| Bioactivity | 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]. | ||||||||||||
| Target | IC50: <3 nM (c-terminal Src kinase in CSK HTRF assay), 4 nM (c-terminal Src kinase in Caliper assay) | ||||||||||||
| In Vivo | 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]. | ||||||||||||
| Name | Src Inhibitor 3 | ||||||||||||
| CAS | 2380027-49-4 | ||||||||||||
| Formula | C34H32ClFN8O4 | ||||||||||||
| Molar Mass | 671.12 | ||||||||||||
| Appearance | Solid | ||||||||||||
| Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
| Storage |
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| 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. |