ALK

A unique collection of xnum kinase inhibitors/regulators for specific targeting of kinases, ready for high-throughput screening and high-content screening.

A unique collection of xnum kinase inhibitors/regulators for high throughput screening and high content screening for drug discovery in kinase related diseases;

ALK-IN-9 effectively inhibits cell growth with IC50 <0.2 nM for Ba/F3-EML4-ALK, KM12, KG-1.

CPD-1224, an oral ALK inhibitor derivative, binds cereblon, targets EML4-ALK fusions, and degrades ALK plus L1196M/G1202R mutants.

PROTAC ALK degrader-3 (4B) is an orally active PROTAC-based ALK degrader, efficiently inducing sustained degradation of ALK fusion protein and significant inhibition of downstream pathways in Karpas 299 cells with an IC50 of 119.33 nM. This compound exhibits antitumor activity.

SIAIS164018 hydrochloride is a PROTAC-based degrader targeting ALK and EGFR, exhibiting IC50 values of 2.5 nM for ALK and 6.6 nM for ALK G1202R.

ALK5 Inhibitor II has IC50s: 4 nM (auto), 18 nM (TGF-β assay), 23 nM (binding, HepG2).

Negative control for TL 13-112 . Displays no degradation of ALK in cell lines. Highly potent ALK inhibitor (IC50 = 0.34 nM).

TL13-22 is a potent inhibitor of ALK and does not lead to degradation of ALK proteins.TL13-22 is often used as a negative control for TL13-12 .

ALK-IN-13 is an ALK inhibitor.

ALK/ROS1-IN-3 (compound C01) is a dual inhibitor targeting ROS1 and ALK, with IC50 values of 42.3 nM for ROS1G2032R and 49.1 nM for ALKG1202R.

TL13-12 is a selective degrader of ALK-PROTAC and inhibits ALK activity (IC50: 0.69 nM).

2-Keto Crizotinib is an active lactam metabolite of crizotinib.

ALK5-IN-84 (Compound 23) is an ALK5 inhibitor with a pKi value of 9.35 for hALK5. Administered via inhalation, ALK5-IN-84 exhibits significant ALK5 inhibitory activity. This compound holds potential for research in developing inhalable ALK5 inhibitors.

Lys-PEG3-BA is a PROTAC degrader targeting EML4-ALK/EGFR, with DC50 values of 1.32 μM for H3122 cells (expressing EML4-ALK fusion protein) and 19.66 μM for H1975 cells (with EGFRL858R/T790M mutations). In vitro studies show that Lys-PEG3-BA can inhibit the proliferation of non-small cell lung cancer cells by modulating the ubiquitin-proteasome system. Lys-PEG3-BA is applicable for research related to non-small cell lung cancer.

ALK-IN-29 (compound 4c) exhibits inhibitory effects on tyrosine protein kinases such as ALK, CDK2/CyclinE1, and FAK, with the strongest inhibition observed against ALK kinase, displaying a 40.63% inhibition rate at a concentration of 10 μM. ALK-IN-29 is applicable in cancer research.

ALK/HDAC-IN-2 (Compound 19b) functions as an ALK/HDAC inhibitor, demonstrating IC₅₀ values of 8 nM for ALK WT and 1.18 μM for total HDACs. It is effective against ALK mutants G1202R, F1174L, and L1196M, with IC₅₀ values of 2.74, 9.23, and 34.28 nM, respectively. The compound shows potent and selective inhibition of HDAC1 (IC₅₀= 0.24 μM), while exhibiting weak inhibition against HDAC7, HDAC6, and HDAC11 (IC₅₀> 10 μM). Additionally, ALK/HDAC-IN-2 has broad-spectrum antiproliferative effects on various cancer cell lines, inducing cell cycle arrest and apoptosis. This compound is applicable for neuroblastoma research.

ALK-IN-12: potent ALK inhibitor (IC50: 0.18 nM), affects IGF1R and InsR (IC50: 20.3/90.6 nM), potential for cancer therapy.

ALK2-IN-6 is a potent and selective ALK2 inhibitor with an IC50 of 9 nM. ALK2-IN-6 exhibits excellent brain permeability and effectively suppresses bone morphogenetic protein signaling across various preclinical cancer models for the treatment of diffuse intrinsic pontine glioma.

EW-7195 inhibits ALK5/TGFβR1 (>300x selective over p38α) with 4.83 nM IC50, blocking TGF-β1 signaling, EMT, and breast cancer lung metastasis.