Src Inhibitor 3

• CAT Number: I017725
• CAS Number: 2380027-49-4
• Molecular Formula: C34H32ClFN8O4
• Molecular Weight: 671.12
• Purity: ≥95%
• Synonyms: N-[3-chloro-4-[(6-methoxypyrazolo[1,5-a]pyridine-3-carbonyl)amino]phenyl]-1-[1-(3-cyano-3-methylbutanoyl)piperidin-4-yl]-5-fluoroindazole-3-carboxamide
• InChI: InChI=1S/C34H32ClFN8O4/c1-34(2,19-37)16-30(45)42-12-10-22(11-13-42)44-29-8-4-20(36)14-24(29)31(41-44)33(47)39-21-5-7-27(26(35)15-21)40-32(46)25-17-38-43-18-23(48-3)6-9-28(25)43/h4-9,14-15,17-18,22H,10-13,16H2,1-3H3,(H,39,47)(H,40,46)
• InChIKey: LQQYARMJQBHKQQ-UHFFFAOYSA-N
• SMILES: CC(C)(CC(=O)N1CCC(CC1)N2C3=C(C=C(C=C3)F)C(=N2)C(=O)NC4=CC(=C(C=C4)NC(=O)C5=C6C=CC(=CN6N=C5)OC)Cl)C#N

Src Inhibitor 3 is a potent, orally active c-terminal Src kinase (CSK) with IC50 values below 3 nM and 4 nM in CSK HTRF and Caliper assay, respectively. Src Inhibitor 3 shows the ability to increase T cell proliferation induced by T cell receptor signaling[1].
Src Inhibitor 3 reduces inhibitory LCK phosphorylation in vivo upon oral dosing and shows the ability to enhance T cell activation in response to antigen stimulation[1].

Reference

[1]. O’Malley DP, et al. Discovery of Pyridazinone and Pyrazolo[1,5-a]pyridine Inhibitors of C-Terminal Src Kinase. ACS Med Chem Lett. 2019 Sep 25;10(10):1486-1491.
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