MedKoo Biosciences

Golvatinib
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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.

Chemical Structure

Golvatinib

CAS# 928037-13-2

Product data Instruction

Theoretical Analysis

MedKoo Cat#: 201072
Name: Golvatinib
CAS#: 928037-13-2
Chemical Formula: C33H37F2N7O4
Exact Mass: 633.29
Molecular Weight: 633.690
Elemental Analysis: C, 62.55; H, 5.89; F, 6.00; N, 15.47; O, 10.10

Price and Availability

Size	Price	Availability
25mg	USD 195	Ready to ship
50mg	USD 350	Ready to ship
100mg	USD 550	Ready to ship
200mg	USD 950	Ready to ship
500mg	USD 1950	Ready to ship
10mg	USD 90	Ready to ship
Bulk inquiry Welcome, Customer: Please do not inquire quote if your intended use is for a patient since our products are for research use and for chemical synthesis use, not for human use . For in-stock products, we listed price in the web page. You may inquire prices for which sizes were not listed. If no price is listed, this means the product is not in stock at the moment, which may be available via custom synthesis. For cost-effective reason, minimum order of 1g is requested (typically very expensive). The lead time is usually 2-4 months. Quote of less than 1g will not be provided. MedKoo may not offer quote for below reasons: (1) current available synthetic method appears to be extremely expensive which is obviously not affordable to most customers; (2) Key raw material to make the product is temporally not available; (3) DEA controlled substances; (4) the product is under patent protection in customer’s country.

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

Appearance: white solid powder

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

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

Product Data:

Product Data

Instruction:

View handling instruction

Biological target:	Golvatinib (E-7050) is a potent dual inhibitor of both c-Met and VEGFR2 kinases with IC50s of 14 and 16 nM, respectively.
In vitro activity:	The new Met-TKI, E7050, reversed 3 HGF-induced resistance mechanisms in EGFR mutant lung cancer. First, E7050 reversed HGF-induced gefitinib resistance by inhibiting Met phosphorylation and thereby suppressing the downstream PI3K/Akt pathway. Second, E7050 inhibited the HGF-induced resistance to next-generation EGFR-TKIs, irreversible EGFR-TKIs, and mutant-selective EGFR-TKIs. Third, E7050 prevented the emergence of resistant clones induced by continuous exposure to HGF. Reference: Clin Cancer Res. 2012 Mar 15;18(6):1663-71. https://clincancerres.aacrjournals.org/content/18/6/1663.long
In vivo activity:	Daily oral administration of E7050 inhibited the growth of all tumors in a dose-dependent manner (Fig. 2). High doses of E7050 caused drastic tumor regression, with 2/5 Hs746T tumors failing to re-grow after E7050 treatment (50 mg/kg) was terminated for 20 days and 5/5 failing to re-grow after 100 mg/kg E7050 treatment (data not shown). As a result, tumor-bearing mice were cured by treatment with E7050. During the treatment with E7050, no other macroscopic changes or loss of body weight were observed (data not shown). Reference: Cancer Sci. 2010 Jan;101(1):210-5. https://onlinelibrary.wiley.com/doi/full/10.1111/j.1349-7006.2009.01343.x

Solubility Data

	Solvent	Max Conc. mg/mL	Max Conc. mM
Solubility
	DMSO	35.0	55.23

Preparing Stock Solutions

The following data is based on the product molecular weight 633.690000000000000000000000000000 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Concentration / Solvent Volume / Mass	1 mg	5 mg	10 mg
1 mM	1.15 mL	5.76 mL	11.51 mL
5 mM	0.23 mL	1.15 mL	2.3 mL
10 mM	0.12 mL	0.58 mL	1.15 mL
50 mM	0.02 mL	0.12 mL	0.23 mL

Formulation protocol:	1. Wang W, Li Q, Takeuchi S, Yamada T, Koizumi H, Nakamura T, Matsumoto K, Mukaida N, Nishioka Y, Sone S, Nakagawa T, Uenaka T, Yano S. Met kinase inhibitor E7050 reverses three different mechanisms of hepatocyte growth factor-induced tyrosine kinase inhibitor resistance in EGFR mutant lung cancer. Clin Cancer Res. 2012 Mar 15;18(6):1663-71. doi: 10.1158/1078-0432.CCR-11-1171. Epub 2012 Feb 8. PMID: 22317763. 3. Wang W, Li Q, Takeuchi S, Yamada T, Koizumi H, Nakamura T, Matsumoto K, Mukaida N, Nishioka Y, Sone S, Nakagawa T, Uenaka T, Yano S. Met kinase inhibitor E7050 reverses three different mechanisms of hepatocyte growth factor-induced tyrosine kinase inhibitor resistance in EGFR mutant lung cancer. Clin Cancer Res. 2012 Mar 15;18(6):1663-71. doi: 10.1158/1078-0432.CCR-11-1171. Epub 2012 Feb 8. PMID: 22317763. 4. Nakagawa T, Tohyama O, Yamaguchi A, Matsushima T, Takahashi K, Funasaka S, Shirotori S, Asada M, Obaishi H. E7050: a dual c-Met and VEGFR-2 tyrosine kinase inhibitor promotes tumor regression and prolongs survival in mouse xenograft models. Cancer Sci. 2010 Jan;101(1):210-5. doi: 10.1111/j.1349-7006.2009.01343.x. Epub 2009 Sep 2. PMID: 19832844.
In vitro protocol:	1. Wang W, Li Q, Takeuchi S, Yamada T, Koizumi H, Nakamura T, Matsumoto K, Mukaida N, Nishioka Y, Sone S, Nakagawa T, Uenaka T, Yano S. Met kinase inhibitor E7050 reverses three different mechanisms of hepatocyte growth factor-induced tyrosine kinase inhibitor resistance in EGFR mutant lung cancer. Clin Cancer Res. 2012 Mar 15;18(6):1663-71. doi: 10.1158/1078-0432.CCR-11-1171. Epub 2012 Feb 8. PMID: 22317763.
In vivo protocol:	1. Wang W, Li Q, Takeuchi S, Yamada T, Koizumi H, Nakamura T, Matsumoto K, Mukaida N, Nishioka Y, Sone S, Nakagawa T, Uenaka T, Yano S. Met kinase inhibitor E7050 reverses three different mechanisms of hepatocyte growth factor-induced tyrosine kinase inhibitor resistance in EGFR mutant lung cancer. Clin Cancer Res. 2012 Mar 15;18(6):1663-71. doi: 10.1158/1078-0432.CCR-11-1171. Epub 2012 Feb 8. PMID: 22317763. 2. Nakagawa T, Tohyama O, Yamaguchi A, Matsushima T, Takahashi K, Funasaka S, Shirotori S, Asada M, Obaishi H. E7050: a dual c-Met and VEGFR-2 tyrosine kinase inhibitor promotes tumor regression and prolongs survival in mouse xenograft models. Cancer Sci. 2010 Jan;101(1):210-5. doi: 10.1111/j.1349-7006.2009.01343.x. Epub 2009 Sep 2. PMID: 19832844.

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1: Nakagawa T, Takeuchi S, Yamada T, Nanjo S, Ishikawa D, Sano T, Kita K, Nakamura T, Matsumoto K, Suda K, Mitsudomi T, Sekido Y, Uenaka T, Yano S. Combined Therapy with Mutant-Selective EGFR Inhibitor and Met Kinase Inhibitor for Overcoming Erlotinib Resistance in EGFR-Mutant Lung Cancer. Mol Cancer Ther. 2012 Oct;11(10):2149-57. doi: 10.1158/1535-7163.MCT-12-0195. Epub 2012 Jul 25. 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, Yano S. Dual inhibition of Met kinase and angiogenesis to overcome HGF-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 2012 Jul 9. PubMed PMID: 22789825. 3: Wang W, Li Q, Takeuchi S, Yamada T, Koizumi H, Nakamura T, Matsumoto K, Mukaida N, Nishioka Y, Sone S, Nakagawa T, Uenaka T, Yano S. Met kinase inhibitor E7050 reverses three different mechanisms of hepatocyte growth factor-induced tyrosine kinase inhibitor resistance in EGFR mutant lung cancer. Clin Cancer Res. 2012 Mar 15;18(6):1663-71. Epub 2012 Feb 8. PubMed PMID: 22317763. 4: Green DR. 'Tit-for-tat' in cell biology. Nat Rev Mol Cell Biol. 2011 Feb;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 and VEGFR-2 tyrosine kinase inhibitor promotes tumor regression and prolongs survival in mouse xenograft models. Cancer Sci. 2010 Jan;101(1):210-5. Epub 2009 Sep 2. PubMed PMID: 19832844.

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