| Bioactivity | 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]. |
| Invitro | VAV1 degrader-3 (0-1 μM, 24 h) 抑制 B 细胞受体介导的活性，具体而言，VAV1 degrader-3 抑制从人血白细胞分离的 PBMC 细胞中的 CD69 表达和 IL-6、lgG 分泌[1]。VAV1 degrader-3 (0-1 μM, 24 h) 抑制原代 T 细胞中 T 细胞受体介导的 CD69 活化、IL-2 分泌和增殖[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. 0 --> VAV1 degrader-3 相关抗体: |
| In Vivo | VAV1 degrader-3 (1-15 mg/kg，口服) 可抑制 MOGss-ss 诱发的多发性硬化症实验性自身免疫性脑脊髓炎 (EAE) 小鼠模型中的疾病进展[1]。VAV1 degrader-3 (1 mg/kg，口服) 可抑制 T 细胞转移诱发的结肠炎模型中的疾病进展，并降低结肠组织中钙卫蛋白亚基 (S100a8/S100a9) 的表达[1]。VAV1 degrader-3 (1 mg/kg，口服) 还可抑制胶原诱发性关节炎 (CIA) 小鼠模型中的疾病进展[1]。 MCE has not independently confirmed the accuracy of these methods. They are for reference only. |
| CAS | 3050683-38-7 |
| Formula | C22H17ClN2O3 |
| Molar Mass | 392.83 |
| Transport | Room temperature in continental US; may vary elsewhere. |
| Storage | Please store the product under the recommended conditions in the Certificate of Analysis. |
| Reference | [1]. Laura Ann Mcallister, et al. Targeted degradation of vav1. Patent. WO2024151547A1. |
VAV1 degrader-3
CAS: 3050683-38-7 F: C22H17ClN2O3 W: 392.83
VAV1 degrader-3 (Example 185) is an orally active VAV1 molecular glue degrader (DC50: 7 nM). VAV1 degrader-3 reduces imm
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