{\WRiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? NY\ufow5OzB|NEm2OVA>
UM-UC-3 MWXD[YxtKH[rYXLpcIl1gSCjc4PhfS=> MonZNEwhOC5yMTygNE4yNCBzIN88US=> MUS3NkBp NUHpO5BE[2WubDD2bYFjcWyrdImg[IVkemWjc3XkJIlvKGFiZH;z[UBl\XCnbnTlcpQhdWGwbnXy MlO3N|A{PDl4NUC=

... Click to View More Cell Line Experimental Data

Assay
Methods Test Index PMID
Western blot
CHEK1 / MLH1 / MSH2 / PMS2 / Rad51; 

PubMed: 30112106     


Western blot of proteins from whole cell lysates of HT1080 cells treated with 0, 0.1, or 1 μM selinexor and ASPS-KY cells treated with 0, 1, or 10 μM selinexor confirmed the RPPA results suggesting down-regulation of CHEK1, MLH1, MSH2, PMS2 and Rad51 protein levels from selinexor treatment in both cell lines.

XPO1 / Cyclin B1 / Cyclin D1 / c-Myc / c-Met / Mcl-1 / p21 Waf1/Cip1 / p53/ Cleaved PARP / Cleaved caspase-9 / Cleaved caspase-3 / Aurora-B; 

PubMed: 28852098     


OGK-M, HTH83, CAL62 and T238 cells were treated with either selinexor (1,000 nM) or DMSO for 24 h. Lysates were analyzed by western blot analysis for the indicated cell cycle and apoptosis proteins (GAPDH, internal loading control).

AXL / phospho-AKT / phospho-P70S6K / AKT / P70S6K; 

PubMed: 28852098     


HTH83 and CAL62 cells were cultured with either selinexor (1,000 nM) or diluent control (DMSO) for 24 h, and the whole-cell lysate was subjected to western blot analysis for AXL, p-AKT, total AKT, p-P70S6K and total P70S6K.

p53 / CDKN1a / Survivin; 

PubMed: 25948791     


Representative western immunoblotting showing nuclear and cytosolic fractions of XPO1/ CRM1, p53, CDKN1a and survivin in DMPM cells exposed to selinexor (IC50). β-actin and TBP were used to confirm equal protein loading on the gel and to show the relative purity of the nuclear fractions.

30112106 28852098 25948791
Immunofluorescence
XPO1 / tubulin; 

PubMed: 30349650     


Immunofluorescent detection of XPO1 (green) in cells treated with vehicle and selinexor. Cells were plated on chamber slides and they were treated with either vehicle or selinexor for 48 hours. Tubulin (red) and DAPI (blue) served to define the nuclear and cytoplasmic compartment, respectively. V = vehicle, S = selinexor.

NPM1 / PU.1; 

PubMed: 30015632     


IF for NPM1 and PU.1 in vehicle- versus selinexor-treated NPM1-mutated AML cells. DAPI was used to stain for nuclei. Images by Nikon Eclipse 400 microscope; original magnification, ×630.

30349650 30015632
Growth inhibition assay
Cell viability; 

PubMed: 28852098     


Cells were treated with selinexor at indicated concentrations for 72 h, and growth inhibition was measured by MTT assay. Results are expressed as mean value ± SD; n = 4. 

28852098
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

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Clinical Trial Information

NCT Number Recruitment interventions Conditions Sponsor/Collaborators Start Date Phases
NCT02091245 Active not recruiting Drug: KPT-330 Relapsed Acute Lymphoblastic Leukemia (ALL)|Refractory Acute Lymphoblastic Leukemia (ALL)|Relapsed Acute Myelogenous Leukemia (AML)|Refractory Acute Myelogenous Leukemia (AML)|Relapsed Mixed Lineage Leukemia|Refractory Mixed Lineage Leukemia|Relapsed Biphenotypic Leukemia|Refractory Biphenotypic Leukemia|Chronic Myelogenous Leukemia (CML) in Blast Crisis Dana-Farber Cancer Institute|William Lawrence and Blanche Hughes Foundation|Karyopharm Therapeutics Inc March 2014 Phase 1
NCT02078349 Unknown status Drug: KPT-330 Solid Tumors National University Hospital Singapore|Karyopharm Therapeutics Inc February 2014 Phase 1
NCT02025985 Completed Drug: Selinexor Ovarian Carcinoma|Endometrial Carcinoma|Cervical Carcinoma|Breast Cancer Karyopharm Therapeutics Inc January 2014 Phase 2
NCT01896505 Completed Drug: KCP-330 Sarcoma Karyopharm Therapeutics Inc July 2013 Phase 1
NCT01607905 Completed Drug: KPT-330 Solid Tumor Karyopharm Therapeutics Inc June 2012 Phase 1
NCT01607892 Completed Drug: KPT-330 Hematological Malignancies Karyopharm Therapeutics Inc June 2012 Phase 1

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID