Selonsertib free base


Catalog No. size PriceQuantity
M7001-2 2mg solid $121
M7001-10 10mg solid $476

Description

Cas:1448428-04-3 (free base)

Product Information

Selonsertib, also known as GS-4997, is an orally bioavailable inhibitor of apoptosis signal-regulating kinase 1 (ASK1), with potential anti-inflammatory, antineoplastic and anti-fibrotic activities. GS-4997 targets and binds to the catalytic kinase domain of ASK1 in an ATP-competitive manner, thereby preventing its phosphorylation and activation. GS-4997 prevents the production of inflammatory cytokines, down-regulates the expression of genes involved in fibrosis, suppresses excessive apoptosis and inhibits cellular proliferation.

 

Chemical Formula: C24H24FN7O

 

Exact Mass: 445.20264

 

Molecular Weight: 445.5

 

Elemental Analysis: C, 64.71; H, 5.43; F, 4.26; N, 22.01; O, 3.59

 

Synonym: 

 

GS-4997

GS4997

GS 4997

Selonsertib free base

 

Chemical Name: 5-(4-cyclopropyl-1H-imidazol-1-yl)-2-fluoro-N-(6-(4-isopropyl-4H-1,2,4-triazol-3-yl)pyridin-2-yl)-4-methylbenzamide

 

InChi Key: 

YIDDLAAKOYYGJG-UHFFFAOYSA-N

 

InChi Code: InChI=1S/C24H24FN7O/c1-14(2)32-13-27-30-23(32)19-5-4-6-22(28-19)29-24(33)17-10-21(15(3)9-18(17)25)31-11-20(26-12-31)16-7-8-16/h4-6,9-14,16H,7-8H2,1-3H3,(H,28,29,33)

 

Smiles Code:

O=C(NC1=NC(C2=NN=CN2C(C)C)=CC=C1)C3=CC(N4C=C(C5CC5)N=C4)=C(C)C=C3F

 

Technical Data:

 

Appearance: White to off-white

Purity: >98% (Note: HPLC, LC/MS may detect up to ~ 5% tautomer depending on

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: >5 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

 

In Vitro

Selonsertib (GS-4997) is a clinical stage ASK1 inhibitor, which has been evaluated as an experimental treatment for diabetic nephropathy and kidney fibrosis. Selonsertib (GS-4997) is a highly selective and potent once-daily oral ASK1 inhibitor that competes with ATP in the ASK1 catalytic kinase domain.

 

 

References

 

  1. Ji N, Yang Y, Cai CY, Lei ZN, Wang JQ, Gupta P, Shukla S, Ambudkar SV, Kong D, Chen ZS. Selonsertib (GS-4997), an ASK1 inhibitor, antagonizes multidrug resistance in ABCB1- and ABCG2-overexpressing cancer cells. Cancer Lett. 2019 Jan;440-441:82-93. doi: 10.1016/j.canlet.2018.10.007. Epub 2018 Oct 10. PubMed PMID: 30315846.

 

  1. Nelson CH, Wang L, Fang L, Weng W, Cheng F, Hepner M, Lin J, Garnett C, Ramanathan S. A Quantitative Framework to Evaluate Proarrhythmic Risk in a First-in-Human Study to Support Waiver of a Thorough QT Study. Clin Pharmacol Ther. 2015 Dec;98(6):630-8. doi: 10.1002/cpt.204. Epub 2015 Sep 29. PubMed PMID: 26259519.

       3. Lin JH, Zhang JJ, Lin SL, Chertow GM. Design of a phase 2 clinical trial of an                   ASK1 inhibitor, GS-4997, in patients with diabetic kidney disease. Nephron.                   2015;129(1):29-33. doi: 10.1159/000369152. Epub 2014 Dec 17. PubMed PMID:             25531162.

 

Products are for research use only. Not for human use.

 

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