One of the final two orphan receptor tyrosine kinases is the transmembrane proto-oncogene receptor tyrosine kinase (RTK) ROS. During development, its typical expression pattern is severely spatiotemporally constrained. Numerous cancers, including glioblastoma multiforme and non-small cell lung cancer, have been reported to produce variable mutant forms of ROS kinase as well as exhibit its ectopic expression, raising the possibility that this enzyme contributes to the development of these tumors. Researchers have begun to consider ROS inhibition as a strategy for the development of new male contraceptives in light of the theory that the c-ROS gene may play a role in some cardiovascular diseases and the observation that homozygous male mice targeted against the c-ROS gene are healthy but infertile.
In glioblastoma, non-small-cell lung cancer (NSCLC), and other neoplasms, ROS1, a transmembrane receptor tyrosine kinase proto-oncogene, has been shown to rearrange with several genes, including intrachromosomal fusion with GOPC as a result of microdeletions at 6q22.1. The presence of ROS1 fusion events in these tumors is significant because they may be amenable to treatment with newer tyrosine kinase inhibitors.
| Structure | Cat No. | Product Name | CAS No. | Product Description |
|---|---|---|---|---|
|
V69267 | APG-2449 | 2196186-84-0 | APG-2449 is an orally bioactive ALK/ROS1/FAK inhibitor (antagonist) with anti-tumor activity in non-small cell lung cancer (NSCLC) mouse models. |
|
V69556 | Keap1-Nrf2-IN-11 | 2796292-75-4 | Keap1-Nrf2-IN-11 is a Keap1-Nrf2 inhibitor (antagonist) with a KD2 value of 0.21 nM. |
|
V69560 | Lamalbid | 52212-87-0 | Lamalbid is a naturally occurring compound found in Lantana montevidensis. |
|
V69561 | Pinealon | 175175-23-2 | Pinealon is a 3-amino acid (AA) peptide with neuro-protection properties. |
|
V76609 | PRDX1-IN-1 | PRDX1-IN-1 is a selective inhibitor of PRDX1 with IC50 of 0.164 μM. | |
|
V69559 | Protein kinase inhibitor 4 | 2278205-04-0 | Protein kinase inhibitor 4 (Compound 3) is a protein kinase inhibitor that can suppress TRK-A and ROS1 (IC50= 3.0 nM and 104 nM, respectively). |
|
V2757 | Repotrectinib (TPX-0005) | 1802220-02-5 | Repotrectinib (TPX-0005, TPX0005) is a novel, oral, rationally-designed, highly potent inhibitor of ALK/ROS1/TRK with IC50of 5.3 nM, 1.01 nM, 1.26 nM and 1.08 nM for SRC, WT ALK, ALK G1202R and ALK L1196M, respectively. |
|
V69557 | ROS kinases-IN-1 | 370096-57-4 | ROS kinases-IN-1 (pag 98) is a ROS tyrosine kinase inhibitor (antagonist) with IC50 of 1.22 μM. |
|
V69562 | ROS kinases-IN-2 | 687576-28-9 | ROS kinases-IN-2 is a ROS kinase inhibitor (antagonist) with an inhibition rate of 21.53% at 10 μM. |
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V69558 | ROS1-IN-1 | 2883232-34-4 | ROS1-IN-1 (Compound 31) is a potent and specific ROS1 kinase inhibitor (antagonist) with IC50 of 0.097 μM. |
|
V69555 | Taletrectinib (DS-6051b; AB-106; IBI-344) | 1505515-69-4 | Taletrectinib (DS-6051b) is a potent, orally bioactive, next-generation selective ROS1/NTRK inhibitor. |
|
V51179 | Zidesamtinib (NVL-520) | 2739829-00-4 | inhibitor of diverse ROS1 fusions and resistance mutations |
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