ROS Kinase

Related Products

The transmembrane proto-oncogene receptor tyrosine kinase (RTK) ROS is one of the last two remaining orphan receptor tyrosine kinases. Its normal expression pattern is tightly spatiotemporally restricted during development. The ectopic expression, as well as the production of variable mutant forms of ROS kinase, has been reported in a number of cancers, such as glioblastoma multiforme, and non-small cell lung cancer, suggesting a role for ROS kinase in deriving such tumors. It is thought also that the c-ROS gene may have a role in some cardiovascular diseases, and the fact that homozygous male mice targeted against the c-ROS gene are healthy but infertile has inspired researchers to think about ROS inhibition as a method for the development of new male contraceptives.

ROS1 is a transmembrane receptor tyrosine kinase proto-oncogene that has been shown to have rearrangements with several genes in glioblastoma, non-small-cell lung cancer (NSCLC), and other neoplasms, including intrachromosomal fusion with GOPC due to microdeletions at 6q22.1. ROS1 fusion events are important findings in these tumors, as they are potentially targetable alterations with newer tyrosine kinase inhibitors.

ROS Kinase Related Products (77)
Antibodies (3)

By Effects:	Inhibitors (55) Degrader (1) Activators (5) Inducers (8)

Cat. No.	Product Name	Effect	Purity	Chemical Structure

HY-149394

PRDX1-IN-1		98.04%
PRDX1-IN-1 is a selective inhibtor of PRDX1 with an IC₅₀ value of 0.164 μM. PRDX1-IN-1 can be used in researches related to cancer.PRDX1-IN-1 promots intracellular ROS accumulation, and inhibits the proliferation, invasion and migration of cancer cells besides inducing apoptosis. PRDX1-IN-1 could be used in cancer research.

HY-B0873

Uniconazole	Inhibitor	99.68%
Uniconazole, a plant growth retardant, is a potent inhibitor of abscisic acid (ABA) catabolism with an IC₅₀ of 68 nM against ABA 8’-hydroxylase. Uniconazole is a potent competitive inhibitor of CYP707A3 activity with a K_i of 8 nM. Uniconazole evidently inhibits gibberellin biosynthesis, and brassinosteroid biosynthesis is also inhibited to some extent.

HY-155163

APG-2449	Inhibitor	98.93%
APG-2449 is an orally active ALK/ROS1/FAK inhibitor. APG-2449 shows antitumor activity in mouse models of non-small cell lung cancer (NSCLC).

HY-13326

ASP3026		99.88%
ASP3026 is a selective and orally active inhibitor of anaplastic lymphoma kinase (ALK). ASP3026 is a selective and oral active anaplastic lymphoma kinase (ALK) inhibitor with a IC₅₀ value of 3.5 nM. ASP3026 can inhibit the phosphorylation of IGF-1R, STAT3, AKT and JNK proteins, and induce the cleavage of caspase 3 and PARP. It also inhibited ROS and ACK. ASP3026 can be used in anti-tumor research.

HY-12678S1

Entrectinib-d₈	Inhibitor	99.82%
Entrectinib-d8 (NMS-E628-d8; RXDX-101-d8) is a deuterated version of Entrectinib (HY-12678). Entrectinib (NMS-E628) is an orally available, blood-brain barrier permeable, central nervous system active TrkA/B/C, ROS1 and ALK inhibitor with IC₅₀ values of 1, 3, 5, 12 and 12, respectively. 7 nM. Entrectinib induces apoptosis and cycle arrest in cancer cells, has anti-tumor activity, and also alleviates bleomycin-induced pulmonary fibrosis in mice.

HY-50878S

Crizotinib-d₅	Inhibitor	≥99.0%
Crizotinib-d₅ is the deuterium labeled Crizotinib. 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.

HY-125711

Capsanthin	Inhibitor
Capsanthin is a carotenoid that has been found in C. annuum. Capsanthin has antioxidant、antitumor and anti-inflammatory effects.

HY-112801

F-1	Inhibitor	98.03%
F-1 is a potent ALK and ROS1 dual inhibitor, suppresses phospho-ALK and its relative downstream signaling pathways, with IC₅₀s of 2.1 nM, 2.3 nM, 1.3 nM and 3.9 nM for ALK^WT, ROS1^WT, ALK^L1196M and ALK^G1202R, respectively.

HY-W402148

10-Methyl-9-(phenoxycarbonyl)acridinium (fluorosulfonate)		99.79%
10-Methyl-9-(phenoxycarbonyl)acridinium fluorosulfonate, a phenyl ester of acridinium esters, is a fluorescent dye that produces chemiluminescent under neutral conditions. 10-Methyl-9-(phenoxycarbonyl)acridinium fluorosulfonate can be used for the measurement of hydrogen peroxide.

HY-17437

Mefloquine	Inducer
Mefloquine (Mefloquin), an orally active and potent quinoline antimalarial agent, is an anti-SARS-CoV-2 entry inhibitor. Mefloquine is also a K⁺ channel (KvQT1/minK) antagonist with an IC₅₀ of ~1 μM. Mefloquine can be used for malaria, systemic lupus erythematosus and cancer research.

HY-148228

ROS kinases-IN-1	Inhibitor	98.30%
ROS kinases-IN-1 (pag 98) is a ROS tyrosine kinase inhibitor with IC₅₀ value of 1.22 μM. ROS kinases-IN-1 shows anti-tumor activity.

HY-12678S

Entrectinib-d₄	Inhibitor
Entrectinib-d4 (NMS-E628-d4; RXDX-101-d4) is the deuterium labeled Entrectinib (HY-12678). Entrectinib 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.

HY-16230

GGTI-2417		98.97%
GGTI-2417 is a potent and selective inhibitor of GGTase I. GGTI-2417 inhibits the Cdk2-mediated phosphorylation of p27^Kip1 at Thr187 and accumulates p27^Kip1 in the nucleus. GGTI-2417 also induces breast cancer cell apoptosis.

HY-15514A

Merestinib dihydrochloride	Inhibitor	99.36%
Merestinib dihydrochloride (LY2801653 dihydrochloride) is a potent, orally bioavailable c-Met inhibitor (K_i=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).

HY-12215R

Lorlatinib (Standard)	Inhibitor
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-131003A

Taletrectinib free base	Inhibitor
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-50878B

Crizotinib acetate	Inhibitor
Crizotinib (PF-02341066) acetate is an orally bioavailable, ATP-competitive ALK and c-Met inhibitor with IC₅₀s of 20 and 8 nM, respectively. Crizotinib acetate 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 acetate is also a ROS1 inhibitor. Crizotinib acetate has effective tumor growth inhibition.

HY-19551

Apogossypolone	Inducer
Apogossypolone (ApoG2) is an orally active Bcl-2 family proteins inhibitor with K_i values of 35, 25 and 660 nM for Bcl-2, Mcl-1 and Bcl-X_L, respectively. Apogossypolone shows antitumor activities, induces cell apoptosis and autophagy. Apogossypolone also has antifungal activity.

HY-111416

WY-135	Inhibitor
WY-135 is an ALK (IC₅₀=1.4 nM) and ROS1 (IC₅₀=1.1 nM) dual inhibitor.

HY-147658

AChE/BChE/BACE-1-IN-1	Inhibitor
AChE/BChE/BACE-1-IN-1 (Compound 4k) is an orally active inhibitor of AChE, BChE, and BACE-1 with IC₅₀ values of 0.058, 0.082 and 0.115 μM against hAChE, hBChE and hBACE-1, respectively. AChE/BChE/BACE-1-IN-1 shows considerable PAS-AChE binding capability, excellent brain permeation, potential disassembly of Aβ aggregates, and neuroprotective activity against Aβ-induced stress. AChE/BChE/BACE-1-IN-1 has remarkable antioxidant potential.

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ROS Kinase

ROS Kinase

ROS Kinase Related Products (77)

Antibodies (3)

ROS Kinase Related Products (77):