Solcitinib | GSK2586184 | GLPG0778 | GSK2586184A | CAS#1206163-45-2 | JAK inhibitor

MedKoo Cat#: 206141 | Name: Solcitinib

Description:

WARNING: This product is for research use only, not for human or veterinary use.

Solcitinib, also known as GSK2586184 or GLPG0778, is a Janus kinase 1 (JAK1) inhibitor. Solcitinib may be potential useful for treatment of psoriasis，systemic lupus erythematosus, ulcerative colitis.

Chemical Structure

Solcitinib

CAS#1206163-45-2

Theoretical Analysis

MedKoo Cat#: 206141

Name: Solcitinib

CAS#: 1206163-45-2

Chemical Formula: C22H23N5O2

Exact Mass: 389.1852

Molecular Weight: 389.45

Elemental Analysis: C, 67.85; H, 5.95; N, 17.98; O, 8.22

Price and Availability

Size	Price	Availability
5mg	USD 90.00	Ready to ship
10mg	USD 150.00	Ready to ship
25mg	USD 250.00	Ready to ship
50mg	USD 450.00	Ready to ship
100mg	USD 750.00	Ready to ship

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Related CAS #

No Data

Synonym

GSK2586184; GSK 2586184; GSK-2586184; GSK2586184A; GSK-2586184A; GSK 2586184A; GLPG-0778; GLPG 0778; GLPG0778; G154578; Solcitinib.

IUPAC/Chemical Name

N-(5-(4-(3,3-dimethylazetidine-1-carbonyl)phenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl)cyclopropanecarboxamide

InChi Key

MPYACSQFXVMWNO-UHFFFAOYSA-N

InChi Code

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)

SMILES Code

O=C(C1CC1)NC2=NN3C(C4=CC=C(C(N5CC(C)(C)C5)=O)C=C4)=CC=CC3=N2 .

Appearance

Solid powder

Purity

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

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, DMF, and ethanol

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

More Info

Product Data

Product Data

Certificate of Analysis

View CoA: current batch, Lot#BBC51123

QC Data

View QC data: current batch, Lot#BBC51123

Safety Data Sheet (SDS)

View Safety Data Sheet (SDS)

Instruction

View handling instruction

Biological target:

Solcitinib is a JAK1 inhibitor with an IC50 of 9.8 nM.

In vitro activity:

To be determined

In vivo activity:

This study demonstrates that 12 weeks of treatment with solcitinib resulted in clinical improvement and was generally well tolerated in patients with moderate-to-severe plaque-type psoriasis. Improvement in itch and quality of life were observed at all doses of solcitinib with the greatest improvement seen in the 400-mg dose group. The incidence of adverse events was similar across treatment groups; there was no relationship between frequency of adverse effects and solcitinib dose. Reference: Br J Dermatol. 2016 May;174(5):985-95. https://pubmed.ncbi.nlm.nih.gov/26785220/

	Solvent	mg/mL	mM
Solubility
	DMF	2.0	5.14
	DMSO	5.0	12.84
	Ethanol	1.0	2.57

Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 389.45 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:

1. De Vries LCS, Ludbrook VJ, Hicks KJ, D'Haens GR. GSK2586184, a JAK1 selective inhibitor, in two patients with ulcerative colitis. BMJ Case Rep. 2017 Aug 7;2017:bcr2017221078. doi: 10.1136/bcr-2017-221078. PMID: 28790099; PMCID: PMC5624036. 2. Ludbrook VJ, Hicks KJ, Hanrott KE, Patel JS, Binks MH, Wyres MR, Watson J, Wilson P, Simeoni M, Schifano LA, Reich K, Griffiths CE. Investigation of selective JAK1 inhibitor GSK2586184 for the treatment of psoriasis in a randomized placebo-controlled phase IIa study. Br J Dermatol. 2016 May;174(5):985-95. doi: 10.1111/bjd.14399. Epub 2016 Apr 7. PMID: 26785220.

In vitro protocol:

To be determined

In vivo protocol:

1. Bapat AS, O'Connor CH, Schwertfeger KL. Targeting the NF-κB pathway enhances responsiveness of mammary tumors to JAK inhibitors. Sci Rep. 2023 Apr 1;13(1):5349. doi: 10.1038/s41598-023-32321-0. PMID: 37005447; PMCID: PMC10067805.