| S2194 |
R406
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R406(R406 besylate) is a potent Syk inhibitor with IC50 of 41 nM in cell-free assays, strongly inhibits Syk but not Lyn, 5-fold less potent to Flt3. R406 induces apoptosis. Phase 1.
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J Allergy Clin Immunol, 2025, 155(2):569-582
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Int J Biol Sci, 2025, 21(12):5287-5304
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Front Immunol, 2025, 16:1636917
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| S1533 |
R406 (free base)
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R406 (free base) is a potent Syk inhibitor with IC50 of 41 nM in a cell-free assay, strongly inhibits Syk but not Lyn, 5-fold less potent to Flt3. This compound triggers apoptosis. Phase 1.
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Autophagy, 2025, 1-17.
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EMBO Rep, 2025, 10.1038/s44319-025-00444-2
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J Transl Med, 2024, 22(1):283
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| S8032 |
PRT062607 (P505-15) HCl
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PRT062607 (P505-15, BIIB057, PRT-2607) HCl is a novel, highly selective Syk inhibitor with IC50 of 1 nM in cell-free assays, >80-fold selective for Syk than Fgr, PAK5, Lyn, FAK, Pyk2, FLT3, MLK1 and Zap70.
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Sci Adv, 2025, 11(31):eadu4270
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Sci Rep, 2024, 14(1):7739
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J Exp Med, 2023, 220(9)e20230054
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| S7523 |
Entospletinib (GS-9973)
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Entospletinib (GS-9973) is an orally bioavailable, selective Syk inhibitor with IC50 of 7.7 nM in a cell-free assay. This compound showed 13- to >1000-fold cellular selectivity for Syk over other kinases (including Jak2, ckit, Flt3, Ret, KDR) as assessed by target protein phosphorylation or functional response.
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Cancer Res, 2023, 83(2):316-331
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Front Immunol, 2023, 14:1279155
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J Leukoc Biol, 2023, qiad025
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| S2625 |
Fostamatinib (R788)
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Fostamatinib (R788), a prodrug of the active metabolite R406, is a Syk inhibitor with IC50 of 41 nM. It strongly inhibits Syk but not Lyn, and is 5-fold less potent to Flt3. Phase 3.
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Autophagy, 2025, 1-17.
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Int Immunopharmacol, 2025, 148:114122
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Exp Ther Med, 2025, 29(6):110
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| S3026 |
Piceatannol
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Piceatannol, a natural stilbene, is a selective Syk inhibitor and ~10-fold selectivity versus Lyn.
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Autophagy, 2025, 1-17.
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Int J Mol Sci, 2025, 26(18)9134
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ACS Appl Mater Interfaces, 2022, 14(21):24144-24159
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| S2206 |
R788 (Fostamatinib) Disodium
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Fostamatinib disodium (R788, Tamatinib Fosdium), a prodrug of the active metabolite R406, is a Syk inhibitor with IC50 of 41 nM in a cell-free assay, strongly inhibits Syk but not Lyn, 5-fold less potent to Flt3. Phase 3.
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Autophagy, 2025, 1-17.
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Sci Rep, 2025, 15(1):25312
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FASEB J, 2024, 38(6):e23564
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| S7006 |
BAY 61-3606 dihydrochloride
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BAY 61-3606 dihydrochloride is a potent and selective inhibitor of Syk kinase (Ki = 7.5 nM). BAY-61-3606 induces cell cycle arrest and apoptosis.
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EMBO Rep, 2025, 10.1038/s44319-025-00444-2
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bioRxiv, 2025, 2025.05.30.657101
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Arterioscler Thromb Vasc Biol, 2024, 44(7):1646-1657
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| S7738 |
PRT-060318 2HCl
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PRT-060318 (PRT318) is a novel selective inhibitor of the Syk tyrosine kinase with an IC50 of 4 nM, as an approach to HIT treatment.
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Microbiol Spectr, 2025, 13(1):e0254921
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Cell Mol Life Sci, 2024, 82(1):14
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PLoS Pathog, 2024, 20(10):e1012674
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| S8442 |
TAK-659 Hydrochloride
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TAK-659 Hydrochloride is a potent and selective inhibitor of spleen tyrosine kinase (SYK) with an IC50 value of 3.2 nM. It is selective against most other kinases, but potent toward both SYK and FLT3.
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Exp Ther Med, 2025, 29(6):110
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Int J Mol Sci, 2024, 25(18)9914
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Int J Mol Sci, 2022, 23(23)14706
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