Spleen Tyrosine Kinase (Syk)

Inhibitor of Src/Syk tyrosine kinases

R788 disodium (R788 Disodium) is the oral prodrug of the active compound R406.

GS-9973 (GS-9973) is an orally bioavailable, selective Syk inhibitor with an IC50 of 7.7 nM.

R406 is an orally available spleen tyrosine kinase (Syk) inhibitor with an IC 50 value of 41nM and competitive inhibitor for ATP binding with a K i of 30nM

Cerdulatinib (PRT062070) (PRT062070) is a selective Tyk2 inhibitor with an IC50 of 0.5 nM. Cerdulatinib (PRT062070) (PRT062070) also is a dual JAK and SYK inhibitor with IC50s of 12, 6, 8 and 32 for JAK1, 2, 3 and SYK, respectively.

novel Syk inhibitor

Syk inhibitor

Syk inhibitor

Fostamatinib (R788) disodium hexahydrate is the oral prodrug of the active compound R406.

BAY 61-3606 is a potent and selective inhibitor of Syk kinase with a K i value of 7.5nM.

TAK-659 hydrochloride is a potent, selective and orally available spleen tyrosine kinase (Syk) inhibitor with an IC50 of 3.2 nM.

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.

PRT062607 (P505-15)(P505-15; PRT-2607; BIIB-057) is a highly specific and potent inhibitor of Syk with IC50 of 1-2 nM; >80-fold selective for Syk than Fgr, Lyn, FAK, Pyk2 and Zap70.

Gusacitinib (ASN-002) (ASN-002) is an orally active and potent dual inhibitor of spleen tyrosine kinase (SYK) and janus kinase (JAK) with IC50 values of 5-46 nM. Gusacitinib (ASN-002) has anti-cancer activity in both solid and hematological tumor types.

A Syk inhibitor

A Syk inhibitor

TAK-659 is a highly potent, selective, reversible and orally available dual inhibitor of spleen tyrosine kinase (SYK) and fms related tyrosine kinase 3 (FLT3), with an IC50 of 3.2 nM and 4.6 nM for SYK and FLT3, respectively. TAK-659 induces cell death in tumor cells but not in nontumor cells, and with potential for the treatment of chronic lymphocytic leukemia (CLL).

Lanraplenib succinate (GS-9876 succinate) is a highly selective and orally active SYK inhibitor (IC50=9.5 nM) in development for the treatment of inflammatory diseases.

Spleen tyrosine kinase (Syk) is a non-receptor tyrosine kinase that upon phosphorylation binds to immunoreceptor tyrosine-based activation motifs and mediates downstream signaling.

Syk-IN-1 (compound 4) is a potent Syk inhibitor, with an IC50 of 35 nM.

SRX3207 is an orally active and first-in-class dual Syk/PI3K inhibitor, with IC50 values of 10.7 nM and 861 nM for Syk and PI3Kα, respectively. SRX3207 relieves tumor immunosuppression.

Syk-IN-4 is a potent, selective and orally bioavailable SYK inhibitor with an IC50 of 0.31 nM.