Cat. No.: HY-10338

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Foretinib

(Synonyms: XL880; GSK1363089; GSK089; EXEL-2880)

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Foretinib is a multi-target tyrosine kinase inhibitor with IC₅₀s of 0.4 nM and 0.9 nM for Met and KDR.

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Pureté: 99.45%
CAS No.: 849217-64-7
Formule: C₃₄H₃₄F₂N₄O₆
Masse moléculaire:632.65

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Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 1 year , -20°C, 6 months

Foretinib Chemical Structure

CAS No.: 849217-64-7

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Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Activité biologique
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
- Essai clinique
Chemical Information
Publications (17)
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Activité biologique

Description

Foretinib is a multi-target tyrosine kinase inhibitor with IC₅₀s of 0.4 nM and 0.9 nM for Met and KDR.

IC₅₀ & Target^[1]

KDR

0.9 nM (IC₅₀)

c-Met

0.4 nM (IC₅₀)

Flt-1

6.8 nM (IC₅₀)

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Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.08 μM Compound: 1, GSK1363089	Cytotoxicity against c-Met-dependent human A549 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against c-Met-dependent human A549 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23628470]
A549	IC₅₀	0.029 μM Compound: 5, GSK1363089	Cytotoxicity against human A549 cells after 72 hrs by DAPI staining-based fluorescence assay Cytotoxicity against human A549 cells after 72 hrs by DAPI staining-based fluorescence assay	[PMID: 23838381]
A549	IC₅₀	0.17 μM Compound: 5, GSK1363089	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 23838381]
A549	IC₅₀	0.11 μM Compound: 1, GSK1363289	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 24012712]
A549	IC₅₀	0.13 μM Compound: Foretinib	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 24485123]
A549	IC₅₀	0.11 μM Compound: 1	Cytotoxicity against human A549 cells assessed as inhibition of cell growth after 72 hrs by MTT assay Cytotoxicity against human A549 cells assessed as inhibition of cell growth after 72 hrs by MTT assay	[PMID: 24996144]
A549	IC₅₀	0.12 μM Compound: Foretinib	Antiproliferative activity against human A549 cells assessed as inhibition of cell growth after 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell growth after 72 hrs by MTT assay	[PMID: 25282672]
A549	IC₅₀	0.13 μM Compound: Foretinib	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 25438768]
A549	IC₅₀	0.19 μM Compound: 6, XL880	Cytotoxicity against human A549 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay Cytotoxicity against human A549 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay	[PMID: 26169763]
A549	IC₅₀	0.64 μM Compound: Foretinib	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 26810712]
A549	IC₅₀	0.17 μM Compound: 2; XL-880	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 26897090]
A549	IC₅₀	0.49 μM Compound: Foretinib	Cytotoxicity against human A549 cells assessed as reduction in cell growth after 72 hrs by MTT assay Cytotoxicity against human A549 cells assessed as reduction in cell growth after 72 hrs by MTT assay	[PMID: 26923692]
A549	IC₅₀	0.13 μM Compound: Foretinib	Cytotoxicity against human A549 cells assessed as cell growth inhibition after 72 hrs by MTT assay Cytotoxicity against human A549 cells assessed as cell growth inhibition after 72 hrs by MTT assay	[PMID: 26944614]
A549	IC₅₀	0.64 μM Compound: Foretinib	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 26964675]
A549	IC₅₀	0.11 μM Compound: Foretinib	Cytotoxicity against human A549 cells measured after 72 hrs by MTT assay Cytotoxicity against human A549 cells measured after 72 hrs by MTT assay	[PMID: 27155466]
A549	IC₅₀	0.26 μM Compound: Foretinib	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 27187857]
A549	IC₅₀	165 nM Compound: Foretinib	Cytotoxicity against human A549 cells Cytotoxicity against human A549 cells	[PMID: 27187857]
A549	IC₅₀	0.14 μM Compound: 1	Cytotoxicity against c-Met over-expressed human A549 cells assessed as cell growth inhibition after 72 hrs by MTT assay Cytotoxicity against c-Met over-expressed human A549 cells assessed as cell growth inhibition after 72 hrs by MTT assay	[PMID: 27490023]
A549	IC₅₀	0.15 μM Compound: 2	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 28011202]
A549	IC₅₀	0.36 μM Compound: Foretinib	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 28384549]
A549	IC₅₀	0.15 μM Compound: 1; XL880	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 28716639]
A549	IC₅₀	1.74 μM Compound: Foretinib	Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 29107421]
A549	IC₅₀	0.32 μM Compound: Foretinib	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 29197731]
A549	IC₅₀	3.13 μM Compound: Foretinib	Cytotoxicity against human A549 cells after 72 hrs by MTT assay Cytotoxicity against human A549 cells after 72 hrs by MTT assay	[PMID: 29203143]
A549	IC₅₀	0.26 μM Compound: 2	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 29317165]
A549	IC₅₀	0.64 μM Compound: Foretinib	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 29331754]
A549	IC₅₀	0.32 μM Compound: Foretinib	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 30216852]
A549	IC₅₀	≥50 nM Compound: Foretinib	Antiproliferative activity against human A549 cells after 72 hrs by MTT assay Antiproliferative activity against human A549 cells after 72 hrs by MTT assay	[PMID: 30248654]
A549	IC₅₀	2.4 μM Compound: Foretinib	Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31546197]
A549	IC₅₀	1.49 μM Compound: 3	Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31629631]
A549	IC₅₀	0.21 μM Compound: Foretinib	Antiproliferative activity against human A549 cells measured after 72 hrs by MTT assay Antiproliferative activity against human A549 cells measured after 72 hrs by MTT assay	[PMID: 31757525]
A549	IC₅₀	0.48 μM Compound: 4; GSK1363089	Antiproliferative activity against human A549 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against human A549 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 31836443]
A549	IC₅₀	1.05 μM Compound: GSK1363089	Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 32224380]
A549	IC₅₀	0.41 μM Compound: Foretinib	Cytotoxicity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Cytotoxicity against human A549 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 32505087]
A549	IC₅₀	0.91 μM Compound: XL880	Antiproliferative against human A549 cells assessed as reduction in cell viability by MTT assay Antiproliferative against human A549 cells assessed as reduction in cell viability by MTT assay	[PMID: 33045329]
A549	IC₅₀	0.08 μM Compound: Foretinib	Antiproliferative activity against human A549 cells assessed as cell growth inhibition by MTT assay Antiproliferative activity against human A549 cells assessed as cell growth inhibition by MTT assay	[PMID: 35696863]
A549	IC₅₀	520 nM Compound: Foretinib	Antiproliferative activity against human A549 cells measured after 72 hrs by MTT assay Antiproliferative activity against human A549 cells measured after 72 hrs by MTT assay	[PMID: 37875056]
BaF3	IC₅₀	10 nM Compound: Foretinib	Inhibition of ROS1 (unknown origin) expressed in mouse BA/F3 cells Inhibition of ROS1 (unknown origin) expressed in mouse BA/F3 cells	[PMID: 25461320]
BaF3	IC₅₀	11 nM Compound: XL-880	Antiproliferative activity against mouse BaF3 cells harboring CD74-ROS1 assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against mouse BaF3 cells harboring CD74-ROS1 assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay	[PMID: 25733882]
BaF3	IC₅₀	69 nM Compound: XL-880	Antiproliferative activity against mouse BaF3 cells harboring CD74-ROS1 G2032R mutant assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against mouse BaF3 cells harboring CD74-ROS1 G2032R mutant assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay	[PMID: 25733882]
BaF3	IC₅₀	8.6 nM Compound: XL-880	Antiproliferative activity against mouse BaF3 cells harboring CD74-ROS1 L2026M mutant assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against mouse BaF3 cells harboring CD74-ROS1 L2026M mutant assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay	[PMID: 25733882]
BaF3	IC₅₀	0.0092 μM Compound: Foretinib	Antiproliferative activity against mouse BA/F3 cells expressing TPR-Met after 72 hrs by CCK8 assay Antiproliferative activity against mouse BA/F3 cells expressing TPR-Met after 72 hrs by CCK8 assay	[PMID: 27068889]
BaF3	IC₅₀	0.048 μM Compound: Foretinib	Antiprolifertive activity against mouse BaF3 cells expressing TPR-RON assessed as inhibition of cell proliferation measured after 72 hrs by Cell Titer Glo assay Antiprolifertive activity against mouse BaF3 cells expressing TPR-RON assessed as inhibition of cell proliferation measured after 72 hrs by Cell Titer Glo assay	[PMID: 35763868]
BT-474	IC₅₀	<100 nM Compound: 1	Inhibition of AXL in lapatinib-sensitive human BT474 cells Inhibition of AXL in lapatinib-sensitive human BT474 cells	[PMID: 26555154]
EBC-1	IC₅₀	4.8 nM Compound: Foretinib	Antiproliferative activity against human EBC1 cells after 72 hrs by MTT assay Antiproliferative activity against human EBC1 cells after 72 hrs by MTT assay	[PMID: 30248654]
FHC	IC₅₀	3.83 μM Compound: Foretinib	Cytotoxicity against human FHC cells assessed as inhibtion of cell proliferation measured after 72 hrs by MTT assay Cytotoxicity against human FHC cells assessed as inhibtion of cell proliferation measured after 72 hrs by MTT assay	[PMID: 32505087]
HCC78	IC₅₀	19 nM Compound: XL-880	Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 fusion protein assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against human HCC78 cells harboring SLC34A2-ROS1 fusion protein assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay	[PMID: 25733882]
HCC78	IC₅₀	21 nM Compound: XL-880	Antiproliferative activity against human HCC78 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay Antiproliferative activity against human HCC78 cells assessed as reduction in cell viability incubated for 72 hrs by CellTiter-Glo assay	[PMID: 25733882]
HCC827	IC₅₀	0.5 μM Compound: 11	Antiproliferative activity against gefitinib resistant EGFR-mutated human HCC827 cells after 72 hrs by MTT assay Antiproliferative activity against gefitinib resistant EGFR-mutated human HCC827 cells after 72 hrs by MTT assay	[PMID: 28787156]
HCT-116	IC₅₀	520 nM Compound: Foretinib	Antiproliferative activity against human HCT-116 cells measured after 72 hrs by MTT assay Antiproliferative activity against human HCT-116 cells measured after 72 hrs by MTT assay	[PMID: 37875056]
HepG2	IC₅₀	2.88 μM Compound: Foretinib	Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 29107421]
HepG2	IC₅₀	2.27 μM Compound: Foretinib	Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay Cytotoxicity against human HepG2 cells after 72 hrs by MTT assay	[PMID: 29203143]
HepG2	IC₅₀	0.48 μM Compound: Foretinib	Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells after 72 hrs by MTT assay	[PMID: 30216852]
HepG2	IC₅₀	2.4 μM Compound: Foretinib	Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31546197]
HepG2	IC₅₀	0.35 μM Compound: 4; GSK1363089	Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 31836443]
HT-29	IC₅₀	0.15 μM Compound: 1, GSK1363089	Cytotoxicity against c-Met-dependent human HT-29 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against c-Met-dependent human HT-29 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23628470]
HT-29	IC₅₀	0.18 μM Compound: 1	Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 23644189]
HT-29	IC₅₀	0.165 μM Compound: 5, GSK1363089	Cytotoxicity against human HT-29 cells after 72 hrs by DAPI staining-based fluorescence assay Cytotoxicity against human HT-29 cells after 72 hrs by DAPI staining-based fluorescence assay	[PMID: 23838381]
HT-29	IC₅₀	0.26 μM Compound: 5, GSK1363089	Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 23838381]
HT-29	IC₅₀	0.19 μM Compound: 1, GSK1363289	Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 24012712]
HT-29	IC₅₀	0.16 μM Compound: Foretinib	Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 24485123]
HT-29	IC₅₀	0.19 μM Compound: foretinib	Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 24882675]
HT-29	IC₅₀	0.19 μM Compound: 1	Cytotoxicity against human HT-29 cells assessed as inhibition of cell growth after 72 hrs by MTT assay Cytotoxicity against human HT-29 cells assessed as inhibition of cell growth after 72 hrs by MTT assay	[PMID: 24996144]
HT-29	IC₅₀	0.19 μM Compound: Foretinib	Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth after 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells assessed as inhibition of cell growth after 72 hrs by MTT assay	[PMID: 25282672]
HT-29	IC₅₀	0.16 μM Compound: Foretinib	Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 25438768]
HT-29	IC₅₀	0.032 μM Compound: 6, XL880	Cytotoxicity against human HT-29 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay Cytotoxicity against human HT-29 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay	[PMID: 26169763]
HT-29	IC₅₀	0.26 μM Compound: 2; XL-880	Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 26897090]
HT-29	IC₅₀	0.26 μM Compound: Foretinib	Cytotoxicity against human HT-29 cells assessed as reduction in cell growth after 72 hrs by MTT assay Cytotoxicity against human HT-29 cells assessed as reduction in cell growth after 72 hrs by MTT assay	[PMID: 26923692]
HT-29	IC₅₀	0.16 μM Compound: Foretinib	Cytotoxicity against human HT-29 cells assessed as cell growth inhibition after 72 hrs by MTT assay Cytotoxicity against human HT-29 cells assessed as cell growth inhibition after 72 hrs by MTT assay	[PMID: 26944614]
HT-29	IC₅₀	0.19 μM Compound: Foretinib	Cytotoxicity against human HT-29 cells measured after 72 hrs by MTT assay Cytotoxicity against human HT-29 cells measured after 72 hrs by MTT assay	[PMID: 27155466]
HT-29	IC₅₀	0.17 μM Compound: Foretinib	Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 27187857]
HT-29	IC₅₀	29 nM Compound: Foretinib	Cytotoxicity against human HT-29 cells Cytotoxicity against human HT-29 cells	[PMID: 27187857]
HT-29	IC₅₀	0.19 μM Compound: 1	Cytotoxicity against c-Met over-expressed human HT-29 cells assessed as cell growth inhibition after 72 hrs by MTT assay Cytotoxicity against c-Met over-expressed human HT-29 cells assessed as cell growth inhibition after 72 hrs by MTT assay	[PMID: 27490023]
HT-29	IC₅₀	0.25 μM Compound: 2	Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 28011202]
HT-29	IC₅₀	0.25 μM Compound: Foretinib	Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay Cytotoxicity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 28384549]
HT-29	IC₅₀	0.21 μM Compound: 1; XL880	Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 28716639]
HT-29	IC₅₀	0.26 μM Compound: Foretinib	Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 29197731]
HT-29	IC₅₀	0.29 μM Compound: 2	Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells after 72 hrs by MTT assay	[PMID: 29317165]
HT-29	IC₅₀	0.22 μM Compound: Foretinib	Cytotoxicity in human HT-29 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity in human HT-29 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31079967]
HT-29	IC₅₀	1.76 μM Compound: 3	Cytotoxicity against human HT-29 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human HT-29 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31629631]
HT-29	IC₅₀	0.25 μM Compound: Foretinib	Antiproliferative activity against human HT-29 cells measured after 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells measured after 72 hrs by MTT assay	[PMID: 31757525]
HT-29	IC₅₀	0.26 μM Compound: Foretinib	Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 32200199]
HT-29	IC₅₀	0.98 μM Compound: GSK1363089	Cytotoxicity against human HT-29 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human HT-29 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 32224380]
HT-29	IC₅₀	0.46 μM Compound: Foretinib	Cytotoxicity against human HT-29 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Cytotoxicity against human HT-29 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 32505087]
HT-29	IC₅₀	0.15 μM Compound: Foretinib	Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition by MTT assay Antiproliferative activity against human HT-29 cells assessed as cell growth inhibition by MTT assay	[PMID: 35696863]
HUVEC	IC₅₀	16 nM Compound: 8, GSK1363089, XL880	Inhibition of VEGFR2 phosphorylation in HUVEC Inhibition of VEGFR2 phosphorylation in HUVEC	[PMID: 23098265]
HUVEC	IC₅₀	0.017 μM Compound: Foretinib	Antiproliferative activity against recombinant human VEGF-stimulated HUVEC after 120 hrs by CCK8 assay Antiproliferative activity against recombinant human VEGF-stimulated HUVEC after 120 hrs by CCK8 assay	[PMID: 27068889]
HUVEC	IC₅₀	17.8 nM Compound: Foretinib	Cytotoxicity against HUVEC after 96 hrs by MTT assay Cytotoxicity against HUVEC after 96 hrs by MTT assay	[PMID: 30248654]
HUVEC	IC₅₀	0.42 μM Compound: Foretinib	Cytotoxicity against human HUVEC cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Cytotoxicity against human HUVEC cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 32505087]
MCF7	IC₅₀	9.47 μM Compound: Foretinib	Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 26810712]
MCF7	IC₅₀	6.25 μM Compound: Foretinib	Cytotoxicity against human MCF7 cells assessed as reduction in cell growth after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells assessed as reduction in cell growth after 72 hrs by MTT assay	[PMID: 26923692]
MCF7	IC₅₀	9.47 μM Compound: Foretinib	Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 26964675]
MCF7	IC₅₀	3.92 μM Compound: Foretinib	Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 29107421]
MCF7	IC₅₀	2.76 μM Compound: Foretinib	Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay Cytotoxicity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 29203143]
MCF7	IC₅₀	9.47 μM Compound: Foretinib	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 29331754]
MCF7	IC₅₀	0.76 μM Compound: Foretinib	Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells after 72 hrs by MTT assay	[PMID: 30216852]
MCF7	IC₅₀	2.4 μM Compound: Foretinib	Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 31546197]
MCF7	IC₅₀	2 μM Compound: Foretinib	Antiproliferative activity against human MCF7 cells measured after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells measured after 72 hrs by MTT assay	[PMID: 31757525]
MCF7	IC₅₀	0.73 μM Compound: 4; GSK1363089	Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as cell growth inhibition measured after 72 hrs by MTT assay	[PMID: 31836443]
MCF7	IC₅₀	0.56 μM Compound: XL880	Antiproliferative against human MCF-7 cells assessed as reduction in cell viability by MTT assay Antiproliferative against human MCF-7 cells assessed as reduction in cell viability by MTT assay	[PMID: 33045329]
MCF7	IC₅₀	520 nM Compound: Foretinib	Antiproliferative activity against human MCF7 cells measured after 72 hrs by MTT assay Antiproliferative activity against human MCF7 cells measured after 72 hrs by MTT assay	[PMID: 37875056]
MDA-MB-231	IC₅₀	0.54 μM Compound: foretinib	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 24882675]
MDA-MB-231	IC₅₀	0.54 μM Compound: Foretinib	Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells after 72 hrs by MTT assay	[PMID: 27187857]
MDA-MB-231	IC₅₀	0.52 μM Compound: Foretinib	Cytotoxicity in human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity in human MDA-MB-231 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31079967]
MDA-MB-231	IC₅₀	0.65 μM Compound: Foretinib	Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 32200199]
MDA-MB-231	IC₅₀	0.95 μM Compound: Foretinib	Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Cytotoxicity against human MDA-MB-231 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 32505087]
MKN-45	IC₅₀	0.03 μM Compound: 1, GSK1363089	Cytotoxicity against c-Met-dependent human MKN45 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against c-Met-dependent human MKN45 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23628470]
MKN-45	IC₅₀	0.031 μM Compound: 1	Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay	[PMID: 23644189]
MKN-45	IC₅₀	0.008 μM Compound: 5, GSK1363089	Cytotoxicity against human MKN45 cells Cytotoxicity against human MKN45 cells	[PMID: 23838381]
MKN-45	IC₅₀	0.023 μM Compound: 5, GSK1363089	Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay	[PMID: 23838381]
MKN-45	IC₅₀	0.032 μM Compound: 1, GSK1363289	Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay	[PMID: 24012712]
MKN-45	IC₅₀	0.032 μM Compound: Foretinib	Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay	[PMID: 24485123]
MKN-45	IC₅₀	0.032 μM Compound: foretinib	Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay	[PMID: 24882675]
MKN-45	IC₅₀	0.032 μM Compound: 1	Cytotoxicity against human MKN45 cells assessed as inhibition of cell growth after 72 hrs by MTT assay Cytotoxicity against human MKN45 cells assessed as inhibition of cell growth after 72 hrs by MTT assay	[PMID: 24996144]
MKN-45	IC₅₀	0.032 μM Compound: Foretinib	Antiproliferative activity against human MKN45 cells assessed as inhibition of cell growth after 72 hrs by MTT assay Antiproliferative activity against human MKN45 cells assessed as inhibition of cell growth after 72 hrs by MTT assay	[PMID: 25282672]
MKN-45	IC₅₀	0.032 μM Compound: Foretinib	Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay	[PMID: 25438768]
MKN-45	IC₅₀	0.12 μM Compound: 6, XL880	Cytotoxicity against human MKN45 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay Cytotoxicity against human MKN45 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay	[PMID: 26169763]
MKN-45	IC₅₀	0.023 μM Compound: 2; XL-880	Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay	[PMID: 26897090]
MKN-45	IC₅₀	0.032 μM Compound: Foretinib	Cytotoxicity against human MKN45 cells assessed as cell growth inhibition after 72 hrs by MTT assay Cytotoxicity against human MKN45 cells assessed as cell growth inhibition after 72 hrs by MTT assay	[PMID: 26944614]
MKN-45	IC₅₀	0.032 μM Compound: Foretinib	Cytotoxicity against human MKN45 cells measured after 72 hrs by MTT assay Cytotoxicity against human MKN45 cells measured after 72 hrs by MTT assay	[PMID: 27155466]
MKN-45	IC₅₀	0.023 μM Compound: Foretinib	Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay	[PMID: 27187857]
MKN-45	IC₅₀	8 nM Compound: Foretinib	Cytotoxicity against human MKN45 cells Cytotoxicity against human MKN45 cells	[PMID: 27187857]
MKN-45	IC₅₀	0.032 μM Compound: 1	Cytotoxicity against c-Met over-expressed human MKN45 cells assessed as cell growth inhibition after 72 hrs by MTT assay Cytotoxicity against c-Met over-expressed human MKN45 cells assessed as cell growth inhibition after 72 hrs by MTT assay	[PMID: 27490023]
MKN-45	IC₅₀	0.32 μM Compound: 2	Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay Cytotoxicity against human MKN45 cells after 72 hrs by MTT assay	[PMID: 28011202]
MKN-45	IC₅₀	0.03 μM Compound: 1; XL880	Antiproliferative activity against human MKN45 cells after 72 hrs by MTT assay Antiproliferative activity against human MKN45 cells after 72 hrs by MTT assay	[PMID: 28716639]
MKN-45	IC₅₀	2.3 nM Compound: Foretinib	Antiproliferative activity against human MKN45 cells after 72 hrs by MTT assay Antiproliferative activity against human MKN45 cells after 72 hrs by MTT assay	[PMID: 30248654]
MKN-45	IC₅₀	0.041 μM Compound: Foretinib	Cytotoxicity in human MKN45 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity in human MKN45 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31079967]
MKN-45	IC₅₀	0.2 μM Compound: 3	Cytotoxicity against human MKN45 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human MKN45 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31629631]
MKN-45	IC₅₀	0.05 μM Compound: Foretinib	Antiproliferative activity against human MKN-45 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human MKN-45 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 32200199]
MKN-45	IC₅₀	0.064 μM Compound: Foretinib	Cytotoxicity against human MKN-45 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay Cytotoxicity against human MKN-45 cells assessed as inhibition of cell proliferation measured after 72 hrs by MTT assay	[PMID: 32505087]
MKN-45	IC₅₀	0.03 μM Compound: Foretinib	Antiproliferative activity against human MKN-45 cells assessed as cell growth inhibition by MTT assay Antiproliferative activity against human MKN-45 cells assessed as cell growth inhibition by MTT assay	[PMID: 35696863]
NCI-H292	IC₅₀	≥50 nM Compound: Foretinib	Antiproliferative activity against human NCI-H292 cells after 72 hrs by MTT assay Antiproliferative activity against human NCI-H292 cells after 72 hrs by MTT assay	[PMID: 30248654]
NCI-H460	IC₅₀	0.18 μM Compound: 1, GSK1363089	Cytotoxicity against c-Met-independent human H460 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against c-Met-independent human H460 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23628470]
NCI-H460	IC₅₀	0.12 μM Compound: 1	Cytotoxicity against human H460 cells after 72 hrs by MTT assay Cytotoxicity against human H460 cells after 72 hrs by MTT assay	[PMID: 23644189]
NCI-H460	IC₅₀	0.21 μM Compound: 5, GSK1363089	Cytotoxicity against human NCI-H460 cells after 72 hrs by MTT assay Cytotoxicity against human NCI-H460 cells after 72 hrs by MTT assay	[PMID: 23838381]
NCI-H460	IC₅₀	0.21 μM Compound: 1, GSK1363289	Cytotoxicity against human H460 cells after 72 hrs by MTT assay Cytotoxicity against human H460 cells after 72 hrs by MTT assay	[PMID: 24012712]
NCI-H460	IC₅₀	0.19 μM Compound: Foretinib	Cytotoxicity against human H460 cells after 72 hrs by MTT assay Cytotoxicity against human H460 cells after 72 hrs by MTT assay	[PMID: 24485123]
NCI-H460	IC₅₀	0.21 μM Compound: foretinib	Cytotoxicity against human H460 cells after 72 hrs by MTT assay Cytotoxicity against human H460 cells after 72 hrs by MTT assay	[PMID: 24882675]
NCI-H460	IC₅₀	0.21 μM Compound: 1	Cytotoxicity against human H460 cells assessed as inhibition of cell growth after 72 hrs by MTT assay Cytotoxicity against human H460 cells assessed as inhibition of cell growth after 72 hrs by MTT assay	[PMID: 24996144]
NCI-H460	IC₅₀	0.21 μM Compound: Foretinib	Antiproliferative activity against human H460 cells assessed as inhibition of cell growth after 72 hrs by MTT assay Antiproliferative activity against human H460 cells assessed as inhibition of cell growth after 72 hrs by MTT assay	[PMID: 25282672]
NCI-H460	IC₅₀	0.19 μM Compound: Foretinib	Cytotoxicity against human H460 cells after 72 hrs by MTT assay Cytotoxicity against human H460 cells after 72 hrs by MTT assay	[PMID: 25438768]
NCI-H460	IC₅₀	0.21 μM Compound: 6, XL880	Cytotoxicity against human H460 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay Cytotoxicity against human H460 cells assessed as inhibition of cell proliferation after 72 hrs by MTT assay	[PMID: 26169763]
NCI-H460	IC₅₀	0.19 μM Compound: Foretinib	Cytotoxicity against human H460 cells assessed as cell growth inhibition after 72 hrs by MTT assay Cytotoxicity against human H460 cells assessed as cell growth inhibition after 72 hrs by MTT assay	[PMID: 26944614]
NCI-H460	IC₅₀	0.21 μM Compound: Foretinib	Cytotoxicity against human H460 cells measured after 72 hrs by MTT assay Cytotoxicity against human H460 cells measured after 72 hrs by MTT assay	[PMID: 27155466]
NCI-H460	IC₅₀	0.21 μM Compound: 1	Cytotoxicity against c-Met over-expressed human H460 cells assessed as cell growth inhibition after 72 hrs by MTT assay Cytotoxicity against c-Met over-expressed human H460 cells assessed as cell growth inhibition after 72 hrs by MTT assay	[PMID: 27490023]
NCI-H460	IC₅₀	0.29 μM Compound: Foretinib	Cytotoxicity against human H460 cells after 72 hrs by MTT assay Cytotoxicity against human H460 cells after 72 hrs by MTT assay	[PMID: 28384549]
NCI-H460	IC₅₀	0.22 μM Compound: 1; XL880	Antiproliferative activity against human H460 cells after 72 hrs by MTT assay Antiproliferative activity against human H460 cells after 72 hrs by MTT assay	[PMID: 28716639]
NCI-H460	IC₅₀	0.28 μM Compound: Foretinib	Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay	[PMID: 29197731]
NCI-H460	IC₅₀	0.36 μM Compound: 2	Antiproliferative activity against human H460 cells after 72 hrs by MTT assay Antiproliferative activity against human H460 cells after 72 hrs by MTT assay	[PMID: 29317165]
NCI-H460	IC₅₀	39.6 nM Compound: Foretinib	Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay Antiproliferative activity against human NCI-H460 cells after 72 hrs by MTT assay	[PMID: 30248654]
NCI-H460	IC₅₀	0.18 μM Compound: Foretinib	Cytotoxicity in human NCI-H460 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity in human NCI-H460 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31079967]
NCI-H460	IC₅₀	1.14 μM Compound: 3	Cytotoxicity against human H460 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human H460 cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31629631]
NCI-H460	IC₅₀	0.24 μM Compound: Foretinib	Antiproliferative activity against human NCI-H460 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay Antiproliferative activity against human NCI-H460 cells assessed as reduction in cell viability measured after 72 hrs by MTT assay	[PMID: 32200199]
NCI-H460	IC₅₀	0.81 μM Compound: GSK1363089	Cytotoxicity against human H460 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human H460 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 32224380]
NCI-H460	IC₅₀	0.18 μM Compound: Foretinib	Antiproliferative activity against human NCI-H460 cells assessed as cell growth inhibition by MTT assay Antiproliferative activity against human NCI-H460 cells assessed as cell growth inhibition by MTT assay	[PMID: 35696863]
PC-3	IC₅₀	0.39 μM Compound: Foretinib	Cytotoxicity against human PC3 cells after 72 hrs by MTT assay Cytotoxicity against human PC3 cells after 72 hrs by MTT assay	[PMID: 26810712]
PC-3	IC₅₀	0.89 μM Compound: Foretinib	Cytotoxicity against human PC3 cells assessed as reduction in cell growth after 72 hrs by MTT assay Cytotoxicity against human PC3 cells assessed as reduction in cell growth after 72 hrs by MTT assay	[PMID: 26923692]
PC-3	IC₅₀	0.39 μM Compound: Foretinib	Cytotoxicity against human PC3 cells after 72 hrs by MTT assay Cytotoxicity against human PC3 cells after 72 hrs by MTT assay	[PMID: 26964675]
PC-3	IC₅₀	1.48 μM Compound: Foretinib	Cytotoxicity against human PC3 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human PC3 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 29107421]
PC-3	IC₅₀	0.39 μM Compound: Foretinib	Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay Antiproliferative activity against human PC3 cells after 72 hrs by MTT assay	[PMID: 29331754]
PC-3	IC₅₀	0.81 μM Compound: Foretinib	Antiproliferative activity against human PC-3 cells measured after 72 hrs by MTT assay Antiproliferative activity against human PC-3 cells measured after 72 hrs by MTT assay	[PMID: 31757525]
PC-3	IC₅₀	23 nM Compound: 81	Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth Antiproliferative activity against human PC-3 cells assessed as inhibition of cell growth	[PMID: 37262349]
Sf9	IC₅₀	0.4 nM Compound: 13; XL-880	Inhibition of NH2-terminal His-tagged MET kinase domain (1051 to 1348 residues) (unknown origin) expressed in baculovirus infected Sf9 insect cells preincubated for 60 mins followed by (poly(Glu, Tyr) 4:1) substrate addition for 2 to 4 hrs by luciferase-c Inhibition of NH2-terminal His-tagged MET kinase domain (1051 to 1348 residues) (unknown origin) expressed in baculovirus infected Sf9 insect cells preincubated for 60 mins followed by (poly(Glu, Tyr) 4:1) substrate addition for 2 to 4 hrs by luciferase-c	[PMID: 27299736]
SMMC-7721	IC₅₀	0.44 μM Compound: 1, GSK1363089	Cytotoxicity against c-Met-dependent human SMMC7721 cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against c-Met-dependent human SMMC7721 cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23628470]
SMMC-7721	IC₅₀	0.3 μM Compound: 1	Cytotoxicity against human SMMC7721 cells after 72 hrs by MTT assay Cytotoxicity against human SMMC7721 cells after 72 hrs by MTT assay	[PMID: 23644189]
SMMC-7721	IC₅₀	0.32 μM Compound: 5, GSK1363089	Cytotoxicity against human SMMC7721 cells after 72 hrs by MTT assay Cytotoxicity against human SMMC7721 cells after 72 hrs by MTT assay	[PMID: 23838381]
SMMC-7721	IC₅₀	0.44 μM Compound: Foretinib	Antiproliferative activity against human SMMC-7721 cells assessed as cell growth inhibition by MTT assay Antiproliferative activity against human SMMC-7721 cells assessed as cell growth inhibition by MTT assay	[PMID: 35696863]
SNU-5	IC₅₀	8.9 nM Compound: Foretinib	Antiproliferative activity against human SNU5 cells after 72 hrs by MTT assay Antiproliferative activity against human SNU5 cells after 72 hrs by MTT assay	[PMID: 30248654]
U-87MG ATCC	IC₅₀	0.9 μM Compound: 1, GSK1363089	Cytotoxicity against c-Met-dependent human U87MG cells assessed as growth inhibition after 72 hrs by MTT assay Cytotoxicity against c-Met-dependent human U87MG cells assessed as growth inhibition after 72 hrs by MTT assay	[PMID: 23628470]
U-87MG ATCC	IC₅₀	1.04 μM Compound: 1	Cytotoxicity against human U87MG cells after 72 hrs by MTT assay Cytotoxicity against human U87MG cells after 72 hrs by MTT assay	[PMID: 23644189]
U-87MG ATCC	IC₅₀	0.47 μM Compound: 5, GSK1363089	Cytotoxicity against human U87MG cells after 72 hrs by MTT assay Cytotoxicity against human U87MG cells after 72 hrs by MTT assay	[PMID: 23838381]
U-87MG ATCC	IC₅₀	1.08 μM Compound: 1, GSK1363289	Cytotoxicity against human U87MG cells after 72 hrs by MTT assay Cytotoxicity against human U87MG cells after 72 hrs by MTT assay	[PMID: 24012712]
U-87MG ATCC	IC₅₀	1.1 μM Compound: Foretinib	Cytotoxicity against human U87MG cells after 72 hrs by MTT assay Cytotoxicity against human U87MG cells after 72 hrs by MTT assay	[PMID: 24485123]
U-87MG ATCC	IC₅₀	1.08 μM Compound: 1	Cytotoxicity against human U87MG cells assessed as inhibition of cell growth after 72 hrs by MTT assay Cytotoxicity against human U87MG cells assessed as inhibition of cell growth after 72 hrs by MTT assay	[PMID: 24996144]
U-87MG ATCC	IC₅₀	1.02 μM Compound: Foretinib	Antiproliferative activity against human U87MG cells assessed as inhibition of cell growth after 72 hrs by MTT assay Antiproliferative activity against human U87MG cells assessed as inhibition of cell growth after 72 hrs by MTT assay	[PMID: 25282672]
U-87MG ATCC	IC₅₀	0.92 μM Compound: Foretinib	Cytotoxicity against human U87MG cells after 72 hrs by MTT assay Cytotoxicity against human U87MG cells after 72 hrs by MTT assay	[PMID: 25438768]
U-87MG ATCC	IC₅₀	1.1 μM Compound: Foretinib	Cytotoxicity against human U87MG cells assessed as cell growth inhibition after 72 hrs by MTT assay Cytotoxicity against human U87MG cells assessed as cell growth inhibition after 72 hrs by MTT assay	[PMID: 26944614]
U-87MG ATCC	IC₅₀	0.96 μM Compound: Foretinib	Cytotoxicity against human U87MG cells after 72 hrs by MTT assay Cytotoxicity against human U87MG cells after 72 hrs by MTT assay	[PMID: 28384549]
U-87MG ATCC	IC₅₀	0.96 μM Compound: 1; XL880	Antiproliferative activity against human U87MG cells after 72 hrs by MTT assay Antiproliferative activity against human U87MG cells after 72 hrs by MTT assay	[PMID: 28716639]
U-87MG ATCC	IC₅₀	0.91 μM Compound: Foretinib	Antiproliferative activity against human U87MG cells after 72 hrs by MTT assay Antiproliferative activity against human U87MG cells after 72 hrs by MTT assay	[PMID: 29197731]
U-87MG ATCC	IC₅₀	1.35 μM Compound: 2	Antiproliferative activity against human U87MG cells after 72 hrs by MTT assay Antiproliferative activity against human U87MG cells after 72 hrs by MTT assay	[PMID: 29317165]
U-87MG ATCC	IC₅₀	2.17 μM Compound: 3	Cytotoxicity against human U87MG cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay Cytotoxicity against human U87MG cells assessed as reduction in cell viability incubated for 72 hrs by MTT assay	[PMID: 31629631]
U-87MG ATCC	IC₅₀	0.9 μM Compound: Foretinib	Antiproliferative activity against human U-87 MG cells assessed as cell growth inhibition by MTT assay Antiproliferative activity against human U-87 MG cells assessed as cell growth inhibition by MTT assay	[PMID: 35696863]

In Vitro

Foretinib inhibits HGF receptor family tyrosine kinases with IC₅₀ values of 0.4 nM for Met and 3 nM for Ron. Foretinib also inhibits KDR, Flt-1, and Flt-4 with IC₅₀ values of 0.9 nM, 6.8 nM and 2.8 nM, respectively. Foretinib inhibits colony growth of B16F10, A549 and HT29 cells with IC₅₀ of 40 nM, 29 nM and 165 nM, respectively^[1]. A recent study indicates Foretinib affects cell growth differently in gastric cancer cell lines MKN-45 and KATO-III. Foretinib inhibits phosphorylation of MET and downstream signaling molecules in MKN-45 cells, while targets GFGR2 in KATO-III cells^[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

Foretinib (100 mg/kg, p.o.) results in substantial inhibition of phosphorylation of B16F10 tumor Met and ligand (e.g., HGFor VEGF)-induced receptor phosphorylation of Met in liver and Flk-1/KDR in lung, which both persist through 24 hours. Foretinib (30-100 mg/kg, once daily, p.o.) results in reduction in tumor burden. The lung surface tumor burden is reduced by 50% and 58% following treatment with 30 and 100 mg/kg Foretinib, respectively. Foretinib treatment of mice bearing B16F10 solid tumors also results in dose-dependent tumor growth inhibition of 64% and 87% at 30 and 100 mg/kg, respectively. For both studies, administration of Foretinib is well tolerated with no significant body weight loss^[1]. Foretinib is developed to target abnormal signaling of HGF through Met and simultaneously target several receptors tyrosine kinase involved in tumor angiogenesis. Foretinib causes tumor hemorrhage and necrosis in human xenografts within 2 to 4 hours, and maximal tumornecrosis is observed at 96 hours (after five daily doses), resulting in complete regression^[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Essai clinique

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 849217-64-7
Appearance Solid
Masse moléculaire 632.65
Formule C₃₄H₃₄F₂N₄O₆
Color White to light yellow
SMILES

O=C(NC1=CC=C(C(F)=C1)OC2=C3C=C(C(OCCCN4CCOCC4)=CC3=NC=C2)OC)C5(CC5)C(NC6=CC=C(C=C6)F)=O
Synonyms

XL880; GSK1363089; GSK089; EXEL-2880
Livraison

Room temperature in continental US; may vary elsewhere.

Stockage

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	1 year
	-20°C	6 months

Publications (17)

All

Sort by:

Journal Impact Factor

Cancer Discov

TRK xDFG Mutations Trigger a Sensitivity Switch from Type I to II Kinase Inhibitors. [Abstract]

2021 Jan;11(1):126-141. PMID: 33004339
Nat Biomed Eng

TLR7/8-agonist-loaded nanoparticles promote the polarization of tumour-associated macrophages to enhance cancer immunotherapy. [Abstract]

2018 Aug;2(8):578-588. PMID: 31015631
Sci Transl Med

PP2A inhibition is a druggable MEK inhibitor resistance mechanism in KRAS-mutant lung cancer cells. [Abstract]

2018 Jul 18;10(450):eaaq1093. PMID: 30021885
J Exp Clin Cancer Res

Dual inhibition of HERs and PD-1 counteract resistance in KRASG12C-mutant head and neck cancer. [Abstract]

2024 Nov 20;43(1):308. PMID: 39567998
Cell Chem Biol

Quantitative, Wide-Spectrum Kinase Profiling in Live Cells for Assessing the Effect of Cellular ATP on Target Engagement. [Abstract]

2018 Feb 15;25(2):206-214.e11. PMID: 29174542
Clin Transl Med

Responsiveness of different MET tumour alterations to type I and type II MET inhibitors. [Abstract]

2025 May;15(5):e70338. PMID: 40437874
RSC Adv

A simple liquid chromatography-tandem mass spectrometry method to accurately determine the novel third-generation EGFR-TKI naquotinib with its applicability to metabolic stability assessment. [Abstract]

2019 Feb 7;9(9):4862-4869. PMID: 35514667
Cell Rep Methods

RECOVER identifies synergistic drug combinations in vitro through sequential model optimization. [Abstract]

2023 Oct 23;3(10):100599. PMID: 37797618
J Cell Mol Med

Inactivation of CDK12 Enhances Mitochondrial Efficiency to Suppress DNA Damage. [Abstract]

2026 Apr;30(7):e71101. PMID: 41896195
BMC Cancer

2026 May 4;26(1):768. PMID: 42082953
Open Chem

2020 Jun.
Biomed Chromatogr

LC-MS/MS assay for the quantification of foretinib in rat plasma and its application to preclinical pharmacokinetic study. [Abstract]

2020 Aug;34(8):e4862. PMID: 32307722
J Pancreatol

2023 Dec 12.
bioRxiv

Protein-ligand binding kinetics are primarily controlled by the protein, not the ligand. [Abstract]

2026 May 22:2026.05.20.726507. PMID: 42239232
bioRxiv

Ras-Responsive Element Binding Protein 1 regulates survival of Group 3 medulloblastoma. [Abstract]

2025 Jul 21:2025.07.16.665230. PMID: 40777316
J Pers Med

Wnt/β-Catenin-Pathway Alterations and Homologous Recombination Deficiency in Cholangiocarcinoma Cell Lines and Clinical Samples: Towards Specific Vulnerabilities. [Abstract]

2022 Aug 1;12(8):1270. PMID: 36013219
Technical University of Munich

24.01.2018.

Solvant et solubilité

In Vitro:

DMSO : 75 mg/mL (118.55 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.5807 mL

7.9033 mL

15.8065 mL

5 mM

0.3161 mL

1.5807 mL

3.1613 mL

10 mM

0.1581 mL

0.7903 mL

1.5807 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Calculateur de molarité

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Calculateur de dilution

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (3.95 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: ≥ 2.5 mg/mL (3.95 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (3.95 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Protocole

Kinase Assay^[1]

Kinase inhibition is investigated using one of three assay formats: [³³P]phosphoryl transfer, luciferase-coupled chemiluminescence, or AlphaScreen tyrosine kinase technology. IC₅₀s are calculated by nonlinear regression analysis using XLFit.³³P -Phosphoryl Transfer Kinase Assay Reactions are performed in 384-well white, clear bottom, high-binding microtiter plates. Plates are coated with 2 μg/well of protein or peptide substrate in a 50 μL volume of coating buffer contained 40 μg/mL substrate (poly(Glu, Tyr) 4:1, 22.5 mM Na₂CO₃, 27.5 mM NaHCO₃, 50 mM NaCl and 3 mM NaN₃. Coated plates are washed once with 50 μL of assay buffer following overnight incubation at room temperature (RT). Test compounds and enzymes are combined with ³³P-γ-ATP (3.3 μCi/nmol) in a total volume of 20 μL. The reaction mixture is incubated at RT for 2 hours and terminated by aspiration. The microtiter plates are subsequently washed 6 times with 0.05% Tween-PBS buffer (PBST). Scintillation fluid (50 μL/well) is added and incorporated ³³P is measured by liquid scintillation spectrometry using a MicroBeta scintillation counter.Luciferase-Coupled Chemiluminescence Assay Reactions are conducted in 384-well white, medium binding microtiter plates. In a first step enzyme and compound are combined and incubated for 60 minutes; reactions are initiated by addition of ATP and peptide substrate (poly(Glu, Tyr) 4:1) in a final voume of 20 μL, and incubated at RT for 2-4 hours. Following the kinase reaction, a 20 μL aliquot of Kinase Glo is added and luminescence signal is measured using a Victor plate reader. Total ATP consumption is limited to 50%. AlphaScreenTM Tyrosine Kinase Assay Donor beads coated with streptavidin and acceptor beads coated with PY100 anti-phosphotyrosine antibody are used. Biotinylated poly(Glu,Tyr) 4:1 is used as the substrate. Substrate phosphorylation is measured by addition of donor/acceptor beads by luminescence following donor-acceptor bead complex formation. Kinase and test compounds are combined and preincubated for 60 minutes, followed by addition of ATP, and biotinylated poly(Glu, Tyr) in a total volume of 20 μL in 384-well white, medium binding microtiter plates. Reaction mixtures are incubated for 1 hour at room temperature. Reactions are quenched by addition of 10 μL of 15-30 μg/mL AlphaScreen bead suspension containing 75 mM Hepes, pH 7.4, 300 mM NaCl, 120 mM EDTA, 0.3% BSA and 0.03% Tween-20. After 2-16 hours incubation at room temperature plates are read using an AlphaQuest reader.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Assay^[1]

B16F10, A549, and HT29 cells (1.2×10³ per well) are mixed with soft agar and seeded in a 96-well plate containing 10% FBS and EXEL-2880 over a base agar layer. For normoxic conditions, the plates are incubated (37°C) for 12 to 14 days in 21% oxygen, 5% CO₂, and 74% nitrogen, whereas incubation (37°C) under hypoxic conditions is done in a hypoxia chamber in 1% oxygen, 5% CO₂, and 94% nitrogen. The number of colonies is evaluated under each condition following addition of 50% Alamar Blue and fluorescence detection.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Administration^[1]

In vivo target modulation studies are done in naive mice or mice bearing B16F10 tumors. Foretinib or vehicle (0.9% normal saline) is administered at 10 mL/kg via oral gavage. For examination of Met phosphorylation in liver, HGF (10 μg/mouse) is administered i.v. 10 min before harvest. For examination of Flk-1/KDR phosphorylation in lung, VEGF (10 μg/mouse) is administered i.v. 30 min before harvest 0.5 h later. Receptor phosphorylation analysis is determined by immunoblot analysis.

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Pureté et documentation

Select Batch:

Pureté: 99.98%

Assay: 99.98%

ee.: 99.98%

Fiche technique (279 KB)
SDS (396 KB)
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COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Instruction de manipulation (2659 KB)

Références

[1]. Qian F, et al. Inhibition of tumor cell growth, invasion, and metastasis by EXEL-2880 (XL880, GSK1363089), a novel inhibitor of HGF and VEGF receptor tyrosine kinases. Cancer Res, 2009, 69(20), 8009-8016. [Content Brief]

[2]. Kataoka Y, et al. Foretinib (GSK1363089), a multi-kinase inhibitor of MET and VEGFRs, inhibits growth of gastric cancer cell lines by blocking inter-receptor tyrosine kinase networks. Invest New Drugs, 2011. [Content Brief]

[3]. Eder JP, et al. A phase I study of foretinib, a multi-targeted inhibitor of c-Met and vascular endothelial growth factor receptor 2. Clin Cancer Res, 2010, 16(13), 3507-3516. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

Storage method and period of stock solution: -80°C, 1 year; -20°C, 6 months. When stored at -80°C, please use it within 1 year. When stored at -20°C, please use it within 6 months.

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	1.5807 mL	7.9033 mL	15.8065 mL	39.5163 mL
	5 mM	0.3161 mL	1.5807 mL	3.1613 mL	7.9033 mL
	10 mM	0.1581 mL	0.7903 mL	1.5807 mL	3.9516 mL
	15 mM	0.1054 mL	0.5269 mL	1.0538 mL	2.6344 mL
	20 mM	0.0790 mL	0.3952 mL	0.7903 mL	1.9758 mL
	25 mM	0.0632 mL	0.3161 mL	0.6323 mL	1.5807 mL
	30 mM	0.0527 mL	0.2634 mL	0.5269 mL	1.3172 mL
	40 mM	0.0395 mL	0.1976 mL	0.3952 mL	0.9879 mL
	50 mM	0.0316 mL	0.1581 mL	0.3161 mL	0.7903 mL
	60 mM	0.0263 mL	0.1317 mL	0.2634 mL	0.6586 mL
	80 mM	0.0198 mL	0.0988 mL	0.1976 mL	0.4940 mL
	100 mM	0.0158 mL	0.0790 mL	0.1581 mL	0.3952 mL

Foretinib

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Foretinib

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Publications Citing Use of MedChemExpress (MCE) Foretinib

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Solvant et solubilité

Protocole

Pureté et documentation

Références

Help & FAQs

Complete Stock Solution Preparation Table

Foretinib Related Classifications

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