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Cbl-b-IN-2 (Example 8) 是一种口服有效的生物化合物,可抑制泛素蛋白酶体通路中的 E3 酶 Casitas b系淋巴瘤原癌基因-b (Cbl-b)。Cbl-b-IN-2 可用于调节免疫系统和易受免疫系统调节的疾病。Cbl-b-IN-2 (Example 8) 还可单独或与一种或多种免疫检查点抑制剂,抗肿瘤剂和放射剂联合应用于癌症。
Cbl-b-IN-2 (Example 8) is an orally bioavailable compound, can inhibit the E3 enzyme Casitas B-lineage lymphoma proto-oncogene-b (Cbl-b) in the ubiquitin Showed Cbl-b activity with an with IC50 values range of 5.1-100 nM and ﹤1 nM in high and low concentration of Cbl-b, respectively.
[1]. Arthur T. Sands, et al. 3-substituted piperidine compounds for cbl-b inhibition, and use of a cbl-b inhibitor in combination with a cancer vaccine and/or oncolytic virus. Patent WO 2020210508A1.
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