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Selinexor (KPT-330)

Name: Selinexor (KPT-330)
Brand: Selleck Chemicals
SKU: S7252
Rating: 5 (91 reviews)

Synonyms: ATG-010

Catalog No.S7252 Purity: 99.74%

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

Selinexor (KPT-330) Chemical Structure

CAS: 1393477-72-9

Selleck's Selinexor (KPT-330) has been cited by 91 publications

Purity & Quality Control

Batch: Purity: 99.74%

99.74

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Cell Data

Cell Lines	Assay Type	Concentration	Incubation Time	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
Clinical Trial Information (data from https://clinicaltrials.gov, updated on 2024-01-11)
NCT05952687	Not yet recruiting	Rhabdoid Tumor\|Atypical Teratoid/Rhabdoid Tumor\|Atypical Teratoid/Rhabdoid Tumor of CNS\|CNS Tumor	St. Jude Children''s Research Hospital	January 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	Recruiting	Extramedullary Multiple Myeloma	Chunrui Li\|Nanjing IASO Biotechnology Co. Ltd.\|Tongji Hospital	January 1 2022	Phase 1

References

Chemical lnformation & 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)	3 years-20°Cpowder	Storage of Stock Solutions Aliquot the stock solutions to avoid repeated freeze-thaw cycles	1 year-80°Cin solvent
Storage (From the date of receipt)	3 years-20°Cpowder		1 month-20°Cin solvent

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

Molecular Weight Calculator

In vivo
Batch:

Add solvents to the product individually and in order.

In vivo Formulation Calculator

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Molarity Calculator

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Dilution Calculator Molecular Weight Calculator

In vivo Formulation Calculator (Clear solution)

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

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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.
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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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