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Chemical Structure : NVL-520
Catalog No.: PC-49635Not For Human Use, Lab Use Only.
Zidesamtinib (NVL-520, NVL520) is a potent, selective, TRK-sparing, and brain-penetrant inhibitor of ROS1 fusions and secondary resistance mutations with IC50 of 0.5-3.5 nM, and 12 nM for ROS1 WT.
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Zidesamtinib (NVL-520, NVL520) is a potent, selective, TRK-sparing, and brain-penetrant inhibitor of ROS1 fusions and secondary resistance mutations with IC50 of 0.5-3.5 nM, and 12 nM for ROS1 WT.
Zidesamtinib (NVL-520) displays >50-fold ROS1 selectivity over 98% of the kinome tested.
Zidesamtinib (NVL-520) is active in vitro against diverse ROS1 fusions and resistance mutations and exhibits 10-to-1,000-fold improved potency for the ROS1 G2032R solvent-front mutation over crizotinib, entrectinib, lorlatinib, taletrectinib, and repotrectinib.
Zidesamtinib (NVL-520) induces tumor regression in G2032R-inclusive intracranial and patient-derived xenograft models.
NVL-520 has a ~100-fold increased potency for ROS1 and ROS1 G2032R over TRK.
In clinical investigations, NVL-520 elicited objective tumor responses in three patients with TKI-refractory ROS1 fusion-positive lung cancers, including two with ROS1 G2032R and one with intracranial metastases, with no observed neurological toxicities.
| M.Wt | 419.46 | |
| Formula | C22H22FN7O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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1. Alexander Drilon, et al. Cancer Discov. 2022 Dec 13;CD-22-0968.
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