Tezacaftor (VX-661)
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MedKoo CAT#: 510264

CAS#: 1152311-62-0

Description: Tezacaftor, also known asVX-661, is CFTR modulator. VX-661 is potentially useful for treatment of cystic fibrosis disease. Cystic fibrosis (CF) is a genetic disease caused by defects in the CF transmembrane regulator (CFTR) gene, which encodes an epithelial chloride channel. The most common mutation, Δ508CFTR, produces a protein that is misfolded and does not reach the cell membrane. VX-661 can correct trafficking of Δ508CFTR and partially restore chloride channel activity.


Price and Availability

Size Price Shipping out time Quantity
10mg USD 150 Same day
25mg USD 250 Same day
50mg USD 450 Same day
100mg USD 650 Same day
200mg USD 950 Same day
500mg USD 1750 Same day
1g USD 2850 2 Weeks
2g USD 3650 2 Weeks
5g USD 5650 2 Weeks
Inquire bulk and customized quantity

Pricing updated 2020-06-02. Prices are subject to change without notice.

Tezacaftor (VX-661), purity > 98%, is in stock. The same day shipping out after order is received.


Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 510264
Name: Tezacaftor (VX-661)
CAS#: 1152311-62-0
Chemical Formula: C26H27F3N2O6
Exact Mass: 520.18212
Molecular Weight: 520.5
Elemental Analysis: C, 60.00; H, 5.23; F, 10.95; N, 5.38; O, 18.44


Synonym: VX-661; VX661; VX 661; Tezacaftor. Trikafta.

IUPAC/Chemical Name: (R)-1-(2,2-difluorobenzo[d][1,3]dioxol-5-yl)-N-(1-(2,3-dihydroxypropyl)-6-fluoro-2-(1-hydroxy-2-methylpropan-2-yl)-1H-indol-5-yl)cyclopropanecarboxamide

InChi Key: MJUVRTYWUMPBTR-MRXNPFEDSA-N

InChi Code: InChI=1S/C26H27F3N2O6/c1-24(2,13-33)22-8-14-7-18(17(27)10-19(14)31(22)11-16(34)12-32)30-23(35)25(5-6-25)15-3-4-20-21(9-15)37-26(28,29)36-20/h3-4,7-10,16,32-34H,5-6,11-13H2,1-2H3,(H,30,35)/t16-/m1/s1

SMILES Code: O=C(C1(C2=CC=C(OC(F)(F)O3)C3=C2)CC1)NC4=CC5=C(N(C[C@@H](O)CO)C(C(C)(C)CO)=C5)C=C4F


Technical Data

Appearance:
Solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Safety Data Sheet (SDS):

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:
2934.99.9001


Additional Information

  
 
 
 


References

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2: Middleton PG, Mall MA, Dřevínek P, Lands LC, McKone EF, Polineni D, Ramsey BW, Taylor-Cousar JL, Tullis E, Vermeulen F, Marigowda G, McKee CM, Moskowitz SM, Nair N, Savage J, Simard C, Tian S, Waltz D, Xuan F, Rowe SM, Jain R; VX17-445-102 Study Group. Elexacaftor-Tezacaftor-Ivacaftor for Cystic Fibrosis with a Single Phe508del Allele. N Engl J Med. 2019 Nov 7;381(19):1809-1819. doi: 10.1056/NEJMoa1908639. Epub 2019 Oct 31. PubMed PMID: 31697873.

3: Erratum: Profile Of Tezacaftor/Ivacaftor Combination And Its Potential In The Treatment Of Cystic Fibrosis [Erratum]. Ther Clin Risk Manag. 2019 Oct 11;15:1207. doi: 10.2147/TCRM.S232419. eCollection 2019. PubMed PMID: 31696867; PubMed Central PMCID: PMC6795023.

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13: Davies JC, Moskowitz SM, Brown C, Horsley A, Mall MA, McKone EF, Plant BJ, Prais D, Ramsey BW, Taylor-Cousar JL, Tullis E, Uluer A, McKee CM, Robertson S, Shilling RA, Simard C, Van Goor F, Waltz D, Xuan F, Young T, Rowe SM; VX16-659-101 Study Group. VX-659-Tezacaftor-Ivacaftor in Patients with Cystic Fibrosis and One or Two Phe508del Alleles. N Engl J Med. 2018 Oct 25;379(17):1599-1611. doi: 10.1056/NEJMoa1807119. Epub 2018 Oct 18. PubMed PMID: 30334693; PubMed Central PMCID: PMC6277022.

14: Keating D, Marigowda G, Burr L, Daines C, Mall MA, McKone EF, Ramsey BW, Rowe SM, Sass LA, Tullis E, McKee CM, Moskowitz SM, Robertson S, Savage J, Simard C, Van Goor F, Waltz D, Xuan F, Young T, Taylor-Cousar JL; VX16-445-001 Study Group. VX-445-Tezacaftor-Ivacaftor in Patients with Cystic Fibrosis and One or Two Phe508del Alleles. N Engl J Med. 2018 Oct 25;379(17):1612-1620. doi: 10.1056/NEJMoa1807120. Epub 2018 Oct 18. PubMed PMID: 30334692; PubMed Central PMCID: PMC6289290.

15: Hussar DA, George J. Erenumab-aooe, Benralizumab, and Tezacaftor/ivacaftor. J Am Pharm Assoc (2003). 2018 Sep - Oct;58(5):579-582. doi: 10.1016/j.japh.2018.07.006. PubMed PMID: 30190109.

16: Sala MA, Jain M. Tezacaftor for the treatment of cystic fibrosis. Expert Rev Respir Med. 2018 Sep;12(9):725-732. doi: 10.1080/17476348.2018.1507741. Epub 2018 Aug 9. Review. PubMed PMID: 30073878.

17: Kirby T. Tezacaftor-ivacaftor is safe and efficacious in patients with cystic fibrosis with Phe508del mutations. Lancet Respir Med. 2018 Jan;6(1):13-14. doi: 10.1016/S2213-2600(17)30439-3. Epub 2017 Dec 14. PubMed PMID: 29248431.

18: Taylor-Cousar JL, Munck A, McKone EF, van der Ent CK, Moeller A, Simard C, Wang LT, Ingenito EP, McKee C, Lu Y, Lekstrom-Himes J, Elborn JS. Tezacaftor-Ivacaftor in Patients with Cystic Fibrosis Homozygous for Phe508del. N Engl J Med. 2017 Nov 23;377(21):2013-2023. doi: 10.1056/NEJMoa1709846. Epub 2017 Nov 3. PubMed PMID: 29099344.

19: Rowe SM, Daines C, Ringshausen FC, Kerem E, Wilson J, Tullis E, Nair N, Simard C, Han L, Ingenito EP, McKee C, Lekstrom-Himes J, Davies JC. Tezacaftor-Ivacaftor in Residual-Function Heterozygotes with Cystic Fibrosis. N Engl J Med. 2017 Nov 23;377(21):2024-2035. doi: 10.1056/NEJMoa1709847. Epub 2017 Nov 3. PubMed PMID: 29099333; PubMed Central PMCID: PMC6472479.

20: Donaldson SH, Pilewski JM, Griese M, Cooke J, Viswanathan L, Tullis E, Davies JC, Lekstrom-Himes JA, Wang LT; VX11-661-101 Study Group. Tezacaftor/Ivacaftor in Subjects with Cystic Fibrosis and F508del/F508del-CFTR or F508del/G551D-CFTR. Am J Respir Crit Care Med. 2018 Jan 15;197(2):214-224. doi: 10.1164/rccm.201704-0717OC. PubMed PMID: 28930490; PubMed Central PMCID: PMC5768901.