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| | 3-(2-chloro-4'-(2-oxopyridin-1(2H)-yl)-[1,1'-biphenyl]-3-yl)piperidine-2,6-dione Basic information |
| | 3-(2-chloro-4'-(2-oxopyridin-1(2H)-yl)-[1,1'-biphenyl]-3-yl)piperidine-2,6-dione Chemical Properties |
| Boiling point | 643.897±55.00 °C(Press: 760.00 Torr)(predicted) | | density | 1.344±0.06 g/cm3(Temp: 25 °C; Press: 760 Torr)(predicted) | | pka | 10.502±0.40(predicted) | | form | Solid | | color | White to off-white |
| | 3-(2-chloro-4'-(2-oxopyridin-1(2H)-yl)-[1,1'-biphenyl]-3-yl)piperidine-2,6-dione Usage And Synthesis |
| Uses | VAV1 degrader-3 (Example 185) is an orally active VAV1 molecular glue degrader (DC50: 7 nM). VAV1 degrader-3 reduces immune cell activation, immune cell proliferation and the production of various cytokines. VAV1 degrader-3 can be used for research of inflammatory or autoimmune disorder. VAV1 degrader-3 inhibits disease progression in experimntal autoimmune encephalomyelitis (EAE) mouse model, Collagen-induced arthritis (CIA) mouse model, etc.[1]. | | in vivo | VAV1 degrader-3 (1-15 mg/kg, p.o.) inhibits disease progression in MOGss-ss-induced multiple sclerosis experimntal autoimmune encephalomyelitis (EAE) mouse model[1].
VAV1 degrader-3 (1 mg/kg, p.o.) inhibits disease progression and reduces expression of calprotectin subunits (S100a8/S100a9) within colon tissue in a T cell transfer-induced model of colitis[1].
VAV1 degrader-3 (1 mg/kg, p.o.) also inhibits disease progression collagen-induced arthritis (CIA) mouse model[1].
| | References | [1] Laura Ann Mcallister, et al. Targeted degradation of vav1. Patent. WO2024151547A1. |
| | 3-(2-chloro-4'-(2-oxopyridin-1(2H)-yl)-[1,1'-biphenyl]-3-yl)piperidine-2,6-dione Preparation Products And Raw materials |
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