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R406 (free base)
$50 – $680
Products Details
Product Description
– R406 free base is an orally available and competitive Syk/FLT3 inhibitor for ATP binding with a Ki of 30 nM, potently inhibits Syk kinase activity in vitro with an IC50 of 41 nM, measured at an ATP concentration corresponding to its Km value. R406 free base reduces immune complex-mediated inflammation[1]. R406 free base also inhibits Lyn (IC50=63 nM) and Lck (IC50=37 nM)[2].
Web ID
– HY-11108
Storage Temperature
– -20°C, 3 years; 4°C, 2 years (Powder)
Shipping
– Room Temperature
Applications
– COVID-19-immunoregulation
Molecular Formula
– C22H23FN6O5
Citations
– Harvard Medical School LINCS LIBRARY|Sci Transl Med. 2018 Jul 18;10(450):eaaq1093.|SSRN. 2023 Jun 29.|ACS Infect Dis. 2021 Mar 12;7(3):661-671.|Ann Transl Med. 2019 Dec;7(23):758.|Arthritis Rheumatol. 2018 Sep;70(9):1419-1428. |Atherosclerosis. 2019 Oct;289:132-142.|Cell Rep. 2023 Mar 20;42(3):112275.|Cell. 2018 Oct 4;175(2):442-457.e23.|Exp Hematol Oncol. 2022 Nov 8;11(1):88.|Front Pharmacol. 2022 May 5;13:885053.|J Biol Chem. 2018 Apr 27;293(17):6410-6433.|J Pharmacol Sci. 2017 May;134(1):29-36.|Nat Commun. 2022 Apr 19;13(1):2136.|Nihon University. School of Medicine. 2014 Mar.|Redox Biol. 3 September 2022, 102461.|Theranostics. 2021 May 24;11(15):7308-7321.
References
– [1]Hoon-Suk Cha , et al. A novel spleen tyrosine kinase inhibitor blocks c-Jun N-terminal kinase-mediated gene expression in synoviocytes. J Pharmacol Exp Ther. 2006 May;317(2):571-8.|[2]Sylvia Braselmann, et al. R406, an orally available spleen tyrosine kinase inhibitor blocks fc receptor signaling and reduces immune complex-mediated inflammation. J Pharmacol Exp Ther. 2006 Dec;319(3):998-1008.
CAS Number
– 841290-80-0
Molecular Weight
– 470.45
Compound Purity
– 99.80
SMILES
– COC1=CC(NC2=NC(NC3=NC(N4)=C(C=C3)OC(C)(C)C4=O)=C(C=N2)F)=CC(OC)=C1OC
Clinical Information
– No Development Reported
Research Area
– Inflammation/Immunology; Cancer
Solubility
– DMSO : 25 mg/mL (ultrasonic;warming;heat to 60°C)
Target
– Apoptosis;FLT3;Syk
Pathway
– Apoptosis;Protein Tyrosine Kinase/RTK
Product type
– Reference compound
Disclaimer: All products are for research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation.
