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Chemical Structure| 1392136-43-4 Chemical Structure| 1392136-43-4

Structure of Verdinexor
CAS No.: 1392136-43-4

Chemical Structure| 1392136-43-4

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Verdinexor is an orally bioavailable selective inhibitor of nuclear export (SINE), inhibits nuclear export protein Exportin 1 (XPO1/CRM1) against canine tumor cell lines and also reduce influenza virus replication in vitro and in vivo.

Synonyms: KPT-335; ATG-527

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Product Details of Verdinexor

CAS No. :1392136-43-4
Formula : C18H12F6N6O
M.W : 442.32
SMILES Code : O=C(NNC1=NC=CC=C1)/C=C\N2N=C(C3=CC(C(F)(F)F)=CC(C(F)(F)F)=C3)N=C2
Synonyms :
KPT-335; ATG-527
MDL No. :MFCD28167840
InChI Key :OPAKEJZFFCECPN-XQRVVYSFSA-N
Pubchem ID :71492799

Safety of Verdinexor

GHS Pictogram:
Signal Word:Warning
Hazard Statements:H302-H315-H319-H335
Precautionary Statements:P261-P305+P351+P338

Isoform Comparison

Biological Activity

Description
Verdinexor (KPT-335) is an innovative, orally-administered selective inhibitor of nuclear export (SINE) that blocks the nuclear export protein Exportin 1 (XPO1/CRM1), showing efficacy against canine cancer cell lines[1].
Target
  • CRM1

In Vitro:

Cell Line
Concentration Treated Time Description References
BEAS-2B cells 1 μM 24 hours To verify the inhibitory effect of KPT-335 on RSV A and B strains. Results showed that 1 μM KPT-335 inhibited replication of RSV A2, Long, and B1 strains. J Virol. 2019 Feb 5;93(4):e01684-18.
A549 cells 1 μM 72 hours To evaluate the inhibitory effect of KPT-335 on RSV replication. Results showed that 1 μM KPT-335 inhibited RSV A2 replication by ~50% without affecting cell viability. J Virol. 2019 Feb 5;93(4):e01684-18.
KYSE510 20 μM 48 hours To evaluate the inhibitory effect of Verdinexor on the proliferation of esophageal cancer cells Int J Biol Sci. 2022 Jan 1;18(1):276-291.
KYSE180 20 μM 48 hours To evaluate the inhibitory effect of Verdinexor on the proliferation of esophageal cancer cells Int J Biol Sci. 2022 Jan 1;18(1):276-291.
KYSE450 20 μM 48 hours To evaluate the inhibitory effect of Verdinexor on the proliferation of esophageal cancer cells Int J Biol Sci. 2022 Jan 1;18(1):276-291.
KYSE30 20 μM 48 hours To evaluate the inhibitory effect of Verdinexor on the proliferation of esophageal cancer cells Int J Biol Sci. 2022 Jan 1;18(1):276-291.
Primary rat cortical neurons 10 μM 48 hours To evaluate the protective effects of SINE compounds against TNF-α-induced neurotoxicity. Results showed that SINE compounds significantly increased cell viability and mitochondrial activity, with at least 50% and 100% increments in preservation of cell viability and cellular enzymatic activity, respectively, compared to non-treated neuronal cells (P<0.05). CNS Neurosci Ther. 2016;22(4):306-315.
SH-SY5Y 0.3 µM 48 hours To evaluate the inhibitory effect of Verdinexor on neuroblastoma cell proliferation. Results showed that Verdinexor significantly inhibited the proliferation of SH-SY5Y cells and induced apoptosis. J Exp Clin Cancer Res. 2021 Aug 12;40(1):255.
SK-N-BE(2) 1.4 µM 48 hours To evaluate the inhibitory effect of Verdinexor on neuroblastoma cell proliferation. Results showed that Verdinexor significantly inhibited the proliferation of SK-N-BE(2) cells and induced apoptosis. J Exp Clin Cancer Res. 2021 Aug 12;40(1):255.
Bone marrow mononuclear cells (BMMC) 0.01 μM, 0.05 μM, 0.1 μM, 0.5 μM, 1 μM, 10 μM 24 hours-4 days To evaluate the effect of Verdinexor on the survival of plasma cells in bone marrow and blood. Results showed that bone marrow-derived plasma cells were less sensitive to Verdinexor compared to those from blood. Front Immunol. 2025 Jan 10;15:1499551.
293T cells 1 μM 6 hours To evaluate the interference effect of Verdinexor on XPO1-NEP binding, results showed that Verdinexor reduced the binding of XPO1 to NEP J Virol. 2014 Sep 1;88(17):10228-43.
MDCK cells 1 μM 2 hours To evaluate the inhibitory effect of Verdinexor on influenza virus replication, results showed that Verdinexor effectively inhibited the replication of influenza virus A/California/04/09 (pH1N1) J Virol. 2014 Sep 1;88(17):10228-43.
A549 cells 1 μM 2 hours To evaluate the inhibitory effect of Verdinexor on influenza virus replication, results showed that Verdinexor effectively inhibited the replication of influenza virus A/WSN/33 (H1N1) J Virol. 2014 Sep 1;88(17):10228-43.
VeroE6 cells 0.1 µM 4 days To evaluate the inhibitory effect of Verdinexor on SARS-CoV-2 replication, results showed that 0.1 µM Verdinexor reduced viral replication by approximately 15%. Front Cell Infect Microbiol. 2022 May 23;12:849017.
A549 cells 0.2μM 2 hours To evaluate the inhibitory effect of Verdinexor on influenza virus replication PLoS One. 2016 Nov 28;11(11):e0167221.

In Vivo:

Species
Animal Model
Administration Dosage Frequency Description References
Nude mice Neuroblastoma xenograft model Oral gavage 10 mg/kg Three times per week for four weeks To evaluate the antitumor effects of Verdinexor in vivo. Results showed that Verdinexor significantly inhibited tumor growth without causing obvious toxic effects. J Exp Clin Cancer Res. 2021 Aug 12;40(1):255.
Nude mice KYSE30 xenograft model Intraperitoneal injection 5 mg/kg 24 days To evaluate the inhibitory effect of Verdinexor on tumor growth of esophageal cancer in vivo Int J Biol Sci. 2022 Jan 1;18(1):276-291.
BALB/c mice Influenza virus infection model Oral 10 or 20 mg/kg Once daily for 3 days To evaluate the antiviral effect of Verdinexor in vivo, results showed that Verdinexor reduced lung viral loads, decreased inflammatory responses, and improved survival rates J Virol. 2014 Sep 1;88(17):10228-43.
Mice Influenza virus infection model Oral 20 mg/kg Once on day 1 and day 3 post-infection To evaluate the inhibitory effect of Verdinexor on influenza virus replication in vivo, results showed that Verdinexor significantly reduced virus shedding and pulmonary inflammatory response PLoS One. 2016 Nov 28;11(11):e0167221.

Protocol

Bio Calculators
Preparing Stock Solutions 1mg 5mg 10mg

1 mM

5 mM

10 mM

2.26mL

0.45mL

0.23mL

11.30mL

2.26mL

1.13mL

22.61mL

4.52mL

2.26mL

Dissolving Methods
Please choose the appropriate dissolution scheme according to your animal administration guide.For the following dissolution schemes, clear stock solution should be prepared according to in vitro experiments, and then cosolvent should be added in turn:

in order to ensure the reliability of the experimental results, the clarified stock solution can be properly preserved according to the storage conditions; The working fluid for in vivo experiment is recommended to be prepared now and used on the same day;

The percentage shown in front of the following solvent refers to the volume ratio of the solvent in the final solution; If precipitation or precipitation occurs in the preparation process, it can be assisted by heating and/or ultrasound.
Protocol 1
Protocol 2

References

 

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