Description
ChemicalBook > CAS DataBase List > AEE788

AEE788

Description
Product Name
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
Formula Weight
440.58
MOL File
497839-62-0.mol
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AEE788 Property

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
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Safety

RTECS 
UY8836200
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Hazard and Precautionary Statements (GHS)

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N-Bromosuccinimide Price

Sigma-Aldrich
Product number
SML1400
Product name
AEE788
Purity
≥98% (HPLC)
Packaging
5mg
Price
$129
Updated
2022/05/15
Cayman Chemical
Product number
18416
Product name
AEE788
Purity
≥98%
Packaging
1mg
Price
$38
Updated
2024/03/01
Cayman Chemical
Product number
18416
Product name
AEE788
Purity
≥98%
Packaging
5mg
Price
$120
Updated
2024/03/01
Cayman Chemical
Product number
18416
Product name
AEE788
Purity
≥98%
Packaging
10mg
Price
$220
Updated
2024/03/01
Cayman Chemical
Product number
18416
Product name
AEE788
Purity
≥98%
Packaging
25mg
Price
$456
Updated
2024/03/01
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AEE788 Chemical Properties,Usage,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 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

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

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

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AEE788 Suppliers

TCI Europe
Tel
320-37350700
Fax
+32 (0)37350701
Email
sales@tcieurope.eu
Country
Europe
ProdList
23671
Advantage
75
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View Lastest Price from AEE788 manufacturers

Career Henan Chemical Co
Product
AEE788 497839-62-0
Price
US $3.00/KG
Min. Order
1KG
Purity
98%
Supply Ability
200KG
Release date
2020-01-12

497839-62-0, AEE788Related Search:


  • 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
  • AEE788
  • (R)-6-(4-((4-Ethylpiperazin-1-yl)methyl)phenyl)-N-(1-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine
  • 6-[4-[(4-Ethyl-1-piperazinyl)methyl]phenyl]-N-[(1R)-1-phenylethyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine
  • 7H-Pyrrolo[2,3-d]pyriMidin-4-aMine, 6-[4-[(4-ethyl-1-piperazinyl)Methyl]phenyl]-N-[(1R)-1-phenylethyl]-
  • [6-[4-(4-ethyl-piperazine-1-ylMethyl)-phenyl]-7H-pyrrolo[2,3-d]pyrinidinpyriMidin-4-yl]-((R)-1-phenyl-ethyl)-aMine
  • AEE 788AEE-788
  • [6-[4-[(4-Ethylpiperazin-1-yl)Methyl]phenyl]-7H-pyrrolo[2,3-d]pyriMidin -4-yl]-((R)-1-phenylethyl)aMine
  • AEE788 (NVP-AEE788)
  • NVP-AEE788
  • 6-[4-[(4-Ethyl-1-piperazinyl)methyl]phenyl]-N-[(1R)-1-phenylethyl]-7H-pyrrolo[2,3-d]pyrimidin-4-amine AEE 788
  • 6-(4-((4-ethylpiperazin-1-yl)methyl)phenyl) -N-(1-phenylethyl)-7H-pyrrolo[2,3-d]pyrimidin-4-amine
  • 6-(4-((4-ethyl-1-piperazinyl)methyl)phenyl)-N-((1R)-1-phenylethyl)-1H-Pyrrolo(2,3-D)pyrimidin-4-amine
  • CS-375
  • AEE788 USP/EP/BP
  • 497839-62-0
  • Inhibitors
  • Amines
  • Chiral Reagents
  • Heterocycles
  • Intermediates & Fine Chemicals
  • Pharmaceuticals
  • Tyrosine Kinase Inhibitors