Chemical Property of (R)-6-(4-((4-Ethylpiperazin-1-yl)methyl)phenyl)-N-(1-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine
Chemical Property:
- Boiling Point:639.246 °C at 760 mmHg
- Flash Point:340.404 °C
- PSA：63.31000
- Density:1.204 g/cm3
- LogP:4.23320
- Storage Temp.:-20°C
- Solubility.:≥22.05 mg/mL in DMSO; insoluble in H2O; ≥14.4 mg/mL in EtOH with ultrasonic
- XLogP3:4.6
- Hydrogen Bond Donor Count:2
- Hydrogen Bond Acceptor Count:5
- Rotatable Bond Count:7
- Exact Mass:440.26884505
- Heavy Atom Count:33
- Complexity:579
- Purity/Quality:
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99%, *data from raw suppliers
AEE 788 *data from reagent suppliers
Safty Information:
- Pictogram(s):
- Hazard Codes:
- MSDS Files:
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SDS file from LookChem
Useful:
- Canonical SMILES:CCN1CCN(CC1)CC2=CC=C(C=C2)C3=CC4=C(N3)N=CN=C4NC(C)C5=CC=CC=C5
- Isomeric SMILES:CCN1CCN(CC1)CC2=CC=C(C=C2)C3=CC4=C(N3)N=CN=C4N[C@H](C)C5=CC=CC=C5
- Recent ClinicalTrials:Study of AEE788 in Patients With Recurrent/Relapse Glioblastoma Multiforme (GBM)
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Description
AEE788 (NVP-AEE788) is a potent inhibitor of EGFR and HER2/ErbB2 with IC50 of 2 nM and 6 nM, less potent to VEGFR2/KDR, c-Abl, c-Src, and Flt-1, does not inhibit Ins-R, IGF-1R, PKCα and CDK1. Phase 1/2. AEE788 is an inhibitor of both epidermal growth factor (EGF) and vascular endothelial growth factor (VEGF) receptor tyrosine kinase family members. It can inhibit EGFR and VEGFR tyrosine kinases with IC50 values of 2, 6, 77, and 59 nM for EGFR, ErbB2, KDR, and FLT1, respectively. AEE788 demonstrates antiproliferative activity against a range of EGFR and ErbB2-overexpressing cell lines and can inhibit the proliferation of EGF- and VEGF-stimulated human umbilical vein endothelial cells. It also has been shown to have antitumor and anti-angiogenic activity in numerous animal models of cancer.
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Uses
AEE788 is a novel multitargeted human epidermal receptor (HER) 1/2 and vascular endothelial growth factor receptor (VEGFR) 1/2 receptor family tyrosine kinases inhibitor with IC50 of 2, 6, 77, 59 nM for EGFR, ErbB2, KDR, and Flt-1. A novel dual receptor tyrosine kinase inhibitor of the EGF and the VEGF receptor, for treatment of human HCC cell lines and in a s.c. xenograft model. AEE788 is an inhibitor of both epidermal growth factor (EGF) and vascular endothelial growth factor (VEGF) receptor tyrosine kinase family members. It can inhibit EGFR and VEGFR tyrosine kinases with IC50 values of 2, 6, 77, and 59 nM for EGFR, ErbB2, KDR, and FLT1, respectively. AEE788 demonstrates antiproliferative activity against a range of EGFR and ErbB2-overexpressing cell lines and can inhibit the proliferation of EGF- and VEGF-stimulated human umbilical vein endothelial cells. It also has been shown to have antitumor and anti-angiogenic activity in numerous animal models of cancer.[Cayman Chemical]
