Bioactivity | 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 proteasome pathway. Cbl-b-IN-2 can be used to modulate the immune system and diseases amenable to immune system modulation. Cbl-b-IN-2 (Example 8) also may be administered to an individual with cancer, either alone or as part of a combination, with one or more of an immune checkpoint inhibitor, an anti-neoplastic agent, and radiation agent[1]. | ||||||||||||
Invitro | Cbl-b-IN-2 (Example 8) is a Cbl-b inhibitor with IC50 values range of 5.1-100 nM and ﹤1 nM in high and low concentration of Cbl-b, respectively[1]. Cell Viability Assay[1] Cell Line: | ||||||||||||
Name | Cbl-b-IN-2 | ||||||||||||
CAS | 2503325-21-9 | ||||||||||||
Formula | C29H30F5N5O2 | ||||||||||||
Molar Mass | 575.57 | ||||||||||||
Appearance | Solid | ||||||||||||
Transport | Room temperature in continental US; may vary elsewhere. | ||||||||||||
Storage |
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Reference | [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. |