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Results for "

ROS1 inhibitor

" in MedChemExpress (MCE) Product Catalog:

By Targets:	Anaplastic lymphoma kinase (ALK) (18) Apoptosis (6) Autophagy (7) Bacterial (1) c-Met/HGFR (7) Cholinesterase (ChE) (1) Discoidin Domain Receptor (2) EGFR (3) FAK (2) FLT3 (2) Fungal (1) Isotope-Labeled Compounds (3) NAMPT (1) p38 MAPK (1) Reactive Oxygen Species (8) ROS Kinase (25) Trk Receptor (5) Xanthine Oxidase (1)
By Research Areas:	Cancer (31) Infection (2) Inflammation/Immunology (4) Neurological Disease (2)

Inhibitors & Agonists

Natural
Products

Isotope-Labeled Compounds

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-157391

ALK/ROS1-IN-3	ROS Kinase Anaplastic lymphoma kinase (ALK)	Cancer
ALK/ROS1-IN-3 (compound C01) is a *ROS1* and ALK dual inhibitor with IC₅₀s of 42.3 nM and 49.1 nM for ROS1 ^G2032R and 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-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 .

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 .

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 .

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-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-152292

Zidesamtinib NVL-520	ROS Kinase	Cancer
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 .

HY-145574

Iruplinalkib WX-0593	Anaplastic lymphoma kinase (ALK) ROS Kinase	Cancer
Iruplinalkib (WX-0593) is a potent, selective, and orally active inhibitor of ALK and *ROS1* tyrosine kinase. Iruplinalkib (WX-0593) shows favorable safety and promising antitumor activity in advanced NSCLC with ALK or ROS1 rearrangement .

HY-112801

F-1	Anaplastic lymphoma kinase (ALK) ROS Kinase	Cancer
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-111416

WY-135

Anaplastic lymphoma kinase (ALK) ROS Kinase Cancer

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

WY-135	Anaplastic lymphoma kinase (ALK) ROS Kinase	Cancer
WY-135 is an ALK (IC₅₀=1.4 nM) and *ROS1* (IC₅₀=1.1 nM) dual inhibitor.

HY-153743

Protein kinase inhibitor 4	ROS Kinase Trk Receptor	Cancer
Protein kinase inhibitor 4 (Compound 3) is a protein kinase inhibitor that inhibits TRK-A and *ROS1* (IC₅₀=3.0 nM and 104 nM respectively) .

HY-12215

Lorlatinib 20+ Cited Publications 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-155163

APG-2449	Anaplastic lymphoma kinase (ALK) ROS Kinase FAK	Others
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-147413

Unecritinib TQ-B3101	EGFR	Cancer
Unecritinib (TQ-B3101) is a potent EGFR tyrosine kinase inhibitor. Unecritinib shows anticancer activity. Unecritinib inhibits ALK, ROS1, and MET. Unecritinib has the potential for the research of solid tumor and relapsed or refractory ALK-positive anaplastic large cell lymphoma .

HY-103022

Repotrectinib 2 Publications Verification TPX-0005	ROS Kinase Trk Receptor Anaplastic lymphoma kinase (ALK)	Cancer
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 .

HY-12678

Entrectinib 15+ Cited Publications NMS-E628; RXDX-101	ROS Kinase Trk Receptor Anaplastic lymphoma kinase (ALK) Autophagy	Cancer
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 .

HY-50878

Crizotinib Maximum Cited Publications 61 Publications Verification PF-02341066	Anaplastic lymphoma kinase (ALK) c-Met/HGFR ROS Kinase Autophagy	Cancer
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-50878B

Crizotinib acetate PF-02341066 acetate	Anaplastic lymphoma kinase (ALK) ROS Kinase c-Met/HGFR	Cancer
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-B0847S

Propiconazole-d7	Fungal Reactive Oxygen Species	Infection
Propiconazole-d₇ is the deuterium labeled Propiconazole. Propiconazole is a broad-spectrum triazole fungicide that inhibits the conversion of lanosterol to ergosterol, leading to fungal cell membrane disruption. Propiconazole inhibits S. cerevisiae, but not rat liver, microsomal cytochrome P450 (IC50s=0.04 and >200 µM, respectively). Propiconazole inhibits the growth of T. deformans and R. stolonifer (ED50s=0.073 and 4.6 µg/mL, respectively). Propiconazole increases production of reactive oxygen species (ROS)[1].

HY-50878S

Crizotinib-d5 PF-02341066-d₅	Anaplastic lymphoma kinase (ALK) c-Met/HGFR ROS Kinase Autophagy	Cancer
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-50878A

Crizotinib hydrochloride Maximum Cited Publications 61 Publications Verification PF-02341066 hydrochloride	Anaplastic lymphoma kinase (ALK) c-Met/HGFR ROS Kinase Autophagy	Cancer
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 .

HY-12678S

Entrectinib-d4 NMS-E628-d₄; RXDX-101-d₄	ROS Kinase Trk Receptor Anaplastic lymphoma kinase (ALK) Autophagy Isotope-Labeled Compounds	Cancer
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-50878AS

Crizotinib-d9 hydrochloride PF-02341066-d₉ hydrochloride	c-Met/HGFR Autophagy Anaplastic lymphoma kinase (ALK) ROS Kinase Isotope-Labeled Compounds	Cancer
Crizotinib-d₉ hydrochloride is deuterated labeled Crizotinib hydrochloride (HY-50878A). 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 .

HY-15514A

Merestinib dihydrochloride 4 Publications Verification LY2801653 dihydrochloride	c-Met/HGFR FLT3 ROS Kinase Discoidin Domain Receptor	Cancer
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-15514

Merestinib 4 Publications Verification LY2801653	c-Met/HGFR FLT3 ROS Kinase Discoidin Domain Receptor	Cancer
Merestinib (LY2801653) is a potent, orally bioavailable c-Met inhibitor (K_i=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) .

HY-12678S1

Entrectinib-d8 NMS-E628-d₈; RXDX-101-d₈	Isotope-Labeled Compounds Autophagy Anaplastic lymphoma kinase (ALK) Trk Receptor ROS Kinase	Cancer
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-155178

Antiproliferative agent-34	EGFR	Cancer
Antiproliferative agent-34 (Compound A14) is a multi-target kinase inhibitor, with an IC₅₀ of 177 nM and 1567 nM for EGFR L858R/T790M and EGFR WT. Antiproliferative agent-34 also inhibits JAK2, ROS1, FLT3, FLT4, PDGFRα with IC₅₀ of 30.93, 106.90, 108.00, 226.60, 42.53 nM. Antiproliferative agent-34 inhibits H1975 and HCC827 cells proliferation with IC₅₀ values below 40 nM under normoxic condition, and the anti-proliferation potency achieves 4–6-fold improvement (IC₅₀ values < 10 nM) under hypoxic condition .

HY-156360

Xanthine oxidase-IN-12	Xanthine Oxidase Reactive Oxygen Species	Inflammation/Immunology
Xanthine oxidase-IN-12 (Compound 11) is a xanthine oxidase (XO) inhibitor with an IC₅₀ of 91 nM. Xanthine oxidase-IN-12 also has antioxidant activity and reduces intracellular ROS .

HY-144697

p38 MAPK-IN-3	p38 MAPK Apoptosis Reactive Oxygen Species	Cancer
p38 MAPK-IN-3 (Compound 2c) is a p38α MAPK inhibitor. p38 MAPK-IN-3 has antitumor activities and induces apoptosis and *ROS* .

HY-147795

Nampt-IN-8	NAMPT Apoptosis Reactive Oxygen Species	Cancer
Nampt-IN-8 (Compound 10d) is an NAMPT inhibitor with an IC₅₀ of 0.183 μM. Nampt-IN-8 is also a relatively good NQO1 substrate. Nampt-IN-8 induces cell apoptosis and *ROS* .

HY-N11887

Linocinnamarin	Reactive Oxygen Species	Inflammation/Immunology
Linocinnamarin is a nature product that could be isolated from Fragaria ananassa Duch. Linocinnamarin has anti-inflammatory activity. Linocinnamarin inhibits antigen-stimulated elevation of intracellular free Ca ²⁺ concentration and reactive oxygen species (ROS) .

HY-122311

Orniplabin SMTP-7	Reactive Oxygen Species	Neurological Disease Inflammation/Immunology
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* .

HY-N1306

Sideroxylin	Bacterial Reactive Oxygen Species Apoptosis	Infection Cancer
Sideroxylin is a C-methylated flavone isolated from Callistemon lanceolatus and exerts antimicrobial activity against *Staphylococcus aureus. Sideroxylin inhibits* ovarian cancer cell proliferation and induces apoptosis, causing DNA fragmentation, depolarization of the mitochondrial membrane, the generation of reactive oxygen species (ROS) .

HY-161358

FAK-IN-20	FAK Apoptosis	Cancer
FAK-IN-20 (Compound 7b) is an inhibitor of FAK with an IC₅₀ value of 0.27 nM. FAK-IN-20 exhibits anticancer activity. It can arrest the cell cycle in the G2/M phase and induce cell apoptosis (apoptosis) by generating ROS .

HY-158016

Antiproliferative agent-49	EGFR Apoptosis	Cancer
Antiproliferative agent-49 (Compound 5a) is a EGFR-TK inhibitor with an IC₅₀ of 0.09 μM. Antiproliferative agent-49 is a anti-proliferative agent. Antiproliferative agent-49 displays good activities against HER3 and HER4 with IC₅₀ values 0.18 and 0.37 µM. Antiproliferative agent-49 induces mitochondrial apoptotic pathway and increased accumulation of ROS .

HY-157437

AChE/BChE-IN-16	Cholinesterase (ChE) Reactive Oxygen Species	Neurological Disease Inflammation/Immunology
AChE/BChE-IN-16 (compound C7) is a potent cholinesterase (ChE) inhibitor with IC₅₀s of 30 nM and 48 nM for human acetylcholinesterase (hAChE) and human butyrylcholinesterase (hBChE), respectively. AChE/BChE-IN-16 exhibits a remarkable capacity to safeguard PC12 cells against H₂O₂-induced apoptosis and effectively suppresses the production of reactive oxygen species (ROS) .

Cat. No.	Product Name	Category	Target	Chemical Structure

HY-N11887

Linocinnamarin	Structural Classification Natural Products Source classification Rosaceae Plants Fragaria × ananassa Duch.	Reactive Oxygen Species
Linocinnamarin is a nature product that could be isolated from Fragaria ananassa Duch. Linocinnamarin has anti-inflammatory activity. Linocinnamarin inhibits antigen-stimulated elevation of intracellular free Ca ²⁺ concentration and reactive oxygen species (ROS) .

HY-N1306

Sideroxylin	Infection Eucalyptus saligna Flavonoids Classification of Application Fields Flavones Source classification Phenols Polyphenols Myrtaceae Plants Disease Research Fields	Bacterial Reactive Oxygen Species Apoptosis
Sideroxylin is a C-methylated flavone isolated from Callistemon lanceolatus and exerts antimicrobial activity against *Staphylococcus aureus. Sideroxylin inhibits* ovarian cancer cell proliferation and induces apoptosis, causing DNA fragmentation, depolarization of the mitochondrial membrane, the generation of reactive oxygen species (ROS) .

Cat. No.	Product Name	Chemical Structure

HY-50878S

Crizotinib-d5
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 .

Crizotinib-d5

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-B0847S

Propiconazole-d7
Propiconazole-d₇ is the deuterium labeled Propiconazole. Propiconazole is a broad-spectrum triazole fungicide that inhibits the conversion of lanosterol to ergosterol, leading to fungal cell membrane disruption. Propiconazole inhibits S. cerevisiae, but not rat liver, microsomal cytochrome P450 (IC50s=0.04 and >200 µM, respectively). Propiconazole inhibits the growth of T. deformans and R. stolonifer (ED50s=0.073 and 4.6 µg/mL, respectively). Propiconazole increases production of reactive oxygen species (ROS)[1].

Propiconazole-d7

Propiconazole-d₇ is the deuterium labeled Propiconazole. Propiconazole is a broad-spectrum triazole fungicide that inhibits the conversion of lanosterol to ergosterol, leading to fungal cell membrane disruption. Propiconazole inhibits S. cerevisiae, but not rat liver, microsomal cytochrome P450 (IC50s=0.04 and >200 µM, respectively). Propiconazole inhibits the growth of T. deformans and R. stolonifer (ED50s=0.073 and 4.6 µg/mL, respectively). Propiconazole increases production of reactive oxygen species (ROS)[1].

HY-12678S

Entrectinib-d4
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 .

Entrectinib-d4

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-50878AS

Crizotinib-d9 hydrochloride
Crizotinib-d₉ hydrochloride is deuterated labeled Crizotinib hydrochloride (HY-50878A). 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 .

Crizotinib-d9 hydrochloride

Crizotinib-d₉ hydrochloride is deuterated labeled Crizotinib hydrochloride (HY-50878A). 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 .

HY-12678S1

Entrectinib-d8
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 .

Entrectinib-d8

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 .

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