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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.

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.
  • $33
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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.
  • $30
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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.
  • $48
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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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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.
  • $51
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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.
  • $43
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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.
  • $36
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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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GSK1904529A
T60031089283-49-7In house
GSK1904529A (GSK 4529) is a specific inhibitor of IGF-1R (IC50=27 nM) and IR(IC50=25 nM) .
  • $34
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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.
  • $48
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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.
  • $43
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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.
  • $51
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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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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.
  • $45
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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.
  • $48
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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).
  • $58
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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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Brigatinib
T36211197953-54-0
Brigatinib (AP-26113) is a highly potent and selective inhibitor of ALK.
  • $30
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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.
  • $58
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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.
  • $48
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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).
  • $34
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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.
  • $41
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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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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.
  • $34
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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.
  • $43
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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).
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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.
  • $41
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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.
  • $33
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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.
  • $50
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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).
  • $52
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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.
  • $79
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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).
  • $51
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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.
  • $33
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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.
  • $30
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PQ401
T2085196868-63-0
PQ401 (IGF-1R Inhibitor II) suppresses autophosphorylation of IGF-1R domain(IC50<1 μM).
  • $63
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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.
  • $40
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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.
  • $31
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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.
  • $89
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PQ401 hydrochloride (196868-63-0(free base))
T4324
PQ401 inhibits autophosphorylation of IGF-1R domain with IC50 of <1 μM.
  • $30
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ALK inhibitor 1
T10285761436-81-1
ALK inhibitor 1 is a selective ALK kinase inhibitor.
  • $48
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Chromeceptin
T60055331859-86-0
Chromeceptin is an inhibitor of the IGF signaling pathway, decreases the numbers of tumorsphere, and inhibits the AKT/mTOR pathway.
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