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主营:抗癌化学试剂和激酶抑制剂
℡ 4000-520-616
℡ 4000-520-616
MedKoo/Golvatinibfeatured/25mg/201072
产品编号:201072
市  场 价:¥3000.00
场      地:美国(厂家直采)
产品分类: 蛋白类>多肽>多肽合成>
联系QQ:1570468124
电话号码:4000-520-616
邮      箱: info@ebiomall.com
美  元  价:$150.00
品      牌: MedKoo
公      司:MedKoo Biosciences, Inc
公司分类:
MedKoo/Golvatinibfeatured/25mg/201072
商品介绍

Golvatinib
featured

WARNING: This product is for research use only, not for human or veterinary use.

MedKoo CAT#:201072

CAS#:928037-13-2

Description:Golvatinib, also known as E7050, is an orally bioavailable dual kinase inhibitor of c-Met (hepatocyte growth factor receptor) and VEGFR-2 (vascular endothelial growth factor receptor-2) tyrosine kinases with potential antineoplastic activity. c-Met/VEGFR kinase inhibitor E7050 binds to and inhibits the activities of both c-Met and VEGFR-2, which may inhibit tumor cell growth and survival of tumor cells that overexpress these receptor tyrosine kinases. c-Met and VEGFR-2 are upregulated in a variety of various tumor cell types and play important roles in tumor cell growth, migration and angiogenesis.

Price and Availability

SizePriceShipping out timeQuantity
25mgUSD 150Same day
50mgUSD 250Same day
100mgUSD 450Same day
200mgUSD 650Same day
500mgUSD 1250Same day
1gUSD 2150Same day
2gUSD 3650Same day
5gUSD 47502 weeks
10gUSD 59502 weeks
Inquire bulk and customized quantity

Pricing updated 2021-01-23.Prices are subject to change without notice.

Golvatinib (or E7050), purity > 98%, is in stock. The same day shipping out after order is received.

Chemical Structure

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Theoretical Analysis

MedKoo Cat#: 201072Name: GolvatinibCAS#: 928037-13-2Chemical Formula: C33H37F2N7O4Exact Mass: 633.28751Molecular Weight: 633.69Elemental Analysis:C, 62.55; H, 5.89; F, 6.00; N, 15.47; O, 10.10

Synonym:E7050; E-7050; E 7050; Golvatinib.

IUPAC/Chemical Name:N-(2-fluoro-4-((2-(4-(4-methylpiperazin-1-yl)piperidine-1-carboxamido)pyridin-4-yl)oxy)phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide

InChi Key:BWEYRDZIIMFBJR-UHFFFAOYSA-N

InChi Code:InChI=1S/C33H37F2N7O4/c1-39-16-18-40(19-17-39)23-9-14-41(15-10-23)32(45)38-29-21-26(8-13-37-29)46-25-6-7-28(27(35)20-25)42(24-4-2-22(34)3-5-24)31(44)33(11-12-33)30(36)43/h2-8,13,20-21,23H,9-12,14-19H2,1H3,(H2,36,43)(H,37,38,45)

SMILES Code:O=C(C1(C(N)=O)CC1)N(C2=CC=C(OC3=CC(NC(N4CCC(N5CCN(C)CC5)CC4)=O)=NC=C3)C=C2F)C6=CC=C(F)C=C6

Technical Data

Appearance:
white solid powder

Purity:
>98% (or refer to the Certificate of Analysis)

Certificate of Analysis:
View CoA: current batch, Lot#SSC21125

QC Data:
View QC data: current batch, Lot#SSC21125

Safety Data Sheet (SDS):
View Safety Data Sheet (SDS)

Shipping Condition:
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.

Storage Condition:
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).

Solubility:
Soluble in DMSO, not in water

Shelf Life:
>2 years if stored properly

Drug Formulation:
This drug may be formulated in DMSO

Stock Solution Storage:
0 - 4 C for short term (days to weeks), or -20 C for long term (months).

HS Tariff Code:
2934.99.9001

Additional Information

E7050 is the first kinase inhibitor with dual action against both c-Met and VEGFR-2. The dual inhibitory activity of E7050 against tumor growth and angiogenesis results in drastic tumor regression and disappearance and also prolongation of lifespan without adverse effects.  E7050 is currently under evaluation in a phase I clinical trial.    ( Cancer Sci . 2010 Jan;101(1):210-5. Epub 2009 Sep 2.).E7050 is the first kinase inhibitor with dual action against both c-Met and VEGFR-2. The dual inhibitory activity of E7050 against tumor growth and angiogenesis results in drastic tumor regression and disappearance and also prolongation of lifespan without adverse effects.  E7050 is currently under evaluation in a phase I clinical trial.    ().      E7050 circumvented 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 prevented the emergence of gefitinib-resistant HCC827 cells induced by continuous exposure to HGF. In the in vivo model, E7050 plus gefitinib resulted in marked regression of tumor growth associated with inhibition of Akt phosphorylation in cancer cells. CONCLUSIONS: A new Met kinase inhibitor, E7050, reverses the three HGF-induced mechanisms of gefitinib resistance, suggesting that E7050 may overcome HGF-induced resistance to gefitinib and next-generation EGFR-TKIs. (source: Clin Cancer Res. 2012 Mar 15;18(6):1663-71. Epub 2012 Feb 8.)E7050 circumvented 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 prevented the emergence of gefitinib-resistant HCC827 cells induced by continuous exposure to HGF. In the in vivo model, E7050 plus gefitinib resulted in marked regression of tumor growth associated with inhibition of Akt phosphorylation in cancer cells. CONCLUSIONS: A new Met kinase inhibitor, E7050, reverses the three HGF-induced mechanisms of gefitinib resistance, suggesting that E7050 may overcome HGF-induced resistance to gefitinib and next-generation EGFR-TKIs. (source:)

References

1: Nakagawa T, Takeuchi S, Yamada T, Nanjo S,Ishikawa D, Sano T, Kita K, Nakamura T, Matsumoto K, Suda K, MitsudomiT, Sekido Y, Uenaka T, Yano S. Combined Therapy with Mutant-SelectiveEGFR Inhibitor and Met Kinase Inhibitor for Overcoming ErlotinibResistance in EGFR-Mutant Lung Cancer. Mol Cancer Ther. 2012Oct;11(10):2149-57. doi: 10.1158/1535-7163.MCT-12-0195. Epub 2012 Jul25. PubMed PMID: 22844075.

2: Takeuchi S, Wang W, Li Q, Yamada T, Kita K, Donev IS, Nakamura T,Matsumoto K, Shimizu E, Nishioka Y, Sone S, Nakagawa T, Uenaka T, YanoS. Dual inhibition of Met kinase and angiogenesis to overcomeHGF-induced EGFR-TKI resistance in EGFR mutant lung cancer. Am J Pathol.2012 Sep;181(3):1034-43. doi: 10.1016/j.ajpath.2012.05.023. Epub 2012Jul 9. PubMed PMID: 22789825.

3: Wang W, Li Q, Takeuchi S, Yamada T, Koizumi H, Nakamura T, MatsumotoK, Mukaida N, Nishioka Y, Sone S, Nakagawa T, Uenaka T, Yano S. Metkinase inhibitor E7050 reverses three different mechanisms of hepatocytegrowth factor-induced tyrosine kinase inhibitor resistance in EGFRmutant lung cancer. Clin Cancer Res. 2012 Mar 15;18(6):1663-71. Epub2012 Feb 8. PubMed PMID: 22317763.

4: Green DR. "Tit-for-tat" in cell biology. Nat Rev Mol Cell Biol. 2011Feb;12(2):73. PubMed PMID: 21252991.

5: Nakagawa T, Tohyama O, Yamaguchi A, Matsushima T, Takahashi K,Funasaka S, Shirotori S, Asada M, Obaishi H. E7050: a dual c-Met andVEGFR-2 tyrosine kinase inhibitor promotes tumor regression and prolongssurvival in mouse xenograft models. Cancer Sci. 2010 Jan;101(1):210-5.Epub 2009 Sep 2. PubMed PMID: 19832844.

品牌介绍
MedKoo,由化学家和药学家陈清奇博士。北卡罗莱纳州的研究三角区(Research Triangle Park, 简称 RTP ),是一家以研发、生产和销售小分子抗癌化合物为主的医药科技公司,该公司的业务范围主要是为全球所有从事抗癌药物研究和开发的制药公司,高校,研究院所,政府相关机构提供与抗癌药物分子相关的产品、试剂和技术服务。
中文名MedKoo中    文美帝药库医药科技公司创立于2008年总部位于美国东海岸
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