Chinese Japanese Germany Korea
ChemicalBook >> CAS DataBase List >>Golvatinib (E7050)

Golvatinib (E7050)

Golvatinib (E7050) Structure
Golvatinib (E7050) structure
CAS No.
928037-13-2
Chemical Name:
Golvatinib (E7050)
Synonyms
E-7050;E-7060;CS-575;Golvatinib;Golvatinib (E7050);E-7060;E7050;E 7050;E-7050 (Golvatinib);Golvatinib E7050 E-7050;Golvatinib (E7050) USP/EP/BP;E7050; E-7050; E 7050; GOLVATINIB.
CBNumber:
CB12589746
Molecular Formula:
C33H37F2N7O4
Molecular Weight:
633.69
MDL Number:
MFCD22124462
MOL File:
928037-13-2.mol
MSDS File:
SDS
Last updated:2023-09-04 15:51:00
Request For Quotation

Golvatinib (E7050) Properties

Melting point 187 - 190°C
Boiling point 867.5±65.0 °C(Predicted)
Density 1.408
storage temp. Refrigerator
solubility DMSO (Slightly), Methanol (Slightly)
pka 12.91±0.70(Predicted)
form Solid
color White to Off-White
CAS DataBase Reference 928037-13-2
FDA UNII 516Z3YP58E
NCI Drug Dictionary golvatinib

SAFETY

Risk and Safety Statements

Symbol(GHS)  GHS hazard pictograms
GHS07
Signal word  Warning
Hazard statements  H315-H319-H335
Precautionary statements  P261-P264-P271-P280-P302+P352-P304+P340-P305+P351+P338-P312-P321-P362+P364-P332+P313-P337+P313-P403+P233-P405-P501
NFPA 704
0
2 0

Golvatinib (E7050) price More Price(23)

Manufacturer Product number Product description CAS number Packaging Price Updated Buy
Cayman Chemical 22143 Golvatinib ≥98% 928037-13-2 1mg $81 2024-03-01 Buy
Cayman Chemical 22143 Golvatinib ≥98% 928037-13-2 5mg $258 2024-03-01 Buy
Cayman Chemical 22143 Golvatinib ≥98% 928037-13-2 10mg $396 2024-03-01 Buy
Cayman Chemical 22143 Golvatinib ≥98% 928037-13-2 25mg $790 2024-03-01 Buy
TRC G410700 Golvatinib 928037-13-2 5mg $225 2021-12-16 Buy
Product number Packaging Price Buy
22143 1mg $81 Buy
22143 5mg $258 Buy
22143 10mg $396 Buy
22143 25mg $790 Buy
G410700 5mg $225 Buy

Golvatinib (E7050) Chemical Properties,Uses,Production

Description

Golvatinib (E7050) is a dual c-Met and VEGFR-2 inhibitor with IC50 of 14 nM and 16 nM, does not inhibit bFGF-stimulated HUVEC growth (up to 1000 nM). Phase 1/2.

In vitro

In vitro studies indicate that E7050 potently inhibits phosphorylation of both c-Met and VEGFR-2. E7050 also potently represses the growth of both c-met amplified tumor cells and endothelial cells stimulated with either HGF or VEGF. E7050 circumvents resistance to all of the reversible, irreversible, and mutant-selective EGFR-TKIs induced by exogenous and/or endogenous HGF in EGFR mutant lung cancer cell lines, by blocking the Met/Gab1/PI3K/Akt pathway in vitro. E7050 also prevents the emergence of gefitinib-resistant HCC827 cells induced by continuous exposure to HGF.

In vivo

In vivo studies using E7050 shows inhibition of the phosphorylation of c-Met and VEGFR-2 in tumors, and strong inhibition of tumor growth and tumor angiogenesis in xenograft models. Treatment of some tumor lines containing c-met amplifications with high doses of E7050 (50–200 mg/kg) induces tumor regression and disappearance. In a peritoneal dissemination model, E7050 shows an antitumor effect against peritoneal tumors as well as a significant prolongation of lifespan in treated mice. In another xenograft model research, tumors produced by HGF-transfected Ma-1 (Ma-1/HGF) cells are more angiogenic than vector control tumors and shows resistance to ZD1839. E7050 alone inhibits angiogenesis and retards growth of Ma-1/HGF tumors. E7050 combined with ZD1839 induces marked regression of tumor growth.

Description

Golvatinib is an orally bioavailable dual inhibitor of the receptor tyrosine kinases c-Met and VEGF receptor 2 (VEGFR2), which are involved in tumor progression. Golvatinib inhibits autophosphorylation of c-Met in MKN45 cells and phosphorylation of VEGFR2 in human umbilical vein endothelial cells (HUVECs; IC50s = 14 and 16 nM, respectively). It also inhibits proliferation of a variety of cancer cell lines and of HUVECs stimulated with hepatocyte growth factor (HGF) and VEGF but not bFGF (IC50s = 17, 84, and >1,000 nM for HGF-, VEGF-, and bFGF-stimulated HUVECs, respectively). In nude mouse xenograft models using MKN45, Hs746T, SNU-5, or EBC-1 cancer cells, golvatinib (25-200 mg/kg, daily) dose-dependently reduces tumor volume, and it increases survival in the model using MKN45 cells.

Uses

E7050 is a dual c-Met and VEGFR-2 inhibitor with IC50 of 14 nM and 16 nM, respectively.

Uses

Golvatinib is a potent and orally available inhibitor of c-MET and VEGFR-2 that exhibits potential antitumor properties by suppressing the overexpression of these receptor tyrosine kinases.

Definition

ChEBI: Golvatinib is an aromatic ether.

target

c-Met

References

[1] nakagawa t, tohyama o, yamaguchi a, et al. e7050: a dual c-met and vegfr-2 tyrosine kinase inhibitor promotes tumor regression and prolongs survival in mouse xenograft models. cancer science, 2010, 101(1): 210-215.

Golvatinib (E7050) Preparation Products And Raw materials

Raw materials

Preparation Products

Golvatinib (E7050) Suppliers

Global( 117)Suppliers
Supplier Tel Email Country ProdList Advantage
ATK CHEMICAL COMPANY LIMITED 		+undefined-21-51877795 ivan@atkchemical.com China 32715 60
Changzhou PBpharmaceutical R&D Co.,Ltd 		0519-83990708 info@pbpharm.com CHINA 498 58
Hubei xin bonus chemical co. LTD 		86-13657291602 linda@hubeijusheng.com CHINA 22968 58
BOC Sciences 		+1-631-485-4226 inquiry@bocsci.com United States 19553 58
CONIER CHEM AND PHARMA LIMITED 		+8618523575427 sales@conier.com China 49391 58
career henan chemical co 		+86-0371-86658258 15093356674; factory@coreychem.com China 29826 58
Dideu Industries Group Limited 		+86-29-89586680 +86-15129568250 1026@dideu.com China 27537 58
Dayang Chem (Hangzhou) Co.,Ltd. 		571-88938639 +8617705817739 info@dycnchem.com CHINA 52861 58
Zhejiang J&C Biological Technology Co.,Limited 		+1-2135480471 +1-2135480471 sales@sarms4muscle.com China 10523 58
InvivoChem 		+1-708-310-1919 +1-13798911105 sales@invivochem.cn United States 6393 58
Supplier Advantage
ATK CHEMICAL COMPANY LIMITED 		60
Changzhou PBpharmaceutical R&D Co.,Ltd 		58
Hubei xin bonus chemical co. LTD 		58
BOC Sciences 		58
CONIER CHEM AND PHARMA LIMITED 		58
career henan chemical co 		58
Dideu Industries Group Limited 		58
Dayang Chem (Hangzhou) Co.,Ltd. 		58
Zhejiang J&C Biological Technology Co.,Limited 		58
InvivoChem 		58

View Lastest Price from Golvatinib (E7050) manufacturers

Image Update time Product Price Min. Order Purity Supply Ability Manufacturer
Golvatinib (E7050) pictures 2022-10-14 Golvatinib (E7050)
928037-13-2
 US $0.00-0.00 / KG 1KG 98% 1Ton Henan Aochuang Chemical Co.,Ltd.
1-N'-[2-fluoro-4-[2-[[4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl]amino]pyridin-4-yl]oxyphenyl]-1-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide pictures 2019-12-24 1-N'-[2-fluoro-4-[2-[[4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl]amino]pyridin-4-yl]oxyphenyl]-1-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
928037-13-2
 US $1.00 / KG 1KG Min98% HPLC g/kg/ton Career Henan Chemical Co

Golvatinib (E7050) Spectrum

Golvatinib (E7050)(928037-13-2)1HNMR

928037-13-2(Golvatinib (E7050))Related Search:

N-Methylbenzylamine 2-Methylaminoethanol N-Methyl pyrrole N-Methylbenzamide N-Methylolacrylamide
N-Methyldiethanolamine Capmatinib Alectinib Dasatinib (2S)-1-[3-Ethyl-7-[[(1-oxido-3-pyridinyl)methyl]amino]pyrazolo[1,5-a]pyrimidin-5-yl]-2-piperidineethanol
Afatinib BEZ235 (NVP-BEZ235, Dactolisib)

1of3

N-[2-Fluoro-4-[[2-[[[4-(4-methylpiperazin-1-yl)piperidin-1-yl]carbonyl]amino]pyridin-4-yl]oxy] E-7050N-[2-Fluoro-4-[[2-[[[4-(4-methylpiperazin-1-yl)piperidin-1-yl]carbonyl]amino]pyridin-4-yl]oxy]phenyl]-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide E-7050 N-[2-Fluoro-4-[[2-[[[4-(4-methylpiperazin-1-yl)piperidin-1-yl]carbonyl]amino]pyridin-4-yl]oxy]phenyl]-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide Golvatinib E-7050 (Golvatinib) Golvatinib (E7050) 1,1-Cyclopropanedicarboxamide, N-[2-fluoro-4-[[2-[[[4-(4-methyl-1-piperazinyl)-1-piperidinyl]carbonyl]amino]-4-pyridinyl]oxy]phenyl]-N'-(4-fluorophenyl)- N-[2-Fluoro-4-[[2-[[[4-(4-methylpiperazin-1-yl)piperidin-1-yl]carbonyl]amino]pyridin-4-yl]oxy]phenyl]-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide Golvatinib(E-7050) 1-N'-[2-fluoro-4-[2-[[4-(4-methylpiperazin-1-yl)piperidine-1-carbonyl]amino]pyridin-4-yl]oxyphenyl]-1-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide E-7060;E7050;E 7050 E-7060 CS-575 E7050; E-7050; E 7050; GOLVATINIB. Golvatinib (E7050) USP/EP/BP N-(2-fluoro-4-(2-(4-(4-methylpiperazin-1-yl)piperidine-1-carboxamido)pyridin-4-yloxy)phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide Golvatinib E7050 E-7050 928037-13-2 C33H37F2N7O4 Inhibitors