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CAS No.: 1206163-45-2

Solcitinib/索西替尼 Catalog No. CSN15697

Synonyms: GSK-2586184;GLPG-0778;GSK-2586184A

Solcitinib is a highly selective JAK1 inhibitor with IC50 value of 9.8 nM, with much less potency against JAK1 and JAK2 with IC50 values >100nM.

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实验方案

技术信息

生物活性

描述The Janus kinase and Signal Transducer and Activator of Transcription protein (JAK/STAT) pathway is known to be involved in inflammatory and neoplastic skin diseases, like psoriasis, atopic dermatitis, alopecia areata, vitiligo and melanoma. JAKs, a small family of kinases - JAK1, JAK2, JAK3 and Tyrosine Kinase 2 (TYK2), bind directly to the intracellular domains of Type I/II cytokine receptors and not to other classes of cytokine receptors. JAKs are located at the cytoplasmic tail of various cytokine receptors, and are activated upon receptor-ligand interaction. Due to the kinase activity, JAK activation results in auto-phosphorylation as well as phosphorylation of the cytokine receptor chains, and the combination of JAKs and the receptor form specific binding sites for one or more members of the STAT [signal transducer and activator of transcription] family. GSK2586184 (Solcitinib) is an orally active, competitive, potent, selective JAK1 inhibitor. In biochemical phosphorylation assays, GSK2586184 has an IC ₅₀ of 9.8 nM, and shows 11-, 55- and 23-fold selectivity over JAK2, JAK3 and TYK2, respectively^[2]. GSK2586184 was administered in two patients 400 mg twice daily for 48 days with moderate-to-severe ulcerative colitis (UC). The result showed that the JAK1 selective inhibitor GSK2586184 was well tolerated and induced clinical and endoscopic response in two patients with moderate-to-severe UC. GSK2586184, a Janus kinase 1 selective inhibitor, induced clinical and endoscopic response in ulcerative colitis, however, the study was discontinued at an early stage due to liver toxicity observed in systemic lupus patients receiving the drug^[3].
作用机制A ring nitrogen and the hydrogen associated with the adjacent exocyclic amine are involved in binding to the hinge region of the JAK1 kinase. This places the conserved cyclopropyl group in a lipophilic pocket.
参考文献

[1] Adwan MH. Drug Reaction with Eosinophilia and Systemic Symptoms (DRESS) Syndrome and the Rheumatologist. Curr Rheumatol Rep. 2017 Jan;19(1):3.
[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.
[3] 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.

实验方案

计算器摩尔计算器总药量计算器工作液计算器
储存液制备
- 1 mg
- 5 mg
- 10 mg
- 1 mM
- 2.5677 mL
- 12.8386 mL
- 25.6772 mL
- 5 mM
- 0.5135 mL
- 2.5677 mL
- 5.1354 mL
- 10 mM
- 0.2568 mL
- 1.2839 mL
- 2.5677 mL

技术信息

CAS号

1206163-45-2

储存条件

粉末: Keep in dark place,Inert atmosphere,Room temperature

液体: -20°C:3-6 月 -80°C:12月

分子式

C22H23N5O2

运输

蓝冰

分子量

389.45

别名

GSK-2586184;GLPG-0778;GSK-2586184A;G154578;索西替尼

溶解度

DMSO	30.0 mg/mL (77.0 mM)
Water	Insoluble
Ethanol	3.0 mg/mL (7.7 mM)

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