Selinexor (KPT-330)

Catalog No.S7252 Synonyms: ATG-010

For research use only.

Selinexor (KPT-330, ATG-010) is an orally bioavailable selective CRM1 inhibitor. Phase 2.

Selinexor (KPT-330) Chemical Structure

CAS No. 1393477-72-9

Selleck's Selinexor (KPT-330) has been cited by 59 publications

Purity & Quality Control

Choose Selective CRM1 Inhibitors

Biological Activity

Description Selinexor (KPT-330, ATG-010) 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 MVrGeY5kfGmxbjDhd5NigQ>? M36xVFAvOSEQvF2= MoDCNlQhcCCxcjC0PEBp MV7pcoR2[2W|IHTp[oZmemWwdHnhcEBCc3Ric3nncoFtcW6pLTDhcoQhdWW2YXLvcIl{dS2jc4PvZ4lifGWmIHflcoUh\XiycnXzd4lwdiCycn;mbYxmey5? Ml7LQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB7OEezPFAoRjNyOUi3N|gxRC:jPh?=
MCF-7 NFG2cZlHfW6ldHnvckBie3OjeR?= NWnzTVBOOC5zIN88US=> NYfmcm5DOjRiaDDvdkA1QCCq NEfKXppqdmS3Y3XzJIRq\m[ncnXueIlidCCDa4Sgd4lodmGuaX7nMUBidmRibXX0ZYJwdGm|bT3hd5Nw[2mjdHXkJIdmdmViZYjwdoV{e2mxbjDwdo9ncWyncz6= Mlm3QIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB7OEezPFAoRjNyOUi3N|gxRC:jPh?=
THP-1 M3nmW2Z2dmO2aX;uJIF{e2G7 Mn;UNlQhcA>? Moe1R4xm[X[jZ3Wgc4YhWEGUUDDhcoQh[2G|cHHz[UA{KHencnWgd5Rzd26pbImg[Y5p[W6lZXSgbY4hfGinIHPvcYJqdmG2aX;uJJRz\WG2bXXueEB4cGWwIHPvcZBiemWmIITvJGFDXC1zOUmgc5IhU1CWLUOzNEBidG:wZR?= M1jZdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyNUm2N|k5Lz5|MEW5OlM6QDxxYU6=
OCI-AML3 MWTGeY5kfGmxbjDhd5NigQ>? NV\RXGdUOjRiaB?= Mkf1R4xm[X[jZ3Wgc4YhWEGUUDDhcoQh[2G|cHHz[UA{KHencnWgd5Rzd26pbImg[Y5p[W6lZXSgbY4hfGinIHPvcYJqdmG2aX;uJJRz\WG2bXXueEB4cGWwIHPvcZBiemWmIITvJGFDXC1zOUmgc5IhU1CWLUOzNEBidG:wZR?= NX\ufow2RGFidHHy[4V1RSehYnzhcosoKGi{ZX[9K4h1fHC|Oj:vdJVjdWWmLn7jZokvdmyvLn7pbE5od3ZxM{C1PVY{QThpPkOwOVk3Ozl6PD;hQi=>
MV4-11 MX7GeY5kfGmxbjDhd5NigQ>? NVvWUHMxOjRiaB?= M12xWWNt\WG4YXflJI9nKFCDUmCgZY5lKGOjc4Dhd4UhOyC5ZYLlJJN1em:wZ3z5JIVvcGGwY3XkJIlvKHSqZTDjc41jcW6jdHnvckB1emWjdH3lcpQhf2inbjDjc41x[XKnZDD0c{BCSlRvMUm5JI9zKEuSVD2zN|Ah[WyxbnW= M3HWdlxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyNUm2N|k5Lz5|MEW5OlM6QDxxYU6=
T24 MWPD[YxtKH[rYXLpcIl1gSCjc4PhfS=> M{POR|AtKDBwMEGsJFAvOSxiMTFOwG0> M17sTVczKGh? NVz6WXIz[2WubDD2bYFjcWyrdImg[IVkemWjc3XkJIlvKGFiZH;z[UBl\XCnbnTlcpQhdWGwbnXy MYG8ZUB1[XKpZYS9K39jdGGwazegbJJm\j1paIT0dJM7Ny:ydXLt[YQvdmOkaT7ucI0vdmmqLnfvek8{ODN2OU[1NEc,OzB|NEm2OVA9N2F-
J82 MmG5R4VtdCC4aXHibYxqfHliYYPzZZk> MUKwMEAxNjBzLDCwMlEtKDFizszN NYPhXWsxPzJiaB?= MWLj[YxtKH[rYXLpcIl1gSCmZXPy[YF{\WRiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? M1HzdVxiKHSjcnfleF0oZ2KuYX7rK{BpemWoPTfoeJRxezpxL4D1Zo1m\C6wY3LpMo5tdS6waXiu[493NzNyM{S5OlUxLz5|MEO0PVY2ODxxYU6=
TCCSUP NY[xUm9PS2WubDD2bYFjcWyrdImgZZN{[Xl? M{fhc|AtKDBwMEGsJFAvOSxiMTFOwG0> MWW3NkBp NGDsNXhk\WyuII\pZYJqdGm2eTDk[YNz\WG|ZXSgbY4h[SCmb4PlJIRmeGWwZHXueEBu[W6wZYK= NHP6[Ww9[SC2YYLn[ZQ:L1:kbHHub{chcHKnZk2nbJR1eHN8Lz;weYJu\WRwbnPibU5vdG1wbnnoModwfi9|MEO0PVY2OCd-M{CzOFk3PTB:L3G+
UM-UC-3 NVrmTVg1S2WubDD2bYFjcWyrdImgZZN{[Xl? M{TzVlAtKDBwMEGsJFAvOSxiMTFOwG0> M3TtV|czKGh? MUXj[YxtKH[rYXLpcIl1gSCmZXPy[YF{\WRiaX6gZUBld3OnIHTldIVv\GWwdDDtZY5v\XJ? Mo\iQIEhfGG{Z3X0QUdg[myjbnunJIhz\WZ;J3j0eJB{Qi9xcIXicYVlNm6lYnmucoxuNm6raD7nc5YwOzB|NEm2OVAoRjNyM{S5OlUxRC:jPh?=
Assay
Methods Test Index PMID
Western blot CHEK1 / MLH1 / MSH2 / PMS2 / Rad51 ; 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 ; AXL / phospho-AKT / phospho-P70S6K / AKT / P70S6K ; p53 / CDKN1a / Survivin 30112106 28852098 25948791
Immunofluorescence XPO1 / tubulin ; NPM1 / PU.1 30349650 30015632
Growth inhibition assay Cell viability 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 (from reference)

Cell Research:[1]
  • 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.
Animal Research:[1]
  • Animal Models: T-ALL and AML orthograft mouse model
  • Dosages: 20 -25 mg/kg
  • Administration: p.o.

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+40%PEG 300+5% Tween80 +ddH2O
For best results, use promptly after mixing.

4mg/mL

Chemical Information

Molecular Weight 443.31
Formula

C17H11F6N7O

CAS No. 1393477-72-9
Storage 3 years -20°C powder
2 years -80°C in solvent
Smiles C1=CN=C(C=N1)NNC(=O)C=CN2C=NC(=N2)C3=CC(=CC(=C3)C(F)(F)F)C(F)(F)F

In vivo Formulation Calculator (Clear solution)

Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)

mg/kg 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.)

% DMSO % % Tween 80 % ddH2O
%DMSO %

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 ddH2O, 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.

Molarity Calculator

Mass Concentration Volume Molecular Weight

Clinical Trial Information

NCT Number Recruitment Interventions Conditions Sponsor/Collaborators Start Date Phases
NCT05170789 Not yet recruiting Drug: Elotuzumab Selinexor and Dexamethasone (ESd) Relapsed Multiple Myeloma|Refractory Multiple Myeloma Tulane University School of Medicine|Karyopharm Therapeutics Inc|Tulane University January 7 2022 Phase 2
NCT05035745 Recruiting Drug: Talazoparib|Drug: Selinexor Advanced Refractory Solid Tumors|Advanced Triple Negative Breast Cancers|Metastatic Triple Negative Breast Cancers National University Hospital Singapore March 1 2021 Phase 1|Phase 2

(data from https://clinicaltrials.gov, updated on 2022-01-17)

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.

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