RIPK1 inhibitor 22b是一种选择性有效的 RIPK1 抑制剂，Kd 值为 4 nM，IC50值为 11 nM。在实验性 B16 黑色素瘤肺转移模型中表现出优异的抗转移活性。 体外活性 在TSZ诱导的HT29细胞坏死模型中，RIPK1 inhibitor 22b 显示出强大的细胞保护效果（EC50为2nM）。RIPK1 inhibitor 22b 对多个其他激酶（Flt4、TrkA、TrkB、TrkC、Axl、HRI、Mer和MAP4K5）也表现出显著活性，其IC50分别为20、26、8、7、35、26、29和27nM。 RIPK1 inhibitor 22b is a potent and selective inhibitor of RIPK1(Kd of 4 nM and an enzymatic IC50 of 11 nM),andexhibits excellent antimetastasis activity in the experimental B16 melanoma lung metastasis model. In vitro activity In the TSZ-induced HT29 cell necroptosis model, RIPK1 inhibitor 22b shows potent cell protection effect (EC50 of 2nM). RIPK1 inhibitor 22b displays considerable activity against several other kinases(Flt4, TrkA, TrkB, TrkC, Axl, HRI, Mer, and MAP4K5 with IC50s of 20, 26, 8, 7, 35, 26, 29, and 27 nM, respectively).
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RIPK1 inhibitor 22b（RIPK1-IN-7）
CAS number：2300982-44-7 molecular formula：C25H22F3N5O2
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| Chinese alias | - | ||
| English alias | RIPK1-IN-7 | 1-(5-(4-Amino-7-ethyl-7H-pyrrolo[2,3-d]pyrimidin-5-yl)indolin-1-yl)-2-(3-(trifluoromethoxy)phenyl)ethan-1-one | ||
| CAS number | 2300982-44-7 | molecular formula | C25H22F3N5O2 |
| molecular weight | 481.47 g/mol | Exact mass | - |
| PSA | 86.300 Ų | logp | 4.400 |
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