CEP-28122 is a highly potent and selective orally active ALK inhibitor with IC50 of 1.9 ± 0.5 nM in an enzyme-based TRF assay.IC50 value: 1.9 ± 0.5 nMTarget: ALKin vitro: CEP-28122 is a potent inhibitor of recombinant ALK activity and cellular ALK tyrosine phosphorylation. CEP-28122 also inhibits Flt4 with IC50 of 46 ±10 nM. CEP-28122 induces concentration-dependent growth inhibition/cytotoxicity of ALK-positive anaplastic large-cell lymphoma (ALCL), non-small celllung cancer (NSCLC), and neuroblastoma cells. [1]in vivo: CEP-28122 displays dose-dependent inhibition of ALK tyrosine phosphorylation in tumor xenografts in mice, with substantial target inhibition (>90%) for more than12 hours following single oral dosing at 30 mg/kg. Dose-dependent antitumor activity was observed in ALK-positive ALCL, NSCLC, and neuroblastoma tumor xenografts in mice administered CEP-28122 orally, with complete/near complete tumor regressions observed following treatment at doses of 30 mg/kg twice daily or higher. [1]
TGFβRI-IN-2 (compound 18) is a potent, selective and orally active (Activin-Like Kinase 5) ALK 5 inhibitor with pIC50 and pEC50 values of 7.6 and 6.63, respectively. TGFβRI-IN-2 can produce observed cardiac toxicity in vivo at high dose[1].
K02288 is a potent inhibitor of ALK, and inhibits ALK1/2/3/6 with IC50s of 1.8/1.1/34.4/6.3 nM; K02288 is less potent against ALK4/5, with IC50s of 302 nM and 321 nM.
ALK5-IN-6 is a potent inhibitor of ALK5. Transforming growth factor beta (TGF-β) is a multifunctional cytokine that is involved in regulating cell proliferation, differentiation and apoptosis through complex receptor signaling pathways on the cell surface in an autocrine, paracrine and endocrine manner. ALK5-IN-6 has the potential for the research of TGF-β-related diseases and conditions, including but not limited to tumors, fibrotic diseases, inflammatory diseases, autoimmune diseases, etc (extracted from patent WO2021129621A1, compound 1)[1].
ALK/EGFR-IN-1 (Compound 8l) is an ALK/EGFR dual inhibitor that blocks the phosphorylation of EGFR and ALK. ALK/EGFR-IN-1 inhibits ALK/EGFR mutants respectively, with IC50 of 4.3 nM for EGFR L858R T790M in H1975 cells and EML4-ALK in BaF3 cells, respectively. and 3.6 nM. ALK/EGFR-IN-1 may be used in NSCLC research[1].
SIAIS117 is a potent Brigatinib-PROTAC degrader. SIAIS117 is a ALK PROTAC based on Brigatinib and VHL-1 conjunction. SIAIS117 can degrade ALK G1202R point mutation effectively. SIAIS117 blocks the growth of SR and H2228 cancer cell lines. SIAIS117 has the potentially anti-proliferation ability of small cell lung cancer[1].
Crizotinib hydrochloride is a potent inhibitor of c-Met and ALK with IC50s of 11 nM and 24 nM in cell-based assays, respectively.
Ceritinib (LDK378) is a potent and specific ALK inhibitor with an IC50 of 0.2 nM.
Lorlatinib is a potent, dual ALK/ROS1 inhibitor, with Kis of 0.02 nM, 0.07 nM, and 0.7 nM for ROS1, wild type ALK, and ALK-L1196M, respectively.
ALK5-IN-7 is a potent inhibitor of ALK5. Transforming growth factor beta (TGF-β) is a multifunctional cytokine that is involved in regulating cell proliferation, differentiation and apoptosis through complex receptor signaling pathways on the cell surface in an autocrine, paracrine and endocrine manner. ALK5-IN-7 has the potential for the research of TGF-β-related diseases and conditions, including but not limited to tumors, fibrotic diseases, inflammatory diseases, autoimmune diseases, etc (extracted from patent WO2021129621A1, compound 4)[1].
Ensartinib (X-396) is a potent and dual ALK/MET inhibitor with IC50s of <0.4 nM and 0.74 nM, respectively.
A 83-01 is a potent inhibitor of TGF-β type I receptor ALK5 kinase, type I activin/nodal receptor ALK4 and type I nodal receptor ALK7, with IC50s of 12, 45 and 7.5 nM, respectively.
Envonalkib is a potent and orally active inhibitor of ALK, with IC50s of 1.96 nM, 35.1 nM, and 61.3 nM for WT and mutated L1196M and G1269S-ALK. Envonalkib can be used for the research of non-small cell lung cancer[1].
CEP-37440 is a novel potent and selective Dual FAK/ALK inhibitor with IC50 s of 2.3 nM (FAK) and 120 nM(ALK cellular IC50 in 75% human plasma).IC50 value: 2.3 nM (FAK); 120 nM (ALK cellular IC50 in 75% human plasma)Target: Dual FAK/ALKPreparation of fused bicyclic 2,4-diaminopyrimidine derivatives as a dual ALK and FAK inhibitorBy Jacobs, Martin J.; Ott, Gregory R. From PCT Int. Appl. (2013), WO 2013134353 A1 20130912.
TL13-22 is a negative control for TL13-12 (HY-122582) and a potent ALK inhibitor with an IC50 of 0.54 nM. TL13-22 does not degrade ALK in cells[1].
NVP-TAE 684 is a highly potent and selective ALK inhibitor, which blocks the growth of ALCL-derived and ALK-dependent cell lines with IC50 values between 2 and 10 nM.
ALK2-IN-5, pyrazolopyrimidine compound, is an ALK2 inhibitor. ALK2-IN-5 can inhibit ALK2 activity and FGFR activity. ALK2-IN-5 can be used for the research of disorders associated with ALK2 activity and/or FGFR activity, such as cancer[1].
AZD-3463 is an ALK/IGF1R inhibitor which overcomes multiple mechanisms of acquired resistance to crizotinib.IC50 Value:Target: ALK/IGF1R
Itacnosertib (TP-0184) is both inhibitor to JAK2, ACVR1 (ALK2) and ALK5 as described in WO2014151871[1].
MS4078 is an anaplastic lymphoma kinase (ALK) PROTAC (degrader) with a Kd of 19 nM for binding affinity to ALK[1].
BIBF0775 is a potent and selective transforming growth factor β (TGFβ) type I receptor (Alk5) inhibitor with an IC50 of 34 nM.