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Fig. 1 · Structure
Cat. No.
A11396
CAS No.
928037-13-2
Formula
C33H37F2N7O4
Mol. Weight
633.69

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Golvatinib (E-7050)

Cat. No. A11396 CAS 928037-13-2

c-Met/VEGFR-2 inhibitor

E7050 (also known as golvatinib 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.

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Biological Activity

Target & Activity

Target Activity Value
c-Met 14 nM
VEGFR2 16 nM

Cellular Effect

Cell Line Activity Value Description Reference
A549 IC50 6.89 μM Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay [PMID: 32173195]
A549 IC50 7.7 μM Cytotoxicity against human A549 cells after 72 hrs by MTT assay [PMID: 33316412]
EBC-1 IC50 6.2 nM Cytotoxicity against human EBC1 cells assessed as inhibition of tumour growth after 3 days by WST-8 assay [PMID: 26717201]
HeLa IC50 4.14 μM Antiproliferative activity against human HeLa cells assessed as reduction in cell viability after 72 hrs by MTT assay [PMID: 32173195]
HeLa IC50 4.23 μM Cytotoxicity against human HeLa cells after 72 hrs by MTT assay [PMID: 33316412]
HepG2 IC50 65.5 μM Antiproliferative activity against human HepG2 cells after 48 hrs by MTT assay [PMID: 25082515]
Hs746T IC50 23 nM Cytotoxicity against human Hs 746T cells assessed as inhibition of tumour growth after 3 days by WST-8 assay [PMID: 26717201]
HUVEC IC50 > 1000 nM Antiangiogenic activity in HUVEC assessed as inhibition of bFGF induced cell proliferation after 3 days by WST-1 assay [PMID: 26717201]
HUVEC IC50 16 nM Inhibition of VEGFR-2 autophosphorylation in HUVEC after 1 hr by Western blot analysis [PMID: 26717201]
HUVEC IC50 16 nM Inhibition of VEGF induced VEGFR2 phosphorylation in HUVEC preincubated for 1 hr followed by VEGF-stimulation for 5 mins by Western blot analysis [PMID: 27299736]
HUVEC IC50 17 nM Antiangiogenic activity in HUVEC assessed as inhibition of HGF induced cell proliferation after 3 days by WST-1 assay [PMID: 26717201]
HUVEC IC50 84 nM Antiangiogenic activity in HUVEC assessed as inhibition of VEGF induced cell proliferation after 3 days by WST-1 assay [PMID: 26717201]
MCF7 IC50 15.44 μM Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay [PMID: 33316412]
MCF7 IC50 20.61 μM Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay [PMID: 32173195]
MCF7 IC50 49.6 μM Antiproliferative activity against human MCF7 cells after 48 hrs by MTT assay [PMID: 25082515]
MKN-45 IC50 14 nM Inhibition of MET autophosphorylation in human MKN45 cells after 2 hrs by Western blot analysis [PMID: 27299736]
MKN-45 IC50 14 nM Inhibition of c-Met autophosphorylation in human MKN45 cells after 2 hrs by Western blot analysis [PMID: 26717201]
MKN-45 IC50 37 nM Cytotoxicity against human MKN45 cells assessed as inhibition of tumour growth after 3 days by WST-8 assay [PMID: 26717201]
SNU-5 IC50 24 nM Cytotoxicity against human SNU5 cells assessed as inhibition of tumour growth after 3 days by WST-8 assay [PMID: 26717201]

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Specifications

Manufacturer Adooq Bioscience
Actions Inhibitor
CAS Number 928037-13-2
Applications

c-Met/VEGFR-2 inhibitor
Formula C33H37F2N7O4
Molecular Weight 633.69
Synonyms E-7050
SMILES
CN1CCN(CC1)C2CCN(CC2)C(=O)NC3=NC=CC(=C3)OC4=CC(=C(C=C4)NC(=O)C5(CC5)C(=O)NC6=CC=C(C=C6)F)F

Storage & Solubility

In Vitro Solubility

Reported Solubility

SolventReported Solubility
DMSO 18 mg/mL (28.4 mM)
Water Insoluble
Ethanol Insoluble

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

In Vivo Preparation

Concentration
28 mg/mL
Vehicle
30% propylene glycol, 5% Tween 80, 65% D5W

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

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