GSK SYK inhibitor | CAS#1345485-66-3 | Inhibitor

MedKoo Cat#: 208247 | Name: GSK SYK inhibitor

Description:

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

The immunoregulator spleen tyrosine kinase (SYK) is upregulated in cutaneous lupus erythematosus (CLE). This double-blind, multicentre, Phase Ib study evaluated the safety, tolerability, pharmacokinetics, pharmacodynamics and clinical efficacy of the selective SYK inhibitor GSK2646264 in active CLE lesions

Chemical Structure

GSK SYK inhibitor

CAS#1345485-66-3

Theoretical Analysis

MedKoo Cat#: 208247

Name: GSK SYK inhibitor

CAS#: 1345485-66-3

Chemical Formula: C21H27FN6

Exact Mass: 382.2281

Molecular Weight: 382.49

Elemental Analysis: C, 65.94; H, 7.12; F, 4.97; N, 21.97

Price and Availability

This product is currently not in stock but may be available through custom synthesis. To ensure cost efficiency, the minimum order quantity is 1 gram. The estimated lead time is 2 to 4 months, with pricing dependent on the complexity of the synthesis (typically high for intricate chemistries). Quotes for quantities below 1 gram will not be provided. To request a quote, please click the button below. Note: If this product becomes available in stock in the future, pricing will be listed accordingly.

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Related CAS #

No Data

Synonym

GSKSYKinhibitor, GSK-SYK inhibitor, GSK-SYK-inhibitor

IUPAC/Chemical Name

7-(1-tert-Butylpyrazol-4-yl)-N-[(3-fluoropiperidin-3-yl)methyl]-1,6-naphthyridin-5-amine

InChi Key

KZHRNYBKXGVNJT-UHFFFAOYSA-N

InChi Code

InChI=1S/C21H27FN6/c1-20(2,3)28-12-15(11-26-28)17-10-18-16(6-4-9-24-18)19(27-17)25-14-21(22)7-5-8-23-13-21/h4,6,9-12,23H,5,7-8,13-14H2,1-3H3,(H,25,27)

SMILES Code

FC1(CNC2=C3C=CC=NC3=CC(C4=CN(C(C)(C)C)N=C4)=N2)CNCCC1

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

To be determined

Shelf Life

>2 years if stored properly

Drug Formulation

To be determined

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

Instruction

View handling instruction

Preparing Stock Solutions

The following data is based on the product molecular weight 382.49 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

1: Audia S, Bonnotte B. Emerging Therapies in Immune Thrombocytopenia. J Clin Med. 2021 Mar 2;10(5):1004. doi: 10.3390/jcm10051004. PMID: 33801294; PMCID: PMC7958340. 2: Morschhauser F, Feugier P, Flinn IW, Gasiorowski R, Greil R, Illés Á, Johnson NA, Larouche JF, Lugtenburg PJ, Patti C, Salles GA, Trněný M, de Vos S, Mir F, Samineni D, Kim SY, Jiang Y, Punnoose E, Sinha A, Clark E, Spielewoy N, Humphrey K, Bazeos A, Zelenetz AD. A phase 2 study of venetoclax plus R-CHOP as first- line treatment for patients with diffuse large B-cell lymphoma. Blood. 2021 Feb 4;137(5):600-609. doi: 10.1182/blood.2020006578. Erratum in: Blood. 2021 Apr 1;137(13):1844. PMID: 33538797; PMCID: PMC7869186. 3: Walker A, Erwig L, Foster K, Nevin K, Wenzel J, Worm M, Williams N, Ratia N, Hoang B, Schneider-Merck T, Gisbert S, Carnarius H, Dickson M. Safety, pharmacokinetics and pharmacodynamics of a topical SYK inhibitor in cutaneous lupus erythematosus: A double-blind Phase Ib study. Exp Dermatol. 2021 Nov;30(11):1686-1692. doi: 10.1111/exd.14253. Epub 2020 Dec 17. PMID: 33336508; PMCID: PMC8596667. 4: Roberts AW, Ma S, Kipps TJ, Coutre SE, Davids MS, Eichhorst B, Hallek M, Byrd JC, Humphrey K, Zhou L, Chyla B, Nielsen J, Potluri J, Kim SY, Verdugo M, Stilgenbauer S, Wierda WG, Seymour JF. Efficacy of venetoclax in relapsed chronic lymphocytic leukemia is influenced by disease and response variables. Blood. 2019 Jul 11;134(2):111-122. doi: 10.1182/blood.2018882555. Epub 2019 Apr 25. PMID: 31023700; PMCID: PMC6624969. 5: Denyer J, Patel V. Syk kinase inhibitors in allergic diseases. Drug News Perspect. 2009 Apr;22(3):146-50. doi: 10.1358/dnp.2009.22.3.1354124. PMID: 19440557. 6: Tang S, Yu Q, Ding C. Investigational spleen tyrosine kinase (SYK) inhibitors for the treatment of autoimmune diseases. Expert Opin Investig Drugs. 2022 Mar;31(3):291-303. doi: 10.1080/13543784.2022.2040014. Epub 2022 Feb 18. PMID: 35130124. 7: Kocatürk E, Maurer M, Metz M, Grattan C. Looking forward to new targeted treatments for chronic spontaneous urticaria. Clin Transl Allergy. 2017 Jan 10;7:1. doi: 10.1186/s13601-016-0139-2. Erratum in: Clin Transl Allergy. 2017 Apr 3;7:11. PMID: 28078079; PMCID: PMC5223554. 8: Lin TS. New agents in chronic lymphocytic leukemia. Curr Hematol Malig Rep. 2010 Jan;5(1):29-34. doi: 10.1007/s11899-009-0039-9. PMID: 20425394. 9: van Bree SH, Gomez-Pinilla PJ, van de Bovenkamp FS, Di Giovangiulio M, Farro G, Nemethova A, Cailotto C, de Jonge WJ, Lee K, Ramirez-Molina C, Lugo D, Skynner MJ, Boeckxstaens GE, Matteoli G. Inhibition of spleen tyrosine kinase as treatment of postoperative ileus. Gut. 2013 Nov;62(11):1581-90. doi: 10.1136/gutjnl-2012-302615. Epub 2012 Dec 13. PMID: 23242119. 10: Paris D, Ait-Ghezala G, Bachmeier C, Laco G, Beaulieu-Abdelahad D, Lin Y, Jin C, Crawford F, Mullan M. The spleen tyrosine kinase (Syk) regulates Alzheimer amyloid-β production and Tau hyperphosphorylation. J Biol Chem. 2014 Dec 5;289(49):33927-44. doi: 10.1074/jbc.M114.608091. Epub 2014 Oct 20. PMID: 25331948; PMCID: PMC425633