Syk-IN-4

• CAT Number: I045762
• CAS Number: 2932264-95-2
• Molecular Formula: C21H25N9O
• Molecular Weight: 419.48
• Purity: ≥95%
• Synonyms: 5-[[4-[4-[(dimethylamino)methyl]-3-methylpyrazol-1-yl]pyrimidin-2-yl]amino]-N,1-dimethylindazole-3-carboxamide
• InChI: InChI=1S/C21H25N9O/c1-13-14(11-28(3)4)12-30(26-13)18-8-9-23-21(25-18)24-15-6-7-17-16(10-15)19(20(31)22-2)27-29(17)5/h6-10,12H,11H2,1-5H3,(H,22,31)(H,23,24,25)
• InChIKey: IXNQUCOVJRJRGJ-UHFFFAOYSA-N
• SMILES: CC1=NN(C=C1CN(C)C)C2=NC(=NC=C2)NC3=CC4=C(C=C3)N(N=C4C(=O)NC)C

Syk-IN-4 is a potent, selective and orally bioavailable SYK inhibitor with an IC50 of 0.31 nM. SYK has emerged as a potential target for autoimmunity and hematological cancers[1].
Syk-IN-4 is a potent inhibitor of hERG with an IC50 of 3.0 μM[1].
Syk-IN-4 inhibits SUDHL-4 and T cell proliferation with GI50s of 0.24 and 2.6 µM, respectively[1].
Syk-IN-4 exhibits moderate oral bioavailability (60%) following oral administration (1 mg/kg) in male Hans Wistar rats[1].
Syk-IN-4 exhibits high plasma clearance (151 mL/min/kg) combined with large volumes of distribution (1.0 L/kg respectively) following i.v. administration (0.5 mg/kg) in male Hans Wistar rats[1].

Reference

[1]. Neil P Grimster, et al. Optimization of a Series of Potent, Selective and Orally Bioavailable SYK Inhibitors. Bioorg Med Chem Lett. 2020 Jul 24;127433.
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