E-3810
- Product Name
- E-3810
- CAS No.
- 1058137-23-7
- Chemical Name
- E-3810
- Synonyms
- E-3810;CS-655;AL3810;CO-3810;CS-1836;S 80881;Lucitanib;AL3810 (AL-3810;Lucitanib(E3810);E-3810 USP/EP/BP
- CBNumber
- CB62624136
- Molecular Formula
- C26H25N3O4
- Formula Weight
- 443.49
- MOL File
- 1058137-23-7.mol
E-3810 Property
- Boiling point:
- 696.5±50.0 °C(Predicted)
- Density
- 1.285±0.06 g/cm3(Predicted)
- storage temp.
- Store at -20°C
- solubility
- Soluble in DMSO
- form
- Powder
- pka
- 14.65±0.46(Predicted)
- color
- White to yellow
Hazard and Precautionary Statements (GHS)
- Symbol(GHS)
-
- Signal word
- Warning
- Hazard statements
-
H302Harmful if swallowed
H315Causes skin irritation
H319Causes serious eye irritation
H335May cause respiratory irritation
- Precautionary statements
-
P261Avoid breathing dust/fume/gas/mist/vapours/spray.
P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.
N-Bromosuccinimide Price
- Product number
- CS-0782
- Product name
- Lucitanib
- Purity
- 99.32%
- Packaging
- 5mg
- Price
- $228
- Updated
- 2021/12/16
- Product number
- CS-0782
- Product name
- Lucitanib
- Purity
- 99.32%
- Packaging
- 10mg
- Price
- $372
- Updated
- 2021/12/16
- Product number
- API0017256
- Product name
- E-3810
- Purity
- 95.00%
- Packaging
- 5MG
- Price
- $427.9
- Updated
- 2021/12/16
- Product number
- orb180999
- Product name
- Lucitanib(E3810)
- Purity
- >98%
- Packaging
- 100mg
- Price
- $690.2
- Updated
- 2021/12/16
- Product number
- CS-0782
- Product name
- Lucitanib
- Purity
- 99.32%
- Packaging
- 50mg
- Price
- $1056
- Updated
- 2021/12/16
E-3810 Chemical Properties,Usage,Production
Uses
Lucitanib (E-3810) is a novel dual inhibitor of VEGFR and FGFR, potently and selectively inhibits VEGFR1, VEGFR2, VEGFR3, FGFR1 and FGFR2 with IC50s of 7 nM, 25 nM, 10 nM, 17.5 nM, and 82.5 nM, respectively[1][2][3].
Definition
ChEBI: A naphthalenecarboxamide obtained from formal condensation of the carboxy group of aminocyclopropyl)methoxy]-6-methoxyquinolin-4-yl}oxy)-1-naphthoic acid with methylamine.
in vivo
Lucitanib (E-3810), at oral dosing of 20 mg/kg for 7 consecutive days, completely inhibits (P<0.01) the bFGF induced angiogenic response compare with the response in vehicle-treated mice. Lucitanib (E-3810) shows a broad spectrum of activity, being active in all the xenografts tested (HT29 colon carcinoma, A2780 ovarian carcinoma, A498, SN12K1, and RXF393 renal carcinomas) with dose-dependent inhibition of tumor growth. E-3810 significantly delays growth during treatment, but tumors resume their growth when treatment is suspended; in a few cases, tumor regression is observed[1]. The activity of Lucitanib (E-3810) given at the doses of 15 mg/kg is tested on MDA-MB-231 breast cancer transplanted subcutaneously, at a late stage, when tumor masses reach 350 to 400 mg. This tumor xenograft is very sensitive to Lucitanib (E-3810), with complete tumor stabilization lasting throughout the 30-day treatment. As in other tumor models, tumors re-grow after withdrawal of Lucitanib (E-3810) at a rate similar to control tumors[3].
target
VEGFR-1
IC 50
VEGFR1: 7 nM (IC50); VEGFR2: 25 nM (IC50); VEGFR3: 10 nM (IC50); FGFR1: 17.5 nM (IC50); FGFR2: 82.5 nM (IC50)
References
[1] Bello E, et al. E-3810 is a potent dual inhibitor of VEGFR and FGFR that exerts antitumor activity in multiple preclinical models. Cancer Res. 2011 Feb 15;71(4):1396-405. DOI:10.1158/0008-5472.CAN-10-2700
[2] Colzani M, et al. Quantitative chemical proteomics identifies novel targets of the anti-cancer multi-kinase inhibitor E-3810. Mol Cell Proteomics. 2014 Jun;13(6):1495-509. DOI:10.1074/mcp.M113.034173
[3] Bello E, et al. The tyrosine kinase inhibitor E-3810 combined with NSC 125973 inhibits the growth of advanced-stage triple-negative breast cancer xenografts. Mol Cancer Ther. 2013 Feb;12(2):131-40 DOI:10.1158/1535-7163.MCT-12-0275-T
E-3810 Preparation Products And Raw materials
Raw materials
Preparation Products
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