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R406 (free base)

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].

Product Specifications

CAS Number

[841290-80-0]

UNSPSC

12352005

Hazard Statement

H302, H315, H319, H335

Target

Apoptosis; FLT3; Syk

Type

Reference compound

Related Pathways

Apoptosis; Protein Tyrosine Kinase/RTK

Applications

COVID-19-immunoregulation

Field of Research

Inflammation/Immunology; Cancer

Assay Protocol

https://www.medchemexpress.com/R406-free-base.html

Purity

99.07

Solubility

DMSO : 25 mg/mL (ultrasonic; warming; heat to 60°C)

Smiles

COC1=CC(NC2=NC(NC3=NC(N4)=C(C=C3)OC(C)(C)C4=O)=C(C=N2)F)=CC(OC)=C1OC

Molecular Formula

C22H23FN6O5

Molecular Weight

470.45

Precautions

H302, H315, H319, H335

References & Citations

[1]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.|[2]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.

Shipping Conditions

Room Temperature

Storage Conditions

-20°C, 3 years; 4°C, 2 years (Powder)

Scientific Category

Reference compound1

Clinical Information

No Development Reported

Citation 01

Adv Mater. 2024 Mar 15:e2311283.|Harvard Medical School LINCS LIBRARY|iScience. 2024 Jan 11;27 (2) :108869.|Mater Today Bio. 2024 Mar 22:26:101037.|Nature. 2025 Nov 26.|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.|bioRxiv. 2022 Dec 21, 519945.|bioRxiv. 2024 Apr 9.|Blood Adv. 2024 Nov 12;8 (21) :5653-5662.|BMC Cardiovasc Disord. 2024 Jul 12;24 (1) :354.|Cell Commun Signal. 2024 Apr 2;22 (1) :210.|Cell Death Dis. 2025 Aug 7;16 (1) :595.|Cell Rep Med. 2025 Jan 16:101922.|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.|iScience. 2024 Jun 28;27 (7) :110415.|iScience. 2024 Mar 27;27 (4) :109607.|J Biol Chem. 2018 Apr 27;293 (17) :6410-6433.|J Neuroinflammation. 2024 Dec 3;21 (1) :318.|J Pharmacol Sci. 2017 May;134 (1) :29-36.|Life Metab. 2025 Jan 29;4 (2) :loaf002.|Mol Immunol. 2024 Jul 31:173:88-98.|Nat Commun. 2022 Apr 19;13 (1) :2136.|Nihon University. School of Medicine. 2014 Mar.|Redox Biol. 2022 Oct:56:102461.|Scand J Immunol. 2024 Apr 26:e13371.|Stony Brook University. 2025.|Theranostics. 2021 May 24;11 (15) :7308-7321.

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