AEE788
- CAS No.
- 497839-62-0
- Chemical Name:
- AEE788
- Synonyms
- AEE788;CS-375;NVP-AEE788;AEE 788AEE-788;AEE788 USP/EP/BP;AEE788 (NVP-AEE788);AEE788 (NVP-AEE788);AEE-788;AEE 788;NVP-AEE 788;(R)-6-(4-((4-Ethylpiperazin-1-yl)methyl)phenyl)-N-(1-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidin-4;6-(4-((4-ethylpiperazin-1-yl)methyl)phenyl) -N-(1-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine;(R)-6-(4-((4-Ethylpiperazin-1-yl)methyl)phenyl)-N-(1-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine
- CBNumber:
- CB02500944
- Molecular Formula:
- C27H32N6
- Molecular Weight:
- 440.58
- MDL Number:
- MFCD11100351
- MOL File:
- 497839-62-0.mol
- MSDS File:
- SDS
| storage temp. | -20°C |
|---|---|
| solubility | ≥22.05 mg/mL in DMSO; insoluble in H2O; ≥14.4 mg/mL in EtOH with ultrasonic |
| form | powder |
| color | white to beige |
| CAS DataBase Reference | 497839-62-0 |
| FDA UNII | F9JLR95I3I |
| NCI Dictionary of Cancer Terms | AEE788 |
| NCI Drug Dictionary | AEE788 |
AEE788 price More Price(39)
| Manufacturer | Product number | Product description | CAS number | Packaging | Price | Updated | Buy |
|---|---|---|---|---|---|---|---|
| Sigma-Aldrich | SML1400 | AEE788 ≥98% (HPLC) | 497839-62-0 | 5mg | $129 | 2022-05-15 | Buy |
| Cayman Chemical | 18416 | AEE788 ≥98% | 497839-62-0 | 1mg | $38 | 2024-03-01 | Buy |
| Cayman Chemical | 18416 | AEE788 ≥98% | 497839-62-0 | 5mg | $120 | 2024-03-01 | Buy |
| Cayman Chemical | 18416 | AEE788 ≥98% | 497839-62-0 | 10mg | $220 | 2024-03-01 | Buy |
| Cayman Chemical | 18416 | AEE788 ≥98% | 497839-62-0 | 25mg | $456 | 2024-03-01 | Buy |
AEE788 Chemical Properties,Uses,Production
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.
Description
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.
Uses
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]
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.
Uses
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.
Definition
ChEBI: AEE788 is a 6-{4-[(4-ethylpiperazin-1-yl)methyl]phenyl}-N-(1-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine which adopts an R-configuration. It is a potent inhibitor of human EGFR, VEGFR and HER2 receptor tyrosine kinases and exhibits anticancer and antiangiogenic activity. It has a role as an epidermal growth factor receptor antagonist, an EC 2.7.10.1 (receptor protein-tyrosine kinase) inhibitor, an antineoplastic agent, an angiogenesis inhibitor, a trypanocidal drug and an apoptosis inducer.
storage
Store at -20°C
References
[1] venkatesan p, bhutia sk, singh ak et al. aee788 potentiates celecoxib-induced growth inhibition and apoptosis in human colon cancer cells. life sci. 2012 oct 22;91(15-16):789-99.
[2] park yw, younes mn, jasser sa et al. aee788, a dual tyrosine kinase receptor inhibitor, induces endothelial cell apoptosis in human cutaneous squamous cell carcinoma xenografts in nude mice. clin cancer res. 2005 mar 1;11(5):1963-73.
[3] traxler p, allegrini pr, brandt r et al. aee788: a dual family epidermal growth factor receptor/erbb2 and vascular endothelial growth factor receptor tyrosine kinase inhibitor with antitumor and antiangiogenic activity. cancer res. 2004 jul 15;64(14):4931-41.
[4] evans ah, pancholi s, farmer i et al. egfr/her2 inhibitor aee788 increases er-mediated transcription in her2/er-positive breast cancer cells but functions synergistically with endocrine therapy. br j cancer. 2010 apr 13;102(8):1235-43.
[5] meco d, servidei t, zannoni gf et al. dual inhibitor aee788 reduces tumor growth in preclinical models of medulloblastoma. transl oncol. 2010 oct 1;3(5):326-35.
AEE788 Preparation Products And Raw materials
Raw materials
Preparation Products
| Supplier | Tel | Country | ProdList | Advantage | |
|---|---|---|---|---|---|
| ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32957 | 60 |
| Hubei xin bonus chemical co. LTD | 86-13657291602 | linda@hubeijusheng.com | CHINA | 22963 | 58 |
| BOC Sciences | +1-631-485-4226 | inquiry@bocsci.com | United States | 19553 | 58 |
| CONIER CHEM AND PHARMA LIMITED | +8618523575427 | sales@conier.com | China | 49374 | 58 |
| career henan chemical co | +86-0371-86658258 +8613203830695 | factory@coreychem.com | China | 29811 | 58 |
| TargetMol Chemicals Inc. | +1-781-999-5354 +1-00000000000 | marketing@targetmol.com | United States | 32161 | 58 |
| Dideu Industries Group Limited | +86-29-89586680 +86-15129568250 | 1026@dideu.com | China | 22784 | 58 |
| Finetech Industry Limited | +86-27-87465837 +8618971612321 | info@finetechnology-ind.com | China | 9639 | 58 |
| Zhejiang J&C Biological Technology Co.,Limited | +1-2135480471 +1-2135480471 | sales@sarms4muscle.com | China | 10473 | 58 |
| InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6391 | 58 |
