GSK SYK inhibitor

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

MedKoo CAT#: 208247

CAS#: 1345485-66-3

Description: 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

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GSK SYK inhibitor
CAS# 1345485-66-3
Instruction

Theoretical Analysis

MedKoo Cat#: 208247
Name: GSK SYK inhibitor
CAS#: 1345485-66-3
Chemical Formula: C21H27FN6
Exact Mass: 382.23
Molecular Weight: 382.490
Elemental Analysis: C, 65.94; H, 7.12; F, 4.97; N, 21.97

Price and Availability

This product is not in stock, which may be available by custom synthesis. For cost-effective reason, minimum order is 1g (price is usually high, lead time is 2~3 months, depending on the technical challenge). Quote less than 1g will not be provided. To request quote, please email to sales @medkoo.com or click below button.
Note: Price will be listed if it is available in the future.

Request quote for custom synthesis

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:

Biological target:
In vitro activity:
In vivo activity:

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.

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:
In vitro protocol:
In vivo protocol:

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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