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Selinexor (KPT-330) CRM1 inhibitor

Name: Selinexor (KPT-330)
Brand: Selleck Chemicals
SKU: S7252
Availability: InStock
Rating: 5 (127 reviews)

Cat.No.S7252

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

Chemical Structure

Molecular Weight: 443.31

Jump to Mechanism of Action Cell Culture & Working Concentration Solubility Chemical Information, Storage & Stability Specificity

Quality Control

Batch: Purity: 99.74%

99.74

Related Targets	CD markers AChR Calcium Channel Sodium Channel Potassium Channel GABA Receptor TRP Channel ATPase GluR NMDAR P2 Receptor Proton Pump P-gp CFTR SGLT Chloride Channel MCT Amino acid transporter GLUT VDAC BCRP NKCC OCT NCX OAT VMAT Aquaporin EAAT GlyT GlyR
Related Products	Eltanexor (KPT-8602) KPT-185 Verdinexor (KPT-335) KPT-276 Exportin-1/CRM1 Antibody [B23M5] Leptomycin B (LMB)

Cell Culture, Treatment & Working Concentration

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

Chemical Information, Storage & Stability

Molecular Weight	443.31	Formula	C₁₇H₁₁F₆N₇O	Storage (From the date of receipt)	3 years-20°Cpowder
CAS No.	1393477-72-9	Download SDF		Storage of Stock Solutions	1 year-80°Cin solvent 1 month-20°Cin solvent
Synonyms	ATG-010			Smiles	C1=CN=C(C=N1)NNC(=O)C=CN2C=NC(=N2)C3=CC(=CC(=C3)C(F)(F)F)C(F)(F)F

Solubility

In vitro
Batch:

DMSO : 89 mg/mL (200.76 mM)
(Moisture-contaminated DMSO may reduce solubility. Use fresh, anhydrous DMSO.)

Ethanol : 89 mg/mL

Water : Insoluble

Molarity Calculator

Mass	Concentration	Volume	Molecular Weight
Mass value Mass unit	Concentration value Concentration unit	Volume value Volume unit	Molecular weight (g/mol)

Dilution Calculator Molecular Weight Calculator

In vivo batch selection In vivo Batch:
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	5%DMSO 1 40%PEG300 2 5%Tween80 3 50%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.500mg/ml (10.15mM)	Taking the 1 mL working solution as an example, add 50 μL of 90 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Clear solution	2%DMSO 1 40%PEG300 2 5%Tween80 3 53%ddH2O Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.	4.000mg/ml (9.02mM)	Taking the 1 mL working solution as an example, add 20 μL 200 mg/ml clarified DMSO stock solution to 400 μL PEG300, mix evenly to clarify it; add 50 μL Tween80 to the above system, mix evenly to clarify it; then continue to add 530 μL ddH2O to adjust the volume to 1 mL. . The mixed solution should be used immediately for optimal results.
Homogeneous suspension	CMC-NA	≥5mg/ml	Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.

In vivo Formulation Calculator (Clear solution)

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

Dosage: mg/kg

Average weight of animals: g

Dosing volume per animal: μL

Number of animals:

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.

Mechanism of Action

Targets/IC₅₀/Ki	CRM1 ^[1] (Cell-free assay)
In vitro	As the clinical candidate analog of KPT-185, Selinexor (KPT-330) exhibits similar effects on the viability of T-ALL cells and elicits rapid apoptotic response. It 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]
In vivo	Selinexor (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, this compound inhibits MM-induced bone lysis and prolongs survival. Moreover, it directly impairs osteoclastogenesis and bone resorption by blocking RANKL-induced NF-κB and NFATc1, with minimal impact on osteoblasts and BMSCs. ^[2]
References	[1] https://pubmed.ncbi.nlm.nih.gov/23373539/ [2] https://pubmed.ncbi.nlm.nih.gov/23588715/

Applications

Methods	Biomarkers	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
Immunofluorescence	XPO1 / tubulin NPM1 / PU.1	30349650
Growth inhibition assay	Cell viability	28852098

Clinical Trial Information

(data from https://clinicaltrials.gov, updated on 2024-05-22)

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

Tech Support

Handling Instructions

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