Cat.No. | Name | Information |
---|---|---|
M2075 | LDK378 | Ceritinib (LDK378) is a highly selective, orally bioavailable ALK inhibitor with IC50 of 0.15 nM. |
M1950 | ASP3026 | 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. |
M1873 | LDN-193189 | LDN-193189 is a highly potent small molecule inhibitor of bone morphogenetic protein (BMP) type I receptors ALK2 and ALK3. |
M1794 | SB431542 | SB-431542 is a potent and selective inhibitor of the transforming growth factor-β (TGF-β) type I receptor activin receptor-like kinase ALK5 (IC50 = 94 nM). |
M1743 | X-376 | X-376 is a potent and highly specific ALK small molecule tyrosine kinase inhibitor with IC50 of 0.61 nM. |
M1720 | AP26113 (Brigatinib) | AP26113 (Brigatinib) is a highly potent ALK inhibitor with IC50 of 0.6 nM. |
M58399 | F-1 | F-1 is a potent ALK and ROS1 dual inhibitor, suppresses phospho-ALK and its relative downstream signaling pathways, with IC50 values of 2.1 nM, 2.3 nM, 1.3 nM and 3.9 nM for ALKWT, ROS1WT, ALKL1196M and ALKG1202R, respectively. |
M57183 | ALK inhibitor 2 | ALK inhibitor 2 is a potent pyrimidin ALK inhibitor. |
M49468 | Neladalkib | Neladalkib (NVL-655, ALK-IN-27) is a novel, brain-permeable, selective ALK inhibitor with antitumor activity. For Ba/F3 CLIP1-LTK cells, NVL-655 has an IC50 of 2.7 nM. Neladalkib (NVL-655, ALK-IN-27) can be used in studies related to ALK-positive non-small cell lung cancer (NSCLC). |
M31136 | Conteltinib | Conteltinib (CT-707) is a potent second-generation mesenchymal lymphoma kinase (ALK) tyrosine kinase inhibitor (TKI) with antitumor activity for studies related to hepatocellular carcinoma (HCC). |
M29459 | ZX-29 | ZX-29 is a potent and selective ALK inhibitor with an IC50 of 2.1 nM, 1.3 nM and 3.9 nM for ALK, ALK L1196M and ALK G1202R mutations, respectively. ZX-29 is inactive against EGFR. ZX-29 induces apoptosis by inducing endoplasmic reticulum (ER) stress and overcomes cell resistance caused by an ALK mutation. ZX-29 also induces protective autophagy and has antitumor effect. |
M28270 | Ensartinib | Ensartinib (X-396) is a potent and dual ALK/MET inhibitor with IC50s of <0.4 nM and 0.74 nM, respectively. |
M14878 | Ensartinib dihydrochloride | Ensartinib dihydrochloride (X-396 dihydrochloride) is a potent and dual ALK/MET inhibitor with IC50s of <0.4 nM and 0.74 nM, respectively. |
M14877 | ALK inhibitor 1 | ALK inhibitor 1 (compound 17) is a potent pyrimidin ALK inhibitor. ALK inhibitor 1 is a potent inhibitor of testis-specific serine/threonine kinase 2 (TSSK2; IC50=31 nM) and focal adhesion kinase (FAK; IC50=2 nM). |
M9397 | MS4078 | MS4078 is a PROTAC degrader of ALK which potently decreases cellular levels of oncogenic active ALK fusion proteins in SU-DHL-1 lymphoma and NCI-H2228 lung cancer cells. |
M6186 | Repotrectinib (TPX-0005) | Repotrectinib (TPX-0005) is a potential best-in-class ALK/ROS1/TRK inhibitor against SRC, wild-type WT ALK, The IC50 values of ALK G1202R and ALK L1196M were 5.3 nM, 1.01 nM, 1.26 nM and 1.08 nM, respectively. |
M6168 | Ceritinib (LDK378) dihydrochloride | Ceritinib dihydrochloride (LDK378 dihydrochloride) is potent inhibitor against ALK with IC50 of 0.2 nM, shows 40- and 35-fold selectivity against IGF-1R and InsR, respectively. |
M5613 | Entrectinib (RXDX-101) | Entrectinib (RXDX-101) is an orally bioavailable pan-TrkA/B/C, ROS1 and ALK inhibitor with IC50 ranging between 0.1 and 1.7 nM. |
M5320 | Crizotinib hydrochloride | Crizotinib is inhibitor of the c-Met kinase and the NPM-ALK. Crizotinib inhibited cell proliferation in ALK-positive ALCL cells (IC50s=30 nM). Crizotinib is useful in treatment of anaplastic large-cell lymphoma. |
M5309 | ALK-IN-1 | ALK-IN-1 is an analog of AP26113 which is a potent and selective ALK inhibitor. It is also an inhibitor of EGFR. |
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