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

MedKoo CAT#: 206141

CAS#: 1206163-45-2

Description: 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

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Solcitinib
CAS# 1206163-45-2
Product data Instruction

Theoretical Analysis

MedKoo Cat#: 206141
Name: Solcitinib
CAS#: 1206163-45-2
Chemical Formula: C22H23N5O2
Exact Mass: 389.19
Molecular Weight: 389.450
Elemental Analysis: C, 67.85; H, 5.95; N, 17.98; O, 8.22

Price and Availability

Size Price Availability Quantity
5mg USD 90 Ready to ship
10mg USD 150 Ready to ship
25mg USD 250 Ready to ship
50mg USD 450 Ready to ship
100mg USD 750 Ready to ship
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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:         

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/

Solubility Data

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

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.

Recalculate based on batch purity %
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. 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.

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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.