Tezacaftor (VX-661)

Catalog No.S7059 Batch:S705903

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Technical Data

Formula

C26H27F3N2O6
Molecular Weight 520.5 CAS No. 1152311-62-0
Solubility (25°C)* In vitro DMSO 100 mg/mL (192.12 mM)
Ethanol 100 mg/mL (192.12 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
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 40%PEG300 5%Tween80 50%ddH2O

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 5.000mg/ml (9.61mM) Taking the 1 mL working solution as an example, add 50 μL of 100 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 make it clear; 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. 
* <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 Tezacaftor (VX-661) is a second F508del CFTR corrector and is believed to help CFTR protein reach the cell surface. Phase 2.
Targets
F508del-CFTR [1]
(Cell-free assay)
In vitro

VX-661, known as a CTFR corrector, allows F508del mutant channels to escape degradation and transit to the cell membrane.

Protocol (from reference)

Cell Assay:

[2]
  • Cell lines

    Primary HBE cells

  • Concentrations

    5 μM

  • Incubation Time

    24 h

  • Method

    Cells were treated with indicated concentration of drug for 24 h.
Animal Study:

[3]
  • Animal Models

    Male FVB/n mice

  • Dosages

    2 mg/kg

  • Administration

    i.p.

References

  • http://investors.vrtx.com/releasedetail.cfm?releaseid=757597
  • https://pubmed.ncbi.nlm.nih.gov/33859562/
  • https://pubmed.ncbi.nlm.nih.gov/34587656/

Customer Product Validation

(B)ΔISC response to forskolin observed in VX-661-treated CF HBE cells (*P = 0.0021, VX661 vs. vehicle) was prevented by chronic VX-770 treatment and significantly different from VX-661-treated cells (#P=0.0126, VX661 vs. VX661+VX770). (C) The response to CFTR inh-172 that was observed in VX-661-treated cells (*P = 0.0111, VX661 vs. vehicle) was significantly decreased in VX809+VX770 treated cells (#P = 0.0038, VX661 vs. VX661+VX770). Primary CF HBE cultures (ΔF508/ΔF508) were derived from 3 different patients, and 3-4 replicates were performed per patient.

Data from [ Sci Transl Med , 2014 , 6(246), 246ra96 ]

Representative WB analysis of CFBE cells stably expressing R560S-, F508del or wt-CFTR, following treatment with VX-809 (3 μM), VX-661(5 μM), DMSO (0.1% v/v) or incubation at 27 °C, for 24 h.

Data from [ , , J Cyst Fibros, 2018, doi:10.1016/j.jcf.2018.07.001 ]

Bar graphs represent maximum percentage change in fluorescence (ΔF) after addition of CFTR agonist, relative to baseline (F0) measurements prior to agonist addition (time = 10 min). Asterisks indicate statistical significance using one-way ANOVA and Tukey’s multiple comparison tests for the three distinct differentiations (*p < 0.05, **p < 0.01, ***p < 0.001).

Data from [ , , NPJ Genom Med. 2017, 2:12 ]

Selleck's Tezacaftor (VX-661) Has Been Cited by 146 Publications

Uncovering Cystic Fibrosis Carrier: Insights From a Heterozygous CFTR-F508del Rabbit Model [ Int Forum Allergy Rhinol, 2026, 10.1002/alr.70128] PubMed: 41758072
Identification of small molecules that enhance aminoglycoside-mediated suppression of CFTR and NF1 nonsense mutations [ Mol Ther Oncol, 2026, 34(2):201173] PubMed: 41939791
Investigation of HE4 expression concerning epithelial-mesenchymal transition (EMT) in cystic fibrosis epithelial cells [ J Cyst Fibros, 2026, S1569-1993(26)00086-X] PubMed: 41936498
Functional, Cohort-Level Assessment of CFTR Modulator Responses Using Biobanked Nasal Epithelial Cells from Individuals with Cystic Fibrosis [ J Pers Med, 2026, 16(1)51] PubMed: 41590543
CFTR rescue in W1282X cystic fibrosis patient-derived intestinal organoids (PDIOs) mediated by translational readthrough-inducing drugs (TRIDs) [ Genet Med Open, 2026, 4:103472] PubMed: 41492359
ACE-tRNAs are a platform technology for suppressing nonsense mutations that cause cystic fibrosis [ Nucleic Acids Res, 2025, 53(13)gkaf675] PubMed: 40650978
Antisense oligonucleotide targeting the E3 ligase RFFL potentiates CFTR modulator efficacy in CF primary bronchial epithelial cells [ Mol Ther Nucleic Acids, 2025, 36(4):102756] PubMed: 41323797
Transcriptomic and functional responses of the cystic fibrosis airway epithelium to CFTR modulator therapy [ JCI Insight, 2025, 10(21)e196018] PubMed: 41212059
Endometrium-derived organoids from cystic fibrosis patients and mice as new models to study disease-associated endometrial pathobiology [ Cell Mol Life Sci, 2025, 82(1):109] PubMed: 40074868
CFTR negatively reprograms Th2 cell responses, and CFTR potentiation restrains allergic airway inflammation [ JCI Insight, 2025, 10(9)e191098] PubMed: 40131363

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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.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.