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Selinexor (KPT-330)

Catalog No. T6106   CAS 1393477-72-9
Synonyms: Selinexor, KPT-330

Selinexor (KPT-330) is a small molecule inhibitor of CRM1 with selective and oral activity. Selinexor blocks the cell cycle, induces apoptosis, and has antitumor activity for the treatment of multiple myeloma.

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Selinexor (KPT-330) Chemical Structure
Selinexor (KPT-330), CAS 1393477-72-9
Pack Size Availability Price/USD Quantity
2 mg In stock $ 39.00
5 mg In stock $ 74.00
25 mg In stock $ 281.00
50 mg In stock $ 422.00
100 mg In stock $ 481.00
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Purity: 100%
Purity: 99.85%
Purity: 99.07%
Purity: 98%
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Biological Description
Chemical Properties
Storage & Solubility Information
Description Selinexor (KPT-330) is a small molecule inhibitor of CRM1 with selective and oral activity. Selinexor blocks the cell cycle, induces apoptosis, and has antitumor activity for the treatment of multiple myeloma.
In vitro METHODS: Six T-ALL cells, MOLT-4, Jurkat, HBP-ALL, KOPTK-1, SKW-3 and DND-41, were treated with Selinexor (0-1000 µM) for 72 h. Cell growth inhibition was detected using Cell Titer Glo assay.
RESULTS: Selinexor treatment inhibited T-ALL cell growth with IC50 values of 34-203 nM. [1]
METHODS: Multiple myeloma cells MM1S were treated with Selinexor (100 nM) for 8 h. The expression levels of target proteins were detected by Western Blot.
RESULTS: Selinexor treatment resulted in the accumulation of p53, IκB, p21 and p27 in the nucleus of MM1S cells. [2]
In vivo METHODS: To assay antitumor activity in vivo, Selinexor (20-25 mg/kg) was administered by gavage to NSG mice harboring the human T-ALL tumor MOLT-4 three times per week for thirty-six days.
RESULTS: Selinexor-treated mice exhibited significant inhibition of leukemia cell growth with significant survival benefit. [1]
METHODS: To assay anti-tumor activity in vivo, Selinexor (20 mg/kg) was administered by gavage three times per week for four weeks to an NSG mouse model of primary AML in patients.
RESULTS: Selinexor was cytotoxic to primary AML cells transplanted into mice. [3]
Synonyms Selinexor, KPT-330
Molecular Weight 443.31
Formula C17H11F6N7O
CAS No. 1393477-72-9

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

H2O: < 1 mg/mL (insoluble or slightly soluble)

Ethanol: 38 mg/mL (85.7 mM)

DMSO: 82 mg/mL (185 mM)

TargetMolReferences and Literature

1. Etchin J, et al. KPT-330 inhibitor of CRM1 (XPO1)-mediated nuclear export has selective anti-leukaemic activity in preclinical models of T-cell acute lymphoblastic leukaemia and acute myeloid leukaemia. Br J Haematol. 2013 Apr;161(1):117-27. 2. Tai YT, et al. CRM1 inhibition induces tumor cell cytotoxicity and impairs osteoclastogenesis in multiple myeloma: molecular mechanisms and therapeutic implications. Leukemia. 2014 Jan;28(1):155-65. 3. Etchin J, et al. Activity of a selective inhibitor of nuclear export, selinexor (KPT-330), against AML-initiating cells engrafted into immunosuppressed NSG mice. Leukemia. 2016 Jan;30(1):190-9.

TargetMolCitations

1. Han Y, Hu A, Qu Y, et al.Covalent targeting the LAS1-NOL9 axis for selective treatment in NPM1 mutant acute myeloid leukemia.Pharmacological Research.2023: 106700.

Related compound libraries

This product is contained In the following compound libraries:
Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library Membrane Protein-targeted Compound Library Drug Repurposing Compound Library Anti-Cancer Approved Drug Library Inhibitor Library Anti-Cancer Drug Library EMA Approved Drug Library FDA-Approved & Pharmacopeia Drug Library Anti-Cancer Compound Library

Related Products

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CRM1-IN-1 KPT330,(E)- KPT185 Verdinexor CRM1-IN-2 Leptomycin A KPT276 LFS-1107

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Keywords

Selinexor (KPT-330) 1393477-72-9 Membrane transporter/Ion channel CRM1 KPT 330 KPT330 Selinexor Selinexor (KPT 330) KPT-330 Selinexor (KPT330) inhibitor inhibit

 

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