Selinexor (KPT-330)

Catalog No.S7252

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

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Selinexor (KPT-330) Chemical Structure

Selinexor (KPT-330) Chemical Structure
Molecular Weight: 443.31

Validation & Quality Control

Quality Control & MSDS

Product Information

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Product Description

Biological Activity

Description Selinexor (KPT-330) 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]
Features

Protocol(Only for 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
Formulation Pluronic F-68/PVP-K29/32
Dosages 20 -25 mg/kg
Administration p.o.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)

SpeciesMouseRatRabbitGuinea pigHamsterDog
Weight (kg)0.020.151.80.40.0810
Body Surface Area (m2)0.0070.0250.150.050.020.5
Km factor36128520
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of resveratrol used for a mouse (22.4 mg/kg) to a dose based on the BSA for a rat, multiply 22.4 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for resveratrol of 11.2 mg/kg.

Rat dose (mg/kg) = mouse dose (22.4 mg/kg) ×  mouse Km(3)  = 11.2 mg/kg
rat Km(6)
1

References

[1] Etchin J, et al. Br J Haematol. 2013, 161(1), 117-127.

[2] Tai YT, et al. Leukemia. 2014, 28(1), 155-165.

Clinical Trial Information( data from http://clinicaltrials.gov, updated on 2016-07-30)

NCT Number Recruitment Conditions Sponsor
/Collaborators
Start Date Phases
NCT02471911 Recruiting Diffuse Large B-Cell Lymphoma Weill Medical College of Cornell University|Karyopharm Th  ...more Weill Medical College of Cornell University|Karyopharm Therapeutics, Inc November 2015 Phase 1
NCT02228525 Recruiting Myelodysplastic Syndromes Memorial Sloan Kettering Cancer Center|M.D. Anderson Canc  ...more Memorial Sloan Kettering Cancer Center|M.D. Anderson Cancer Center|Columbia University|Karyopharm Therapeutics, Inc August 2014 Phase 2
NCT02213133 Terminated Squamous Cell Carcinoma Karyopharm Therapeutics, Inc July 2014 Phase 2
NCT02091245 Recruiting Relapsed Acute Lymphoblastic Leukemia (ALL)|Refractory Acute Lymphoblastic Leukemia (ALL)|Relapsed Acute Myelogenous Leukemia (AML)|Refractory Acut  ...more Relapsed Acute Lymphoblastic Leukemia (ALL)|Refractory Acute Lymphoblastic Leukemia (ALL)|Relapsed Acute Myelogenous Leukemia (AML)|Refractory Acute Myelogenous Leukemia (AML)|Relapsed Mixed Lineage Leukemia|Refractory Mixed Lineage Leukemia|Relapsed Biphenotypic Leukemia|Refractory Biphenotypic Leukemia|Chronic Myelogenous Leukemia (CML) in Blast Crisis Dana-Farber Cancer Institute|William Lawrence and Blanche  ...more Dana-Farber Cancer Institute|William Lawrence and Blanche Hughes Foundation|Karyopharm Therapeutics, Inc March 2014 Phase 1
NCT02078349 Recruiting Solid Tumors National University Hospital, Singapore|Karyopharm Therap  ...more National University Hospital, Singapore|Karyopharm Therapeutics, Inc February 2014 Phase 1

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Chemical Information

Download Selinexor (KPT-330) SDF
Molecular Weight (MW) 443.31
Formula

C17H11F6N7O

CAS No. 1393477-72-9
Storage 3 years -20℃powder
2 years -80℃in solvent
Synonyms N/A
Solubility (25°C) * In vitro DMSO 89 mg/mL (200.76 mM)
Ethanol 40 mg/mL (90.23 mM)
Water <1 mg/mL
In vivo 2% DMSO+49% PEG 300+dd H2O 5mg/mL
* <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.
Chemical Name (Z)-3-(3-(3,5-bis(trifluoromethyl)phenyl)-1H-1,2,4-triazol-1-yl)-N'-(pyrazin-2-yl)acrylohydrazide

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.

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
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