Solcitinib - 98%, high purity , Tyrosine-protein kinase JAK1 inhibitor, CAS No.1206163-45-2, Tyrosine-protein kinase JAK1 inhibitor

Item Number
S413366
Grouped product items
SKUSizeAvailabilityPrice Qty
S413366-5mg
5mg
In stock
$199.90
S413366-25mg
25mg
In stock
$686.90

JAK1 Selective Inhibitors

Basic Description

SynonymsAS-56075 | A14405 | A892157 | GSK 2586184 | NSC 59989 | SB16965 | GLPG-0778;Solcitinib | MPYACSQFXVMWNO-UHFFFAOYSA-N | VERATRALDEHYDE [FHFI] | Q10395590 | s5917 | SOLCITINIB [WHO-DD] | G154578 | G-154578 | GLPG-0788 | Cyclopropanecarboxamide, N-(5-(4-((3,
Specifications & PurityMoligand™, ≥98%
Biochemical and Physiological MechanismsSolcitinib (GLPG0778, GSK2586184) is an inhibitor of JAK1 with an IC50 of 8-9 nM, and shows 11-, 55- and 23-fold selectivity over JAK2, JAK3 and TYK2, respectively.
Storage TempStore at -20°C
Shipped InIce chest + Ice pads
GradeMoligand™
Action TypeINHIBITOR
Mechanism of actionTyrosine-protein kinase JAK1 inhibitor
Product Description

Information

Solcitinib (GLPG0778, GSK2586184) is an inhibitor ofJAK1with an IC50 of 8-9 nM, and shows 11-, 55- and 23-fold selectivity over JAK2, JAK3 and TYK2, respectively.


Targets

JAK2 ; JAK3 ; TYK2 ; JAK1 ; 8-9 nM

Product Properties

ALogP3.118
HBD Count1
Rotatable Bond4

Associated Targets(Human)

TYK2 Tclin Non-receptor tyrosine-protein kinase TYK2 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
JAK3 Tclin Tyrosine-protein kinase JAK3 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
JAK1 Tclin Tyrosine-protein kinase JAK1 (2 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
JAK2 Tclin Tyrosine-protein kinase JAK2 (1 Activities)
Activity TypeActivity Value -log(M)Mechanism of ActionActivity ReferencePublications (PubMed IDs)
JAK3 Tclin Tyrosine-protein kinase JAK3 (8349 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
JAK1 Tclin Tyrosine-protein kinase JAK1 (8569 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
JAK2 Tclin Tyrosine-protein kinase JAK2 (12915 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
TYK2 Tclin Tyrosine-protein kinase TYK2 (5029 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Associated Targets(non-human)

Hdac6 Histone deacetylase 6 (222 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
rep Replicase polyprotein 1ab (378 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID
SARS-CoV-2 (38078 Activities)
Activity TypeRelationActivity valueUnitsAction TypeJournalPubMed IddoiAssay Aladdin ID

Names and Identifiers

IUPAC Name N-[5-[4-(3,3-dimethylazetidine-1-carbonyl)phenyl]-[1,2,4]triazolo[1,5-a]pyridin-2-yl]cyclopropanecarboxamide
INCHI InChI=1S/C22H23N5O2/c1-22(2)12-26(13-22)20(29)16-10-6-14(7-11-16)17-4-3-5-18-23-21(25-27(17)18)24-19(28)15-8-9-15/h3-7,10-11,15H,8-9,12-13H2,1-2H3,(H,24,25,28)
InChi Key MPYACSQFXVMWNO-UHFFFAOYSA-N
Canonical SMILES CC1(CN(C1)C(=O)C2=CC=C(C=C2)C3=CC=CC4=NC(=NN43)NC(=O)C5CC5)C
Isomeric SMILES CC1(CN(C1)C(=O)C2=CC=C(C=C2)C3=CC=CC4=NC(=NN43)NC(=O)C5CC5)C
PubChem CID 44603362
Molecular Weight 389.45

Certificates

Certificate of Analysis(COA)

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2 results found

Lot NumberCertificate TypeDateItem
F2218528Certificate of AnalysisApr 02, 2024 S413366
F2218530Certificate of AnalysisApr 02, 2024 S413366

Chemical and Physical Properties

SolubilitySolubility (25°C) In vitro DMSO: 30 mg/mL (77.03 mM); Ethanol: 3 mg/mL (7.7 mM); Water: Insoluble;
DMSO(mg / mL) Max Solubility30
DMSO(mM) Max Solubility77.0317113878547
Water(mg / mL) Max Solubility<1

Related Documents

References

1. Kahl L, Patel J, Layton M, Binks M, Hicks K, Leon G, Hachulla E, Machado D, Staumont-Sallé D, Dickson M et al..  (2016)  Safety, tolerability, efficacy and pharmacodynamics of the selective JAK1 inhibitor GSK2586184 in patients with systemic lupus erythematosus..  Lupus,  25  (13): (1420-1430).  [PMID:27055521]
2. Ludbrook VJ, Hicks KJ, Hanrott KE, Patel JS, Binks MH, Wyres MR, Watson J, Wilson P, Simeoni M, Schifano LA et al..  (2016)  Investigation of selective JAK1 inhibitor GSK2586184 for the treatment of psoriasis in a randomized placebo-controlled phase IIa study..  Br J Dermatol,  174  (5): (985-95).  [PMID:26785220]

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