Description In vitro In vivo
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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 100 India 1 United States 15 Global 117
AdooQ BioScience, LLC
Tel
+1 (866) 930-6790
Fax
+1 (866) 333-9607
Email
info@adooq.com
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United States
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2784
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Target molecule Corp.
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857-239-0968
Fax
857-239-8801
Email
service1@targetmol.com
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United States
ProdList
2559
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Musechem
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+1-800-259-7612
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+1-800-259-7612
Email
info@musechem.com
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United States
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4662
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InvivoChem
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+1-708-310-1919 +1-13798911105
Fax
708-557-7486
Email
sales@invivochem.cn
Country
United States
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6393
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Cckinase, Inc.
Tel
+1 (732)236-3202
Email
sales@cckinase.com
Country
United States
ProdList
2738
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58
BOC Sciences
Tel
+1-631-485-4226
Fax
1-631-614-7828
Email
inquiry@bocsci.com
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United States
ProdList
19553
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58
Aladdin Scientific
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+1-833-552-7181
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sales@aladdinsci.com
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United States
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57511
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TargetMol Chemicals Inc.
Tel
+1-781-999-5354
Email
support@targetmol.com
Country
United States
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19973
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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