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Tyrosine Kinase/Adaptors

Discoidin Domain Receptor (DDR)

IGF-1R

The insulin-like growth factor 1 (IGF-1) receptor is a protein found on the surface of human cells. It is a transmembrane receptor that is activated by a hormone called insulin-like growth factor 1 (IGF-1) and by a related hormone called IGF-2. It belongs to the large class of tyrosine kinase receptors. This receptor mediates the effects of IGF-1, which is a polypeptide protein hormone similar in molecular structure to insulin. IGF-1 plays an important role in growth and continues to have anabolic effects in adults – meaning that it can induce hypertrophy of skeletal muscle and other target tissues. Mice lacking the IGF-1 receptor die late in development, and show a dramatic reduction in body mass, testifying to the strong growth-promoting effect of this receptor.

Filter HomeSignaling PathwaysTyrosine Kinase/AdaptorsIGF-1R

Linsitinib

T6017867160-71-2

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.

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Insulin (human)

T822111061-68-0

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.

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Insulin(cattle)

TP112511070-73-8

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.

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GIP (human) acetate

TP2018L

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.

$238

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GSK1904529A

T60031089283-49-7In house

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

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NBI-31772

T8906374620-70-9

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.

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Kaempferitrin

T3386482-38-2

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.

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PD173074

T2642219580-11-7

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.

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Rhoifolin

T275517306-46-6

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

$120

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Ceritinib dihydrochloride

T1791L1380575-43-8

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.

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I-OMe-Tyrphostin AG 538

T115931094048-77-7In house

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.

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Tyrphostin AG 538

T67707133550-18-2In house

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.

$100

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Ganitumab

T76810905703-97-1

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.

$289

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Ceritinib

T17911032900-25-6

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.

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Brigatinib

T36211197953-54-0

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

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AZD-3463

T19671356962-20-3

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

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Picropodophyllin

T6943477-47-4

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).

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Protonstatin-1

T71812521972-99-6

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.

$195

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KW-2450 free base

T68405904899-25-8In house

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.

$588

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Indirubin Derivative E804

T11654854171-35-0In house

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

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Urolithin C

TN7108165393-06-6

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

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AG1024

T269365678-07-1

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

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HNMPA

T21761132541-52-7In house

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.

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Xentuzumab

T767951417158-65-6

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.

$347

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NVP-AEW541

T6080475489-16-8

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.

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GIP (3-42), human

T375891802086-25-4

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.

$196

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BMS-754807

T23491001350-96-4

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.

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AZ7550

T135641421373-99-0

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

$133

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NVP-TAE 226

T1918761437-28-9

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.

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BMS-536924

T6419468740-43-4

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.

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GSK1838705A

T30791116235-97-2

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.

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NT157

T46051384426-12-3

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.

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NVP-ADW742

T6079475488-23-4

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.

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GIP (1-30) amide, porcine acetate

T37588L

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.

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XL228

T17267898280-07-4

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).

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PD168393

T6932194423-15-9

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

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URMC-099

T60571229582-33-5

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).

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AZ7550 hydrochloride

T13564L2309762-40-9

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

$126

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Ginsenoside Rg5

T6S1487186763-78-0

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

$115

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MSDC 0160

T2607146062-49-9

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.

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PQ401

T2085196868-63-0

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

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ALK-IN-1

T30591197958-12-5

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.

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Xenin 8 acetate

TP2209L

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%).

$243

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WAY-270250

T77624852367-46-5

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

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Lenaldekar

T24398418800-15-4

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.

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