igf-1r

OSI-906 (Linsitinib (OSI-906)) is an orally bioavailable small molecule inhibitor of the insulin-like growth factor 1 receptor (IGF-1R) with potential antineoplastic activity. Linsitinib selectively inhibits IGF-1R, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. Overexpressed in a variety of human cancers, IGF-1R stimulates cell proliferation, enables oncogenic transformation, and suppresses apoptosis.

I-OMe-Tyrphostin AG 538 is a specific IGF-1R inhibitor and ATP-competitive inhibitor of PI5P4Kα (IC50: 1 µM).I-OMe-Tyrphostin AG 538 inhibits IGF-1R-mediated signaling and exhibits preferential cytotoxicity to nutrient-deficient PANC1 cells.

Indirubin Derivative E804 is a potent insulin-like growth factor type 1 receptor (IGF1R) inhibitor with potential antitumor activity.

GSK1904529A (GSK 4529) is a specific inhibitor of IGF-1R (IC50=27 nM) and IR(IC50=25 nM) .

Tyrphostin AG 538 is a chalcone compound, an IGF-1 receptor kinase inhibitor (IC₅0 : for 400 nM) that is potent, cell-permeable, reversible, and competitive.

Ceritinib (LDK378) is an ALK tyrosine kinase inhibitor (IC50=200 pM) with selective, ATP-competitive, and oral activity. Ceritinib also inhibits IGF-1R, InsR, and STK22D (IC50=8/7/23 nM). Ceritinib has antitumor activity.

ALK-IN-1 is a Brigatinib analog and an ALK inhibitor commonly used in anti-tumor research.

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

Lenaldekar (LDK) inhibits T-cell expansion and autoimmune encephalomyelitis. Lenaldekar causes dephosphorylation of members of the PI3 kinase/AKT/mTOR pathway and delays sensitive cells in late mitosis.

PQ401 inhibits autophosphorylation of IGF-1R domain with IC50 of <1 μM.

ALK inhibitor 1 is a selective ALK kinase inhibitor.

AZ7550, an active metabolite of AZD9291, inhibits the activity of IGF1R (IC50: 1.6 μM).

AZ7550 hydrochloride (AZ7550 hydrochloride ), an active metabolite of AZD9291, inhibits the activity of IGF1R (IC50: 1.6 μM).

AZ7550 trimesylate salt (AZ7550 Mesylate) is the active metabolite of ositinib, AZ7550 trimesylate salt inhibits IGF1R activity and can be used in the study of non-small cell lung cancer.

XL228 is an inhibitor of multi-targeted tyrosine kinase (IC50s: 5, 3.1, 1.6, 6.1, 2 nM for Bcr-Abl, Aurora A, IGF-1R, Src, and Lyn, respectively).

Ceritinib dihydrochloride (LDK378 dihydrochloride) is a selective, orally bioavailable, 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], demonstrating significant antitumor potency.

NVP-TAE 226 (TAE226) is a potent FAK inhibitor (IC50: 5.5 nM), exhibiting even greater efficacy against Pyk2 (IC50: 3.5 nM), and is 10- to 100-fold less effective against IGF-1R, InsR, c-Met, and ALK.

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

IGF-1Rinhibitor-4 (compound 22) is a potent inhibitor of IGF-1R, demonstrating an inhibition rate of 63% at a concentration of 10 μM. This compound plays a significant role in cancer research.

IGF-1Rinhibitor-5 (compound 19) is a potent IGF-1R inhibitor with an IC50 of 6 μM, showing potential for cancer research.

PQ401 (IGF-1R Inhibitor II) suppresses autophosphorylation of IGF-1R domain(IC50<1 μM).

NVP-ADW742 is an IGF-1R inhibitor with IC50 of 0.17 μM, >16-fold more potent against IGF-1R than InsR; little activity to HER2, PDGFR, VEGFR-2, Bcr-Abl and c-Kit.

Dual IGF-1R/InsR Inhibitor BMS-754807 is an oral small molecule inhibitor of insulin-like growth factor 1 receptor (IGF-1R) and insulin receptor (InsR) tyrosine kinases with potential antineoplastic activity.

AG1024 (Tyrphostin) suppresses IGF-1R autophosphorylation(IC50=7 μM), and is less potent for IR(IC50=57 μM).