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.

Insulin (human) is a peptide hormone that promotes glycogen synthesis and regulates glucose levels in the blood. Insulin (human) has hypoglycemic activity and is used clinically to treat hyperglycemia in diabetic patients.

Insulin(cattle) is a peptide hormone that promotes glycogen synthesis and regulates glucose levels in the blood. Insulin has hypoglycemic activity and is used clinically to treat hyperglycemia in diabetic patients.

NBI-31772 (NBI 31772) is the potent inhibitor of insulin-like growth factor-1 binding protein (IGFBP, Ki = 47 nM). NBI-31772 can be used in research on IGF-responsive diseases.

Kaempferitrin (Lespenephryl) has antidepressant-like effect related to the serotonergic system, principally 5-HT1A. Kaempferitrin exerts cytotoxic and antitumor effects against HeLa cells. Kaempferitrin stimulates glucose-metabolizing enzymes, promotes glucose homeostasis. Kaempferitrin exerts immunostimulatory effects on immune responses mediated by splenocytes, macrophages, PBMC and NK cells. Kaempferitrin induces cytotoxic effects to include: cell cycle arrest in G1 phase and apoptosis via the intrinsic pathway in a caspase-dependent pathway.

Picropodophyllin (Picropodophyllin (PPP)) (PPP) is a specific IGF-1R inhibitor (IC50: 1 nM). Picropodophyllin specifically inhibits the activity and downregulates the cellular expression of IGF1R without interfering with activities of other growth factor receptors, such as receptors for insulin, epidermal growth factor, platelet-derived growth factor, fibroblast growth factor and mast stem cell growth factor (KIT).

Rhoifolin (Apigenin 7-O-neohesperidoside) is extracted from Turpinia arguya Seem dried leaves.

GIP (human) acetate is a stimulator of glucose-dependent insulin secretion and a weak inhibitor of gastric acid secretion. GIP (human) acetate plays a vital role in lipid metabolism and the development of obesity.

URMC-099 is an orally bioavailable, brain penetrant MLK inhibitor (IC50: 19/42/14/150 nM, for MLK1/MLK2/MLK3/DLK), and also inhibits LRRK2 activity (IC50: 11 nM).

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.

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.

PD173074 is an effective FGFR1 inhibitor (IC50: 25 nM) and also inhibits VEGFR2 (IC50: 100-200 nM) in cell-free assays. The selectivity is higher ~1000-fold for FGFR1 than PDGFR and c-Src.

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.

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

Ganitumab (AMG 479) is a highly potent monoclonal antibody targeting the type 1 insulin-like growth factor receptor (IGF1R). Recognized for binding IGF1R at low concentrations with a KD value of 0.22 nM, Ganitumab inhibits IGF1R interactions with IGF1 and IGF2 in mice, making it useful for cancer research.

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

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

KW-2450 free base is an orally bioavailable inhibitor of insulin-like growth factor 1 receptor (IGF-1R) and insulin receptor (IR) tyrosine kinases with potential antineoplastic activity. IGF-1R/IR inhibitor KW-2450 free base selectively binds to and inhibits the activities of IGF-1R and IR, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. IGF-R1 and IR tyrosine kinases, overexpressed in a variety of human cancers, play significant roles in the stimulation of cellular proliferation, oncogenic transformation, and suppression of apoptosis.

Protonstatin-1 is used as a hypoglycemic agent and as a compound for the treatment of Alzheimer's disease, inhibits IGFIR kinase activity and can be used in cancer research.

1. Ginsenoside Rg5 could be a beneficial agent for the treatment of Alzheimer's disease. 2. Ginsenoside Rg5 suppresses LPS-induced nitric oxide (NO) production and proinflammatory TNF-α secretion. 3. Ginsenoside Rg5 can ameliorate lung inflammation possib

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

Urolithin C is a gut metabolite of ellagic acid. Urolithin C induces apoptosis in PC12 cells through a mitochondria-mediated pathway.

HNMPA is a membrane impermeable inhibitor of insulin receptor tyrosine kinase. HNMPA inhibits tyrosine and serine autophosphorylation by the human insulin receptor. HNMPA exhibits no effect on cyclic AMP-dependent protein kinase or protein kinase C activities.

Xentuzumab (BI836845) is a recombinant monoclonal antibody to humanised IGF ligand that inhibits IGF1 and IGF2 growth-promoting signalling and inhibits AKT activation for the study of solid tumours.

NVP-AEW541 (AEW541), a potent inhibitor of IGF-1R(IC50=150 nM) and InsR(IC50=140 nM), exhibits excellent efficiency and specificity for IGF-1R in a cell-based assay.

GIP (3-42), human (Gastric Inhibitory Polypeptide (3-42) (human)) is a peptide that acts as a glucose-dependent proinsulinotropic polypeptide (GIP) receptor antagonist and regulates insulin secretion and the metabolic effects of GIP in vivo, which can be used to study type 2 diabetes.

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.

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.

BMS-536924 (BMS 536924) is an ATP-competitive IGF-1R IR inhibitor with IC50 of 100 nM 73 nM, modest activity for Mek, Fak, and Lck with very little activity for Akt1, MAPK1 2.

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

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.

NVP-ADW742 (ADW) 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.

GIP (1-30) amide, porcine acetate is an agonist of fully glucose-dependent insulinotropic polypeptide (GIP) receptor. GIP (1-30) amide, porcine acetate can weakly inhibit gastric acid secretion and strongly stimulate insulin.

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).

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.

Picropodophyllotoxin (AXL 1717) is a cyclolignan alkaloid found in the mayapple plant family (Podophyllum peltatum), and a small molecule inhibitor of the insulin-like growth factor 1 receptor (IGF1R) with potential antineoplastic activity. Picropodophyllotoxin (AXL 1717) specifically inhibits the activity and downregulates the cellular expression of IGF1R without interfering with activities of other growth factor receptors, such as receptors for insulin, epidermal growth factor, platelet-derived growth factor, fibroblast growth factor and mast/stem cell growth factor (KIT). This agent shows potent activity in the suppression o f tumor cell proliferation and the induction of tumor cell apoptosis. IGF1R, a receptor tyrosine kinase overexpressed in a variety of human cancers, plays a critical role in the growth and survival of many types of cancer cells.

PD168393 is an irreversible EGFR inhibitor (IC50: 0.70 nM), irreversibly alkylate Cys-773; inactive against PKC, FGFR, PDGFR, and insulin.

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

NT157 is a small molecule tyrphostin targeting IRS protein and has the potential to inhibit IGF-1R and STAT3 signaling pathways in TME cancer cells and stromal cells, resulting in decreased cancer cell survival.

MSDC 0160 (CAY10415) is a prototype mTOT-modulating insulin sensitizer being used in trials studying the treatment of Type 2 Diabetes and Alzheimer's Disease.

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

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.

Xenin 8 acetate is a biologically active fragment of Xenin in the neurotensin/xenopsin family. Xenin 8 acetate augments Arginine-induced insulin release (by 40%) and potentiates the glucagon responses to both Arginine (by 60%), Carbachol (by 50%).

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.

WAY-270250 is an IGF-1R/SRC inhibitor.

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

ALK inhibitor 1 is a selective ALK kinase inhibitor.

Chromeceptin is an inhibitor of the IGF signaling pathway, decreases the numbers of tumorsphere, and inhibits the AKT/mTOR pathway.