Scientific Reviews
Product Guides
Blogs
Topics
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!2025-02-06
82 Results for "
ROS1
" in MedChemExpress (MCE) Product Catalog:
Products (82)
82 Results for "ROS1" in MCE Product Catalog:
89
Target:
Ligands for Target Protein for PROTAC Anaplastic lymphoma kinase (ALK) c-Met/HGFR ROS Kinase
Research Areas:
Crizotinib (PF-02341066) is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. Crizotinib is also a ROS1 inhibitor. Crizotinib has effective tumor growth inhibition [1] .
89
89 Publications Verification
Cat. No.: HY-50878A
CAS No.: 1415560-69-8
Synonyms: PF-02341066 hydrochloride
Research Areas:
Crizotinib hydrochloride (PF-02341066 hydrochloride) is an orally bioavailable, selective, and ATP-competitive dual ALK and c-Met inhibitor with IC50s of 20 and 8 nM, respectively. Crizotinib hydrochloride (PF-02341066 hydrochloride) inhibits tyrosine phosphorylation of NPM-ALK and tyrosine phosphorylation of c-Met with IC50s of 24 and 11 nM in cell-based assays, respectively. It is also a ROS proto-oncogene 1 (ROS1) inhibitor. Crizotinib hydrochloride (PF-02341066 hydrochloride) has effective tumor growth inhibition [1] .
38
Research Areas:
Lorlatinib (PF-06463922) is a selective, orally active, brain-penetrant and ATP-competitive ROS1/ALK inhibitor with anticancer activity. Lorlatinib has Kis of <0.025 nM, <0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALK L1196M, respectively. Lorlatinib targets to EML4-ALK, and inhibits ALK phosphorylation with IC50s of 15-43 nM (ALK L1196), 14-80 nM (ALK G1269A), 38-50 nM (ALK 1151Tins), 77-113 nM (ALK G1202R), respectively [1] .
31
31 Cited Publications
Synonyms: NMS-E628; RXDX-101
Research Areas:
Entrectinib (NMS-E628) is an orally active, BBB-penetrated and centrally active inhibitor of TrkA/B/C, ROS1 and ALK, with IC50 values of 1, 3, 5, 12 and 7 nM, respectively. Entrectinib induces apoptosis and cycle arrest in cancer cells, has antitumor activity, and attenuates bleomycin-induced lung fibrosis in mice [1] .
17
17 Cited Publications
Cat. No.: HY-W015913
CAS No.: 113-24-6
Synonyms: Sodium 2-oxopropanoate; Acetylformic acid sodium
8
Research Areas:
Repotrectinib (TPX-0005) is a potent ROS1 (IC50=0.07 nM) and TRK (IC50=0.83/0.05/0.1 nM for TRKA/B/C) inhibitor. Repotrectinib potently inhibits WT ALK (IC50=1.01 nM). Repotrectinib has anti-cancer activity [1] .
8
8 Cited Publications
Synonyms: Apigenin-7-O-β-D-glucopyranoside; Cosmosiin; Apigetrin
Category:
Flavonoids Flavones Dendranthema morifolium (Ramat.) Tzvel. Phenols Polyphenols Plants Compositae Disease Research Fields Cancer
Target:
6
Research Areas:
Merestinib (LY2801653) is a potent, orally bioavailable c-Met inhibitor (Ki=2 nM) with anti-tumor activities. Merestinib (LY2801653) also has potent activity against MST1R (IC50=11 nM), FLT3 (IC50=7 nM), AXL (IC50=2 nM), MERTK (IC50=10 nM), TEK (IC50=63 nM), ROS1, DDR1/2 (IC50=0.1/7 nM) and MKNK1/2 (IC50=7 nM) [1] .
6
6 Cited Publications
Synonyms: LY2801653 dihydrochloride
Research Areas:
Merestinib dihydrochloride (LY2801653 dihydrochloride) is a potent, orally bioavailable c-Met inhibitor (Ki=2 nM) with anti-tumor activities. Merestinib dihydrochloride also has potent activity against MST1R (IC50=11 nM), FLT3 (IC50=7 nM), AXL (IC50=2 nM), MERTK (IC50=10 nM), TEK (IC50=63 nM), ROS1, DDR1/2 (IC50=0.1/7 nM) and MKNK1/2 (IC50=7 nM) [1] .
3
3 Cited Publications
Synonyms: DS-6051b; AB-106; IBI-344
Target:
Research Areas:
Taletrectinib (DS-6051b) is a potent, orally active, and next-generation selective ROS1/NTRK inhibitor. Taletrectinib potently inhibits recombinant ROS1, NTRK1, NTRK2, and NTRK3 with IC50s of 0.207, 0.622, 2.28, and 0.98 nM, respectively. Taletrectinib also inhibits ROS1 G2032R and other Crizotinib-resistant ROS1 mutants [1] .
2
2 Cited Publications
Cat. No.: HY-W015913S
CAS No.: 142014-11-7
Synonyms: Sodium 2-oxopropanoate-13C3; Acetylformic acid-13C3 sodium
1
1 Cited Publications
Synonyms: Tetrahydroxy-1,4-benzoquinone; Tetrahydroxybenzoquinone
Research Areas:
Tetrahydroxyquinone (Tetrahydroxy-1,4-benzoquinone), a primitive anticataract agent, is a redox active benzoquinone. Tetrahydroxyquinone can take part in a redox cycle with semiquinone radicals, leading to the formation of reactive oxygen species (ROS) .
1
1 Cited Publications
Cat. No.: HY-B1106A
CAS No.: 1215458-51-7
Synonyms: Tetrahydroxy-1,4-benzoquinone monohydrate; Tetrahydroxybenzoquinone monohydrate
Research Areas:
Tetrahydroxyquinone monohydrate (Tetrahydroxy-1,4-benzoquinone monohydrate), a primitive anticataract agent, is a redox active benzoquinone. Tetrahydroxyquinone monohydrate can take part in a redox cycle with semiquinone radicals, leading to the formation of reactive oxygen species (ROS) .
Synonyms: NVL-520; NUV-520
Target:
Research Areas:
Zidesamtinib (NVL-520) is a potent, selective, orally active and brain-penetrant inhibitor of diverse ROS1 fusions and resistance mutations, with IC50s of 0.7 and 7.9 nM for wild-type ROS1 and ROS1 G2032R, respectively, and spares TRK inhibition. Zidesamtinib can be used for the research of cancer [1].
Synonyms: WX-0593
Research Areas:
Iruplinalkib (WX-0593) is an orally active and selective ALK/ROS1 inhibitor. Iruplinalkib can effectively inhibit tyrosine autophosphorylation of ALK and mutant ALK, EGFR, with the IC50 between 5.38 and 16.74 nM. Iruplinalkib is also a suppressive agent of the transporter MATE1, MATE2K, P-gp and BCRP. Iruplinalkib can be used in the study of non-small cell lung cancer [1] .
Cat. No.: HY-12215R
CAS No.: 1454846-35-5
Synonyms: PF-06463922 (Standard)
Research Areas:
Lorlatinib (Standard) is the analytical standard of Lorlatinib. This product is intended for research and analytical applications. Lorlatinib (PF-06463922) is a selective, orally active, brain-penetrant and ATP-competitive ROS1/ALK inhibitor with anticancer activity. Lorlatinib has Kis of <0.025 nM, <0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALK L1196M, respectively. Lorlatinib targets to EML4-ALK, and inhibits ALK phosphorylation with IC50s of 15-43 nM (ALK L1196), 14-80 nM (ALK G1269A), 38-50 nM (ALK 1151Tins), 77-113 nM (ALK G1202R), respectively [1] .
Research Areas:
APG-2449 is an orally active inhibitor for BCL-2 and multikinase (ALK/FAK/ROS1) with potent antitumor activities. APG-2449 reduces cell viability and enhances apoptosis in acute myeloid leukemia cells in vitro. APG-2449 decreases activation of FAK and its downstream effectors. APG-2449 can be studied in research for mesothelioma tumor, non-small cell lung cancer, ovarian cancer, hematologic and solid malignancies [1] .
Cat. No.: HY-N2693
CAS No.: 66777-70-6
Cat. No.: HY-159147
CAS No.: 2570251-69-1
Target:
Research Areas:
SIAIS039 is an orally active c-ros oncogene 1 (ROS1)-specific PROTAC with DC50s of 154.46 nM, 126.47 nM, 143.69 nM for HCC78 cells, Ba/F3 expressing the CD74-ROS1 fusion and Ba/F3 expressing the SDC4-ROS1 fusion, respectively. SIAIS039 suppresses cell proliferation, induces cell cycle arrest and apoptosis, and inhibits clonogenicity against ROS1-positive cells. SIAIS039 demonstrates anti-tumour effects against ROS1-driven tumor growth vivo. SIAIS039 is composed of the ALK inhibitor Brigatinib (HY-12857), a linker EM-12 (HY-138793), and a VHL ligand E3 ubiquitin ligase 1-Butyne (Red: Brigatinib; Blue: VHL ligand; Black: linker) [1].
Synonyms: SMTP-7
Target:
Research Areas:
Orniplabin (SMTP-7) is a low-molecular-weight compound that enhances plasminogen–fibrin binding, urokinase-catalyzed activation of plasminogen, and urokinase and plasminogen-mediated fibrin degradation. Orniplabin shows potential thrombolytic and anti-inflammatory effects. Orniplabin inhibits ROS .
-
-
Protocols
Targeted therapy! The Capetin Prize winning "Click Chemistry" can be used like this!Targeted therapy! The Nobel Prize winning "Click Chemistry" can be used like this!A suitable model is crucial in drug screening experiments. Organs can mimic the three-dimensional functional structure of internal organs, have similar spatial organization to corresponding organs, maintain some key characteristics, and reproduce some physiological functions. They are widely used for modeling and personalized drug screening physiological functions.2025-02-06
