Selinexor (KPT-330)

Catalog No.S7252 Batch:S725207

Technical Data

Formula

C₁₇H₁₁F₆N₇O

Molecular Weight

443.31

CAS No.

1393477-72-9

Solubility (25°C)*

In vitro

DMSO

89 mg/mL (200.76 mM)

Ethanol

89 mg/mL (200.76 mM)

Water

Insoluble

In vivo (Add solvents to the product individually and in order)

Clear solution

2%DMSO 1 40%PEG300 2 5%Tween80 3 53%ddH2O

4.0mg/ml

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.

* <1 mg/ml means slightly soluble or insoluble.
* 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.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

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]

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 Assay:^{^[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 Study:^{^[1]}	Animal Models T-ALL and AML orthograft mouse model Dosages 20 -25 mg/kg Administration p.o.

Cell Assay:^{^[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 Study:^{^[1]}

Animal Models
T-ALL and AML orthograft mouse model
Dosages
20 -25 mg/kg
Administration
p.o.

References

Customer Product Validation

: , , Mol Cancer Ther, 2017, 16(4):717-728

: Data from [Data independently produced by , , J Cell Mol Med, 2018, doi:10.1111/jcmm.13886]

: Data from [Data independently produced by , , BMC Cancer, 2018, 18(1):764]

: Data from [Data independently produced by , , Biochem Biophys Res Commun, 2018, 503(3):1773-1779]

Selleck's Selinexor (KPT-330) has been cited by 95 publications

Dual Inhibition of CDK4/6 and XPO1 Induces Senescence With Acquired Vulnerability to CRBN-Based PROTAC Drugs [ Gastroenterology, 2024, S0016-5085(24)00062-3]	PubMed: 38262581
p300 nucleocytoplasmic shuttling underlies mTORC1 hyperactivation in Hutchinson-Gilford progeria syndrome [ Nat Cell Biol, 2024, 10.1038/s41556-023-01338-y]	PubMed: 38267537
Androgen deprivation induces double-null prostate cancer via aberrant nuclear export and ribosomal biogenesis through HGF and Wnt activation [ Nat Commun, 2024, 15(1):1231]	PubMed: 38336745
UCHL1 is a potential molecular indicator and therapeutic target for neuroendocrine carcinomas [ Cell Rep Med, 2024, S2666-3791(23)00610-9]	PubMed: 38244540
Phase-separated nuclear bodies of nucleoporin fusions promote condensation of MLL1/CRM1 and rearrangement of 3D genome structure [ Cell Rep, 2023, 42(8):112884]	PubMed: 37516964
KPT330 promotes the sensitivity of glioblastoma to olaparib by retaining SQSTM1 in the nucleus and disrupting lysosomal function [ Autophagy, 2023, 1-16.]	PubMed: 37712615
Nuclear export inhibition jumbles epithelial-mesenchymal states and gives rise to migratory disorder in healthy epithelia [ Elife, 2023, 12e81048]	PubMed: 36805020
Exportin 1-mediated nuclear/cytoplasmic trafficking controls drug sensitivity of classical Hodgkin's lymphoma [ Mol Oncol, 2023, 10.1002/1878-0261.13386]	PubMed: 36727672
Cytoplasmic Expression of TP53INP2 Modulated by Demethylase FTO and Mutant NPM1 Promotes Autophagy in Leukemia Cells [ Int J Mol Sci, 2023, 24(2)1624]	PubMed: 36675134
Azacitidine Is Synergistically Lethal with XPO1 Inhibitor Selinexor in Acute Myeloid Leukemia by Targeting XPO1/eIF4E/c-MYC Signaling [ Int J Mol Sci, 2023, 24(7)6816]	PubMed: 37047788

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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

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