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Results for "

ROS1-IN-1

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Anaplastic lymphoma kinase (ALK) (6) Apoptosis (4) PROTACs (1) ROS Kinase (10)
By Research Areas:	Cancer (10)
Click Chemistry:	Azide (1)

Inhibitors & Agonists

Screening Libraries

Click Chemistry

Targets Recommended: Dan family AIM2 NEKs

Cat. No.	Product Name	Target	Research Areas	Chemical Structure

HY-131003

Taletrectinib 1 Publications Verification DS-6051b; AB-106; IBI-344	ROS Kinase	Cancer
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 .

HY-12215

Lorlatinib Maximum Cited Publications 31 Publications Verification PF-06463922	Anaplastic lymphoma kinase (ALK) ROS Kinase Apoptosis	Cancer
Lorlatinib (PF-06463922) is a selective, orally active, brain-penetrant and ATP-competitive *ROS1/ALK* inhibitor with anticancer activity. Lorlatinib has K_is 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 .

HY-12215R

Lorlatinib (Standard)	Anaplastic lymphoma kinase (ALK) ROS Kinase Apoptosis	Cancer
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 K_is 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 .

HY-150974

*ROS1-IN-1*	ROS Kinase	Cancer
ROS1-IN-1 (Compound 31) is a potent and selective *ROS1* kinase inhibitor with an IC₅₀ of 0.097 μM .

HY-130794

ALK/ROS1-IN-1	Anaplastic lymphoma kinase (ALK) ROS Kinase	Cancer
ALK/ROS1-IN-1 (compound 2e) is a potent and selective anti crizotinib-resistant *ALK/ROS1* dual inhibitor, with IC₅₀s of 0.174 μM and 0.530 μM for ALK and ROS1 enzyme, respectively.

HY-131003A

Taletrectinib free base DS-6051b free base; AB-106 free base; IBI-344 free base	ROS Kinase	Cancer
Taletrectinib (DS-6051b) free base is a potent, orally active, and next-generation selective *ROS1/NTRK* inhibitor. Taletrectinib free base potently inhibits recombinant ROS1, NTRK1, NTRK2, and NTRK3 with IC₅₀s of 0.207, 0.622, 2.28, and 0.98 nM, respectively. Taletrectinib free base also inhibits ROS1 G2032R and other Crizotinib-resistant ROS1 mutants .

HY-160172

ALK/ROS1-IN-4	Anaplastic lymphoma kinase (ALK) ROS Kinase	Cancer
ALK/ROS1-IN-4 (example 13) is a dual inhibitor of ALK and *ROS1 kinase* .

HY-160172A

ALK/ROS1-IN-4 hydrate	Anaplastic lymphoma kinase (ALK) ROS Kinase	Cancer
ALK/ROS1-IN-4 (hydrate) (example 13) is a dual inhibitor of ALK and *ROS1 kinase* .

HY-159147

SIAIS039	PROTACs ROS Kinase Apoptosis	Cancer
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) .

HY-135509

Lorlatinib acetate PF-06463922 acetate	Anaplastic lymphoma kinase (ALK) ROS Kinase Apoptosis	Cancer
Lorlatinib (PF-06463922) acetate is a selective, orally active, brain-penetrant and ATP-competitive *ROS1/ALK* inhibitor with anticancer activity. Lorlatinib acetate has K_is of <0.025 nM, <0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALK ^L1196M, respectively. Lorlatinib acetate 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 .

Cat. No.	Product Name

HY-L075

Anti-Lung Cancer Compound Library	2,167 compounds
Lung cancer is a major global health problem, as it is the leading cause of cancer-related deaths worldwide. Lung cancer is divided into two categories: small cell lung cancer and non-small cell lung cancer (NSCLC). Non-small cell lung cancer accounts for about 85 percent of lung cancers. As with all cancers, lung cancer may be treated with surgery, chemotherapy, radiation therapy, targeted therapy, immunotherapy or a combination thereof. Targeted therapy is one of the most exciting developments in lung cancer medicine, especially for NSCLC. Extensive genomic characterization of NSCLC has led to the identification of molecular subtypes of NSCLC that are oncogene addicted and exquisitely sensitive to targeted therapies. These include activating mutations in epidermal growth factor receptor (EGFR) and BRAF or echinoderm microtubule-associated protein-like 4 (EML4)-anaplastic lymphoma kinase (ALK) fusions and ROS1 receptor tyrosine kinase fusions. These are important targets for target therapy. MCE offers a unique collection of 2,167 compounds with identified and potential anti-lung cancer activity. These compounds target lung cancer’s major targets and signaling pathways. MCE anti-lung cancer compound library is a useful tool for anti-lung cancer drugs screening and other related research.

Anti-Lung Cancer Compound Library

2,167 compounds

Lung cancer is a major global health problem, as it is the leading cause of cancer-related deaths worldwide. Lung cancer is divided into two categories: small cell lung cancer and non-small cell lung cancer (NSCLC). Non-small cell lung cancer accounts for about 85 percent of lung cancers.

As with all cancers, lung cancer may be treated with surgery, chemotherapy, radiation therapy, targeted therapy, immunotherapy or a combination thereof. Targeted therapy is one of the most exciting developments in lung cancer medicine, especially for NSCLC. Extensive genomic characterization of NSCLC has led to the identification of molecular subtypes of NSCLC that are oncogene addicted and exquisitely sensitive to targeted therapies. These include activating mutations in epidermal growth factor receptor (EGFR) and BRAF or echinoderm microtubule-associated protein-like 4 (EML4)-anaplastic lymphoma kinase (ALK) fusions and ROS1 receptor tyrosine kinase fusions. These are important targets for target therapy.

MCE offers a unique collection of 2,167 compounds with identified and potential anti-lung cancer activity. These compounds target lung cancer’s major targets and signaling pathways. MCE anti-lung cancer compound library is a useful tool for anti-lung cancer drugs screening and other related research.

Cat. No.	Product Name		Classification

HY-159147

SIAIS039		Azide
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) .

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