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
- Molecular Weight:
- 633.69
- MDL Number:
- MFCD22124462
- MOL File:
- 928037-13-2.mol
- MSDS File:
- SDS
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) | GHS07 |
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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 |
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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 |
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
Supplier | Tel | Country | ProdList | Advantage | |
---|---|---|---|---|---|
ATK CHEMICAL COMPANY LIMITED | +undefined-21-51877795 | ivan@atkchemical.com | China | 32760 | 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 +8613203830695 | factory@coreychem.com | China | 29825 | 58 |
Dideu Industries Group Limited | +86-29-89586680 +86-15129568250 | 1026@dideu.com | China | 24330 | 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 | 10522 | 58 |
InvivoChem | +1-708-310-1919 +1-13798911105 | sales@invivochem.cn | United States | 6393 | 58 |
View Lastest Price from Golvatinib (E7050) manufacturers
Image | Update time | Product | Price | Min. Order | Purity | Supply Ability | Manufacturer | |
---|---|---|---|---|---|---|---|---|
2022-10-14 | Golvatinib (E7050)
928037-13-2
|
US $0.00-0.00 / KG | 1KG | 98% | 1Ton | Henan Aochuang Chemical Co.,Ltd. | ||
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)
928037-13-2
- US $0.00-0.00 / KG
- 98%
- 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
928037-13-2
- US $1.00 / KG
- Min98% HPLC
- Career Henan Chemical Co