Golvatinib (E7050)

Description In vitro In vivo

Product Name: Golvatinib (E7050)
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
Formula Weight: 633.69
MOL File: 928037-13-2.mol

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Golvatinib (E7050) Property

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

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P264Wash hands thoroughly after handling.

P264Wash skin thouroughly after handling.

P271Use only outdoors or in a well-ventilated area.

P280Wear protective gloves/protective clothing/eye protection/face protection.

P302+P352IF ON SKIN: wash with plenty of soap and water.

P304+P340IF INHALED: Remove victim to fresh air and Keep at rest in a position comfortable for breathing.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

P312Call a POISON CENTER or doctor/physician if you feel unwell.

P321Specific treatment (see … on this label).

P332+P313IF SKIN irritation occurs: Get medical advice/attention.

P337+P313IF eye irritation persists: Get medical advice/attention.

P403+P233Store in a well-ventilated place. Keep container tightly closed.

P405Store locked up.

P501Dispose of contents/container to..…

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N-Bromosuccinimide Price

Cayman Chemical

Product number: 22143
Product name: Golvatinib
Purity: ≥98%
Packaging: 1mg
Price: $81
Updated: 2024/03/01

Cayman Chemical

Product number: 22143
Product name: Golvatinib
Purity: ≥98%
Packaging: 5mg
Price: $258
Updated: 2024/03/01

Cayman Chemical

Product number: 22143
Product name: Golvatinib
Purity: ≥98%
Packaging: 10mg
Price: $396
Updated: 2024/03/01

Cayman Chemical

Product number: 22143
Product name: Golvatinib
Purity: ≥98%
Packaging: 25mg
Price: $790
Updated: 2024/03/01

TRC

Product number: G410700
Product name: Golvatinib
Packaging: 5mg
Price: $225
Updated: 2021/12/16

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Golvatinib (E7050) Chemical Properties,Usage,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

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Golvatinib (E7050) Suppliers

Canada 1 China 105 India 1 United States 16 Global 123

Shanghai Boyle Chemical Co., Ltd.

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View Lastest Price from Golvatinib (E7050) manufacturers

Henan Aochuang Chemical Co.,Ltd.

Product: Golvatinib (E7050) 928037-13-2
Price: US $0.00-0.00/KG
Min. Order: 1KG
Purity: 98%
Supply Ability: 1Ton
Release date: 2022-10-13

Career Henan Chemical Co

Product: 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
Price: US $1.00/KG
Min. Order: 1KG
Purity: Min98% HPLC
Supply Ability: g/kg/ton
Release date: 2019-12-23

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)

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