XL880
N1'-[3-fluoro-4-[[6-methoxy-7-(3-morpholinopropoxy)-4-quinolyl]oxy]phenyl]-N1-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
CAS: 849217-64-7
Molecular Formula: C34H34F2N4O6
XL880 - Names and Identifiers
| Name | N1'-[3-fluoro-4-[[6-methoxy-7-(3-morpholinopropoxy)-4-quinolyl]oxy]phenyl]-N1-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide |
| Synonyms | XL880 Foretinib EXEL-2880 GSK 1363089 XL-880,Foretinib XL880(GSK1363089) N1'-[3-fluoro-4-[[6-methoxy-7-(3-morpholinopropoxy)-4-quinolyl]oxy]phenyl]-N1-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide N-[3-Fluoro-4-[[6-methoxy-7-[3-(4-morpholinyl)propoxy]-4-quinolinyl]oxy]phenyl]-N'-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide N-[3-Fluoro-4-[[6-(methyloxy)-7-[[3-(morpholin-4-yl)propyl]oxy]quinolin-4-yl]oxy]phenyl]-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide |
| CAS | 849217-64-7 |
| InChI | InChI=1/C34H34F2N4O6/c1-43-30-20-25-27(21-31(30)45-16-2-13-40-14-17-44-18-15-40)37-12-9-28(25)46-29-8-7-24(19-26(29)36)39-33(42)34(10-11-34)32(41)38-23-5-3-22(35)4-6-23/h3-9,12,19-21H,2,10-11,13-18H2,1H3,(H,38,41)(H,39,42) |
XL880 - Physico-chemical Properties
| Molecular Formula | C34H34F2N4O6 |
| Molar Mass | 632.65 |
| Density | 1.372 |
| Melting Point | >98°C (dec.) |
| Boling Point | 828.5±65.0 °C(Predicted) |
| Flash Point | 454.846°C |
| Solubility | DMSO ≥122mg/mL Water <1.2mg/mL Ethanol ≥10mg/mL |
| Vapor Presure | 0mmHg at 25°C |
| Appearance | Yellow powder. |
| Color | Pale Yellow to Yellow |
| pKa | 13.14±0.70(Predicted) |
| Storage Condition | Sealed in dry,Store in freezer, under -20°C |
| Refractive Index | 1.649 |
| Use | An ATP-competitive inhibitor of tyrosine kinases including Flt-1, Flt-4, Met, and Ron. |
| In vitro study | XL880 inhibits HGF receptor family tyrosine kinases with IC50 values of 0.4 nM and 3 nM for Met and Ron, respectively. 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 inhibited the growth of B16F10,A549 and HT29 cell colonies with IC50 of 40 nM,29 nM and 165 nM, respectively. A recent study showed that XL880 differentially affects cell growth in gastric cancer cell lines MKN-45 and KATO-III. XL880 inhibits phosphorylation of MET and downstream signaling molecules in MKN-45 cells, while targeting GFGR2 in KATO-III cells. |
| In vivo study | XL880(100 mg/kg, single dose, oral intensive feeding) largely inhibits phosphorylation of B16F10 tumor Met and ligands (e. G., HGFor VEGF) induction of Met in the liver and Flk-1/KDR receptor phosphorylation in the lung, both of which can be sustained for 24 hours. XL880 (30-100 mg/kg, once daily, oral intensive feeding) treatment resulted in a reduction in tumor burden. Treatment with 30 and 100 mg/kg XL880 reduced lung surface tumor burden by 50% and 58%, respectively. XL880 treatment of mice bearing B16F10 solid tumors also resulted in dose-dependent tumor growth inhibition, with 30 and 100 mg/kg resulting in 64% and 87% inhibition, respectively. For both studies, XL880 administration was well tolerated and there was no significant weight loss. XL880 can further target the abnormal signal of HGF through Met, and simultaneously target several receptor tyrosine kinases involved in tumor angiogenesis. XL880 caused hemorrhagic tumor necrosis in human xenografts 2 to 4 hours after administration, with maximum tumor necrosis observed at 96 hours (5 days after administration), resulting in complete tumor regression. |
XL880 - Introduction
Foretinib (GSK1363089) is an ATP competitive HGFR and VEGFR inhibitor, which has the strongest effect on Met and KDR. IC50 is 0.4 nM and 0.9 nM respectively. It has slightly weaker effect on Ron, Flt-1/3/4, Kit, PDGFRα/β and Tie-2, and has almost no inhibitory activity on FGFR1 and EGFR.
Last Update：2022-10-16 17:29:20
XL880 - Reference Information
| biological activity | Foretinib (GSK1363089) is an ATP-competitive inhibitor of HGFR and VEGFR, the effects on Met and KDR were the strongest, with IC50 of 0.4 nM and 0.9 nM respectively, and the effects on Ron, Flt-1/4, Kit, PDGFRα/β and Tie-2 were slightly weaker, there was little inhibitory activity against FGFR1 and EGFR. Phase 2. Foretinib (GSK1363089, EXEL-2880, XL-880, GSK089) is an ATP competitive inhibitor of HGFR and VEGFR, with the strongest effect on Met (c-Met) and KDR, the IC50 values in the cell-free assay were 0.4 nM and 0.9 nM, respectively. The effect on Ron, Flt-1/3/4, Kit (c-Kit), PDGFRα/β and Tie-2 was slightly weak, and there was almost no inhibitory activity on FGFR1 and EGFR. Phase 2. |
| Target | Value |
| Met (Cell-free assay) | 0.4 nM |
| KDR (Cell-free assay) | 0.86 nM |
| Tie-2 (Cell-free assay) | 1.1 nM |
| VEGFR3/FLT4 (Cell-free assay) | 2.8 nM |
| RON (Cell-free assay) | 3 nM |
Last Update：2024-04-09 21:01:54
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Product Name: N-(3-Fluoro-4-((6-methoxy-7-(3-morpholinopropoxy)quinolin-4-yl)-oxy)phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide Visit Supplier Webpage Request for quotationCAS: 849217-64-7
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Mobile: +86-18621343501
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Multiple SpecificationsSpot supply
Product Name: XL880; GSK1363089; GSK089; EXEL-2880 Visit Supplier Webpage Request for quotationCAS: 849217-64-7
Tel: 609-228-6898
Email: sales@medchemexpress.com
tech@medchemexpress.com
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