Home Transmembrane Transporters CRM1 inhibitor Selinexor (KPT-330) For research use only.

Selinexor (KPT-330)

Synonyms: ATG-010

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

Selinexor (KPT-330) Chemical Structure

Selinexor (KPT-330) Chemical Structure

CAS No. 1393477-72-9

Purity & Quality Control

Selinexor (KPT-330) Related Products

Cell Data

Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
BT474 cells Function assay 0.1 μM 24 h or 48 h induces differential Akt signaling- and metabolism-associated gene expression profiles. 30987380
MCF-7 Function assay 0.1 μM 24 h or 48 h induces differential Akt signaling- and metabolism-associated gene expression profiles. 30987380
THP-1 Function assay 24 h Cleavage of PARP and caspase 3 were strongly enhanced in the combination treatment when compared to ABT-199 or KPT-330 alone 30596398
OCI-AML3 Function assay 24 h Cleavage of PARP and caspase 3 were strongly enhanced in the combination treatment when compared to ABT-199 or KPT-330 alone 30596398
MV4-11 Function assay 24 h Cleavage of PARP and caspase 3 were strongly enhanced in the combination treatment when compared to ABT-199 or KPT-330 alone 30596398
T24 Cell viability assay 0, 0.01, 0.1, 1 μM 72 h cell viability decreased in a dose dependent manner 30349650
J82 Cell viability assay 0, 0.01, 0.1, 1 μM 72 h cell viability decreased in a dose dependent manner 30349650
TCCSUP Cell viability assay 0, 0.01, 0.1, 1 μM 72 h cell viability decreased in a dose dependent manner 30349650
UM-UC-3 Cell viability assay 0, 0.01, 0.1, 1 μM 72 h cell viability decreased in a dose dependent manner 30349650
Click to View More Cell Line Experimental Data

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
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 Research 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.
Experimental Result Images Methods Biomarkers Images PMID
Western blot p53 / CDKN1a / Survivin AXL / phospho-AKT / phospho-P70S6K / AKT / P70S6K 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 CHEK1 / MLH1 / MSH2 / PMS2 / Rad51 25948791
Immunofluorescence NPM1 / PU.1 XPO1 / tubulin 30015632
Growth inhibition assay Cell viability 28852098
In Vivo
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]
Animal Research Animal Models T-ALL and AML orthograft mouse model
Dosages 20 -25 mg/kg
Administration p.o.
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT05952687 Withdrawn
Rhabdoid Tumor|Atypical Teratoid/Rhabdoid Tumor|Atypical Teratoid/Rhabdoid Tumor of CNS|CNS Tumor
St. Jude Children''s Research Hospital
 March 2024 Phase 1
NCT05698147 Recruiting
Central Nervous System Lymphoma
Tong Chen|Antengene Corporation|Huashan Hospital
 August 3 2023 Phase 1|Phase 2
NCT05954780 Recruiting
Multiple Myeloma
iOMEDICO AG|Stemline Switzerland GmbH|Climedo Health GmbH
 June 28 2023 --
NCT05170789 Withdrawn
Relapsed Multiple Myeloma|Refractory Multiple Myeloma
Tulane University School of Medicine|Karyopharm Therapeutics Inc|Tulane University
 April 27 2022 Phase 2
NCT05201118 Unknown status
Extramedullary Multiple Myeloma
Chunrui Li|Nanjing IASO Biotechnology Co. Ltd.|Tongji Hospital
 January 1 2022 Phase 1

Chemical Information & Solubility

Molecular Weight 443.31 Formula

C17H11F6N7O
CAS No. 1393477-72-9 SDF Download Selinexor (KPT-330) SDF
Smiles C1=CN=C(C=N1)NNC(=O)C=CN2C=NC(=N2)C3=CC(=CC(=C3)C(F)(F)F)C(F)(F)F
Storage (From the date of receipt)

In vitro
Batch:

DMSO : 89 mg/mL ( (200.76 mM) Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 89 mg/mL

Water : Insoluble


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In vivo
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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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