alk tyrosine kinase receptor

Tyrosine kinase-IN-7 is a potent inhibitor of the tyrosine kinase EGFR, inhibiting EGFR(WT) and EGFR(T790M) and showing anti-cancer and anti-tumor activity in a variety of cancer cell lines. Tyrosine kinase-IN-7 has potential anti-inflammatory and antiviral activities.

EML4-ALK kinase inhibitor 1 (EML4 ALK kinase inhibitor 1) is a potent oral active inhibitor of echinoderm microtubule-associated protein-like 4-anaplastic lymphoma kinase (EML4-ALK), with an IC50 of 1 nM.

SAR348830 is an ALK inhibitor, targeting anaplastic lymphoma kinase.

Tyrosine kinase inhibitor is a tyrosine kinase inhibitor used in combination with fragmenting aromatic nitrogen compounds as antiproliferative agents.

EGFR Protein Tyrosine Kinase Substrate is a EGFR protein tyrosine kinase substrate.

Tyrosine kinase-IN-1 is a multi-targeted tyrosine kinase inhibitor（KDR, Flt-1, FGFR1 and PDGFRα with IC50s of 4nM, 20nM, 4nM, 2 nM ,respectively）

PDGFR Tyrosine Kinase Inhibitor III (PDGF Receptor Tyrosine Kinase Inhibitor III) (PDGF Receptor Tyrosine Kinase Inhibitor III) is a multikinase inhibitor that inhibits PDGFR, EGFR, FGFR, PKA, and PKC, respectively. PDGFR Tyrosine Kinase Inhibitor III can be used for the research of amyotrophic lateral sclerosis [1].

Tyrosine Protein Kinase JAK 2 (Phospho-Tyr8, 9) is a peptide derived from mouse JAK2, specifically composed of amino acids 475 to 491.

Tyrosine kinase-IN-6 is a potent inhibitor of RON splice variants, demonstrating significant anticancer and antineoplastic effects [1].

Casein Kinase II Receptor Peptide, a substrate for casein kinase II, exhibits a Km value of 500 µM. It is utilized to measure the activity of casein kinase II in crude enzyme preparations [1].

Tyrosine Kinase Peptide 1 is a control substrate peptide for c-Src assay.

Tyrosine kinase-IN-4 (EXAMPLE 107) is a protein tyrosine kinase inhibitor [1].

Ceritinib (LDK378) is a specific ALK inhibitor (IC50: 0.2 nM).

Repotrectinib (TPX-0005) is a potent ALK/ROS1/TRK inhibitor, with IC50 of 1.01 nM, 5.3 nM, 1.08 nM and 1.26 nM for WT ALK, SRC, ALK L1196M and ALK G1202R, respectively.

Alectinib (RG-7853) is an orally available inhibitor of the receptor tyrosine kinase anaplastic lymphoma kinase (ALK) with antineoplastic activity.

Belizatinib (TSR-011) is an effective, oral and dual inhibitor of ALK (IC50: 0.7 nM, wild-type recombinant ALK) and TRKA, TRKB, and TRKC.

Brigatinib (AP-26113) is a highly potent and selective ALK inhibitor.

Lorlatinib (PF-6463922) is an orally available, ATP-competitive inhibitor of the receptor tyrosine kinases, anaplastic lymphoma kinase (ALK) and C-ros oncogene 1 (Ros1), with potential antineoplastic activity.

Entrectinib (RXDX-101) is an inhibitor of TrkA (IC50: 1.7 nM), TrkB (IC50: 0.1 nM), and TrkC (IC50: 0.1 nM), as well as anaplastic lymphoma kinase (ALK; IC50: 1.6 nM) and C-ros oncogene 1 (ROS1; IC50: 0.2 nM). Entrectinib blocks proliferation of ALK-dependent cell lines, including those with C1156Y or L1196M resistance mutations, and inhibits ALK‐dependent signaling. It has been shown to inhibit the growth of a non-small cell lung Y cell line bearing an EML4-ALK rearrangement. In mice bearing various ROS1, Trk, or ALK-driven xenografts, Entrectinib has been shown to induce tumor regression.

Crizotinib (PF-02341066) is an ATP-competitive small-molecule tyrosine kinases inhibitor of c-MET (IC50: 8 nM) and ALK (IC50: 20 nM) receptor.

F-1 is IC50s of 2.1 nM, 2.3 nM, 1.3 nM and 3.9 nM for ALKWT, ROS1WT, ALKL1196M and ALKG1202R, respectively. F-1 is a potent ALK and ROS1 dual inhibitor, suppresses phospho-ALK and its relative downstream signaling pathways.

KRCA-0008 is an effective and specific ALK/Ack1 inhibitor (IC50: 12/4 nM); displays drug-like properties without hERG liability.

CEP-37440 is an effective and specific Dual FAK/ALK inhibitor with IC50s of 120 nM(ALK cellular in 75% human plasma) and 2.3 nM (FAK).

Ensartinib hydrochloride (X-396 dihydrochloride) is a potent new-generation ALK inhibitor with high activity against CNS metastases and a broad range of known crizotinib-resistant ALK mutations. It potently inhibits both wild-type ALK and ALK variants (C1156Y, F1174, G1202R, L1196M, S1206R, and T1151 mutants) with in vitro IC50s of <4 nM.

ALK inhibitor 1 is a selective ALK kinase inhibitor.

ASP3026 has been used in trials studying the treatment of Solid Tumor, B-Cell Lymphoma, Advanced Malignancies, Positive for Anaplastic Lymphoma Kinase, and Positive for Proto-Oncogene Tyrosine-Protein Kinase ROS.

MS4078 is an inhibitor and aplastic lymphoma kinase (ALK) PROTAC (degrader) based on Cereblon ligand, with a Kd of 19 nM for binding affinity to ALK.

JH-VIII-157-02 is an inhibitor of ALK and inhibits echinoderm microtubule-associated protein-like 4-ALK (EML4-ALK) with IC50s of 2 nM for EML4-ALK G1202R, EML4-ALKwt, EML4-ALK C1156Y, EML4-ALK F1174L, and EML4-ALK F1174L.

HG-14-10-04 is a potent and specific ALK inhibitor.

R-268712 is a specific activin receptor-like kinase 5 (ALK5) inhibitor(IC50 of 2.5 nM). It is also an orally active transforming growth factor-β type I receptor inhibitor.

Ceritinib dihydrochloride (LDK378 dihydrochloride) is a selective, orally bioavailable and ATP-competitive inhibitor of ALK tyrosine kinase(IC50 of 200 pM), and also inhibits IGF-1R, InsR, and STK22D (IC50 values of 8, 7, and 23 nM, respectively), shows great antitumor potency

GSK1838705A is an effective IGF-1R inhibitor (IC50: 2.0 nM), modestly potent to IR (IC50: 1.6 nM) and ALK (IC50: 0.5 nM), respectively, and little inhibition to other protein kinases.

Alectinib-d8 is a deuterated compound of Alectinib. Alectinib has a CAS number of 1256580-46-7. CH5424802 is an orally available inhibitor of the receptor tyrosine kinase anaplastic lymphoma kinase (ALK) with antineoplastic activity.

X-376 (Ensartinib) is an orally available small molecule inhibitor of the receptor tyrosine kinase anaplastic lymphoma kinase (ALK) with potential antineoplastic activity. Upon oral administration, X-396 binds to and inhibits ALK kinase, ALK fusion proteins, and ALK point mutation variants. Inhibition of ALK leads to the disruption of ALK-mediated signaling and eventually inhibits tumor cell growth in ALK-expressing tumor cells. ALK belongs to the insulin receptor superfamily and plays an important role in nervous system development.

ALK-IN-1 (AP26113) is a potent ALK inhibitor with IC50 of 0.62 nM in a cell-free assay, demonstrated ability overcome Crizotinib resistance mediated by a L1196M mutation. Phase 2.

6-Demethoxytangeretin is a citrus flavonoid isolated from Citrus depressa.

Crizotinib hydrochloride (PF-02341066 hydrochloride) is a novel inhibitor of anaplastic lymphoma kinase and c-Met(IC50s of 20 and 8 nM)

CEP-28122 is a highly potent and selective orally active ALK inhibitor.

Alectinib hydrochloride (RO5424802 Hydrochloride) is a selective, and orally available inhibitor of ALK( IC50 : 1.9 nM)

Ficonalkib is a potent antineoplastic agent that inhibits the Anaplastic Lymphoma Kinase (ALK) tyrosine kinase receptor.

ZX-29 is a potent and selective inhibitor of ALK(IC50 of 2.1 nM, 1.3 nM and 3.9 nM for ALK, ALK L1196M and ALK G1202R mutations, respectively), and also induces protective autophagy and has antitumor effect.

PF-06439015 overcomes clinical ALK (receptor tyrosine kinase anatropic lymphoma kinase) mutations resistant to krizotinib. Pf-06439015 is an effective selective inhibitor.

ALK inhibitor 2 is a new-type and selective inhibitor for the ALK kinase.

AZD-3463 (ALK/IGF1R inhibitor) , an orally bioavailable ALK inhibitor (Ki: 0.75 nM), can inhibit IGF1R with equivalent potency.

NVP-TAE 684 (TAE684) is a excellently effective and specific ALK inhibitor(IC50=3 nM).