| Customization: | Available |
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| Powder: | Yes |
| Customized: | Customized |
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| Product Name | Repotrectinib |
| Color | White to Off-white |
| Shelf Life | 2Years |
| Sample | Available |
| Test Method | HPLC,UV |
Repotrectinib is a small (low molecular weight), macrocyclic tyrosine kinase inhibitor of ROS1, TRK and ALK. Repotrectinib was designed to efficiently bind with the active kinase conformation and avoid steric interference from a variety of clinically resistant mutations. The compact and rigid three-dimensional structure enables repotrectinib to precisely and efficiently bind deep into the ATP binding pocket of the kinase, and potentially circumvent the steric interference that results in resistance to bulkier kinase inhibitors, especially the solvent-front and gatekeeper mutations of ROS1, TRK and ALK kinases.
Repotrectinib is a next generation ROS1 inhibitor, a novel three-dimensional macrocyle with a much smaller size (MW <370) than current ROS1 inhibitors. It was specifically designed to overcome resistance mutations. Preclinical studies have shown activity against gatekeeper and solvent mutations, including G2032R, D2033N, L2026M, S1986F/Y, L1951R, and kinases involved in bypass signaling such as focal adhesion kinase, SRC proto-oncogene, and non-receptor tyrosine kinase.
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