AEE-788 - CAS 497839-62-0
Catalog number: B0084-258485
Category: Inhibitor
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Molecular Formula:
C27H32N6
Molecular Weight:
440.595
COA:
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Targets:
EGFR | VEGFR
Description:
AEE-788 is an orally bioavailable multiple-receptor tyrosine kinase inhibitor. AEE788 inhibits phosphorylation of the tyrosine kinases of epidermal growth factor receptor (EGFR), human epidermal growth factor receptor 2 (HER2), and vascular endothelial growth factor receptor 2 (VEGF2), resulting in receptor inhibition, the inhibition of cellular proliferation, and induction of tumor cell and tumor-associated endothelial cell apoptosis.
Ordering Information
Catalog Number Size Price Stock Quantity
B0084-258485 10 mg $198 In stock
B0084-258485 50 mg $598 In stock
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Purity:
>98%
Appearance:
Solid Powder
Synonyms:
AEE 788; AEE788; 6-[4-[(4-ethylpiperazin-1-yl)methyl]phenyl]-N-[(1R)-1-phenylethyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine
MSDS:
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InChIKey:
OONFNUWBHFSNBT-HXUWFJFHSA-N
InChI:
InChI=1S/C27H32N6/c1-3-32-13-15-33(16-14-32)18-21-9-11-23(12-10-21)25-17-24-26(28-19-29-27(24)31-25)30-20(2)22-7-5-4-6-8-22/h4-12,17,19-20H,3,13-16,18H2,1-2H3,(H2,28,29,30,31)/t20-/m1/s1
Canonical SMILES:
CCN1CCN(CC1)CC2=CC=C(C=C2)C3=CC4=C(N3)N=CN=C4NC(C)C5=CC=CC=C5
1.Effect of AEE788 and/or Celecoxib on colon cancer cell morphology using advanced microscopic techniques.
Venkatesan P;Das S;Krishnan MM;Chakraborty C;Chaudhury K;Mandal M Micron. 2010 Apr;41(3):247-56. doi: 10.1016/j.micron.2009.10.008. Epub 2009 Nov 10.
Analysis of changes in cancer cell morphology and cytoskeletal element induced by external stimuli is focus of current cancer chemotherapeutic studies. Cancer cell cytoskeleton is complex network of interwoven protein fibers composed of microtubules, microfilaments and intermediate filaments. These interwoven protein fibers are responsible for maintaining cell morphology, movement, adhesion and transmembrane signal transmission. In this study, morphological and cytoskeletal changes induced by AEE788 and/or Celecoxib on colon cancer cell HCT 15 were analyzed using advanced microscopic techniques. Cell proliferation assay was used for determining IC(50) of AEE788 and/or Celecoxib on HCT 15. Confocal microscopic analysis of AEE788 and/or Celecoxib treated HCT 15 was performed using Rhodamine-Phalloidin (actin stain) and Hoechst 33342 (nuclear stain). Atomic force (AFM) and scanning electron microscopic (SEM) studies were also performed to analyze cell morphology and cell wall extension (filopodia and lamellipodia). In addition, quantitative analysis of morphological parameters was studied using cellular image processing technique. This is the first report that combination of AEE788 and Celecoxib additively increase growth inhibition and cell death on human colon cancer cell HCT 15 as estimated by cell proliferation assay.
2.Simultaneous inhibition of EGFR, VEGFR, and platelet-derived growth factor receptor signaling combined with gemcitabine produces therapy of human pancreatic carcinoma and prolongs survival in an orthotopic nude mouse model.
Yokoi K;Sasaki T;Bucana CD;Fan D;Baker CH;Kitadai Y;Kuwai T;Abbruzzese JL;Fidler IJ Cancer Res. 2005 Nov 15;65(22):10371-80.
Although gemcitabine has been approved as the first-line chemotherapeutic reagent for pancreatic cancer, its response rate is low and average survival duration is still only marginal. Because epidermal growth factor receptor (EGFR), vascular endothelial growth factor receptor (VEGFR), and platelet-derived growth factor receptor (PDGFR) modulate tumor progression, we hypothesized that inhibition of phosphorylation of all three on tumor cells, tumor-associated endothelial cells, and stroma cells would improve the treatment efficacy of gemcitabine in an orthotopic pancreatic tumor model in nude mice and prolong survival. We implanted L3.6pl, a human pancreatic cancer cell, in the pancreas of nude mice. We found that tumor-associated endothelial cells in this model highly expressed phosphorylated EGFR, VEGFR, and PDGFR. Oral administration of AEE788, a dual tyrosine kinase inhibitor against EGFR and VEGFR, decreased phosphorylation of EGFR and VEGFR. PDGFR phosphorylation was inhibited by STI571. Although i.p. injection of gemcitabine did not inhibit tumor growth, its combination with AEE788 and STI571 produced >80% inhibition of tumor growth and prolonged survival in parallel with increases in number of tumor cells and tumor-associated endothelial cell apoptosis, decreased microvascular density, decreased proliferation rate, and prolonged survival.
3.Dual inhibition of epidermal growth factor receptor and vascular endothelial growth factor receptor phosphorylation by AEE788 reduces growth and metastasis of human colon carcinoma in an orthotopic nude mouse model.
Yokoi K;Thaker PH;Yazici S;Rebhun RR;Nam DH;He J;Kim SJ;Abbruzzese JL;Hamilton SR;Fidler IJ Cancer Res. 2005 May 1;65(9):3716-25.
We studied growth factors and their receptors in tumor cells and tumor-associated endothelial cells as the therapeutic targets in colon cancer. Immunohistochemical analysis of 13 surgical specimens of human colon adenocarcinoma revealed that both tumor cells and tumor-associated endothelial cells in 11 of the 13 specimens expressed the epidermal growth factor (EGF), transforming growth factor alpha (TGF-alpha), EGF receptor (EGFR), phosphorylated EGFR (pEGFR), vascular endothelial growth factor (VEGF), VEGF receptor (VEGFR), and phosphorylated VEGFR (pVEGFR). HT29 human colon cancer cells growing orthotopically in the cecum of nude mice expressed a high level of EGF, EGFR, pEGFR, VEGF, VEGFR, and pVEGFR. Double-immunofluorescence staining found that tumor-associated mouse endothelial cells also expressed pEGFR and pVEGFR. Tumors in mice treated for 5 weeks with oral AEE788 (an inhibitor of EGFR and VEGFR tyrosine kinase) as a single agent or with CPT-11 alone were smaller (>50%) than those in control mice. Mice treated with the combination of AEE788 and CPT-11 had significantly smaller tumors (P < 0.01) and complete inhibition of lymph node metastasis. AEE788 alone or in combination with CPT-11 inhibited pEGFR, pVEGFR, and phosphorylated Akt expression on tumor-associated endothelial cells as well as on tumor cells.
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CAS 497839-62-0 AEE-788

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