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Signaling Pathway

Foretinib

HY-10338

(XL880; GSK1363089; GSK089; EXEL-2880)

Foretinib

Foretinib Chemical Structure

Foretinib (GSK1363089; XL880; EXEL-2880; GSK089) is an ATP-competitive inhibitor of HGFR and VEGFR, mostly for Met and KDR with IC50 of 0.4 nM and 0.9 nM. Less potent against Ron, Flt-1/3/4, Kit, PDGFRα/β and Tie-2, and little activity to FGFR1 and EGFR.

Size Price Stock Quantity
10 mM * 1 mL in DMSO $66 In-stock
10 mg $60 In-stock
50 mg $220 In-stock
100 mg $365 In-stock
200 mg Get quote
500 mg Get quote
Size Price Stock Quantity
10 mM * 1 mL in DMSO €65 In-stock
10 mg €59 In-stock
50 mg €216 In-stock
100 mg €358 In-stock
200 mg Get quote
500 mg Get quote

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Product name: Foretinib
Cat. No.: HY-10338

Foretinib Data Sheet

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    Purity: 99.45%

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Biological Activity of Foretinib

Foretinib (GSK1363089; XL880; EXEL-2880; GSK089) is an ATP-competitive inhibitor of HGFR and VEGFR, mostly for Met and KDR with IC50 of 0.4 nM and 0.9 nM. Less potent against Ron, Flt-1/3/4, Kit, PDGFRα/β and Tie-2, and little activity to FGFR1 and EGFR.
IC50 value: 0.4 nM/0.9 nM (Met/KDR) [1]
Target:
in vitro: XL880 inhibits HGF receptor family tyrosine kinases with IC50 values of 0.4 nM for Met and 3 nM for Ron. XL880 also inhibits KDR, Flt-1, and Flt-4 with IC50 values of 0.9 nM, 6.8 nM and 2.8 nM, respectively. XL880 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 XL880 affects cell growth differently in gastric cancer cell lines MKN-45 and KATO-III. XL880 inhibits phosphorylation of MET and downstream signaling molecules in MKN-45 cells, while targets GFGR2 in KATO-III cells [2].
in vivo: A single 100 mg/kg oral gavage dose of XL880 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 persisted through 24 hours. Treatment with XL880 (30-100 mg/kg, once daily, oral gavage) 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 XL880, respectively. XL880 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 XL880 is well tolerated with no significant body weight loss [1]. XL880 is developed to target abnormal signaling of HGF through Met and simultaneously target several receptors tyrosine kinase involved in tumor angiogenesis. XL880 caused 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].

Protocol (Extracted from published papers and Only for reference)

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Chemical Information

M.Wt 632.65 Storage Please store the product under the recommended conditions in the Certificate of Analysis.
Formula C34H34F2N4O6
CAS No 849217-64-7
Solvent & Solubility

DMSO ≥122mg/mL Water <1.2mg/mL Ethanol ≥10mg/mL

Preparing Stock Solutions

1 mg 5 mg 10 mg
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

Clinical Information of Foretinib

Product Name Sponsor Only Condition Start Date End Date Phase Last Change Date
Foretinib NCIC Clinical Trials Group Metastatic breast cancer 30-JUN-10 30-APR-13 Phase 2 13-AUG-13
GlaxoSmithKline plc Renal cell carcinoma 30-JUN-06 31-JUL-12 Phase 2 08-NOV-13
NCIC Clinical Trials Group Metastatic breast cancer 31-MAY-10 31-JAN-16 Phase 2 12-AUG-13
GlaxoSmithKline plc Head and neck tumor 31-AUG-07 31-MAY-09 Phase 2 22-MAR-13
GlaxoSmithKline plc Squamous cell carcinoma 31-AUG-07 31-MAY-09 Phase 2 22-MAR-13

References on Foretinib

Inhibitor Kit

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