Product Name: IGF1R antagonist
Product Number: PE-05AAC95
| Size: | 200 µg | Price: | 90.00 | |
| 1 mg | $US | 184.00 | ||
| 5 mg | 386.00 |
Peptide Name: IGF1R antagonist
Product Use: Peptide has binding affinity to IGF-1R and an antagonistic effect on IGF-1 dependent growth of SW480 cells.
Peptide Production Method: Solid-phase peptide synthesis
Peptide Origin: Homo sapiens
Peptide Sequence: DFYGCLLDLSLGVPSLGWRRRCITA
Peptide Modifications N Terminus: Free amino
Peptide Modifications C Terminus: Amide
Peptide Modifications Other: C-C cyclized
Peptide Molecular Mass Calculated: 2811.3 Da
Peptide Purity Percent after Synthesis and Purification: >95
Product Use: Peptide has binding affinity to IGF-1R and an antagonistic effect on IGF-1 dependent growth of SW480 cells.
Peptide Production Method: Solid-phase peptide synthesis
Peptide Origin: Homo sapiens
Peptide Sequence: DFYGCLLDLSLGVPSLGWRRRCITA
Peptide Modifications N Terminus: Free amino
Peptide Modifications C Terminus: Amide
Peptide Modifications Other: C-C cyclized
Peptide Molecular Mass Calculated: 2811.3 Da
Peptide Purity Percent after Synthesis and Purification: >95
Peptide Appearance: White powder
Peptide Form: Solid
Storage Conditions: -20°C
Peptide Form: Solid
Storage Conditions: -20°C
Scientific Background: IGF1R is a protein-tyrosine kinase of the TK group and InsR family. It mediates the effects of its ligand insulin-like growth factor 1 (IGF1) to promote cell growth and survival. The pre-dimerized receptor also displays weak affinity for both insulin and IGF2. Once ligand bound, the IGF1R undergoes autophosphorylation and activates several downstream signalling pathways, including the PI3K-Akt pathway and the Ras/Raf/MAP kinase pathway to induce cell growth and survival. Autophosphorylation Y1161 and Y346 increases its phosphotransferase activity and induces interaction with Src. Y1346 autophosphorylation also mediates GRB10 binding to IGF1R. Y980, Y1161, Y1165 and Y1166 autophosphorylation also increases its phosphotransferase activity. Y980 autophosphorylation also appears to mediate IRS1 or Shc1 interactions with IGF1R. IGFR1 is an oncoprotein (OP). Cancer-related mutations in human tumours point to a gain of function of the protein kinase. The active form of the protein kinase normally acts to promote tumour cell proliferation. IGF1R been shown to be an important signalling component in several types of human cancers. In particular, the activated receptor is critical for tumour transformation, malignant cell survival, and the maintenance of the transformed phenotype. In addition, activated IGF1R protein functions to inhibit apoptosis via indirect phosphorylation of the BAD protein via Akt, as well as plays an important role in the regulation of cancer cell motility and metastasis. Several cancer types display increased expression of IGF1R and/or increased catalytic activity of the protein, including prostate cancer, colorectal adenoma, and melanoma. Additionally, cross-talk between the IGF signalling pathway and the estrogen receptor signalling pathway has been demonstrated in breast cancer cells as a central mechanism of cell growth regulation. Furthermore, therapies aimed at the inhibition of IGF1R signalling have shown promise as potential cancer treatments. Insertional mutagenesis studies in mice support a role for this protein kinase in mouse cancer oncogenesis.
© Kinexus Bioinformatics Corporation 2017