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- Hamzehlou S, .et al. Anti-tumor activity of neratinib, a pan-HER inhibitor, in gastric adenocarcinoma cells, Eur J Pharmacol, 2019, Nov 15;863:172705 PMID: 31574259
- Hayato Ogura, .et al. TKI-addicted ROS1-rearranged cells are destined to survival or death by the intensity of ROS1 kinase activity, Sci Rep, 2017, 7: 5519 PMID: 28717217
- Fuse MJ, .et al. Mechanisms of Resistance to NTRK Inhibitors and Therapeutic Strategies in NTRK1-Rearranged Cancers, Mol Cancer Ther, 2017, Oct;16(10):2130-2143 PMID: 28751539
- Ryohei Katayama, .et al. Cabozantinib overcomes crizotinib resistance in ROS1 fusion positive cancer, Clin Cancer Res. , 2015, Jan 1; 21(1): 166–174. PMID: 25351743
Biological Activity
Foretinib (GSK1363089), a multikinase inhibitor of c-Met and VEGFR-2, blocks proliferation, induces Anoikis, and impairs ovarian cancer metastasis.
Targets
| Target | Value |
|---|---|
| Met | IC50: 0.4nM |
| KDR | IC50: 0.86nM |
| Tie-2 | IC50: 1.1nM |
| VEGFR3/FLT4 | IC50: 2.8nM |
| RON | IC50: 3nM |
| FLT3 | IC50: 3.6nM |
| PDGFRα | IC50: 3.6nM |
| Kit | IC50: 6.7nM |
| VEGFR1/FLT1 | IC50: 6.8nM |
| PDGFRβ | IC50: 9.6nM |
| FGFR1 | IC50: 660nM |
| EGFR | IC50: 2.99μM |
| In vitro (25°C) | DMSO | 87 mg/mL (137.51 mM) | |
| Water | Insoluble | ||
| Ethanol | Insoluble | ||
| In vivo | 30% propylene glycol, 5% Tween 80, 65% D5W | 28 mg/mL | |
|
* <1 mg/ml means slightly soluble or insoluble. * Please note that Adooq tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations. |
|||
| Concentration / Solvent Volume / Mass | 1 mg | 5 mg | 10 mg |
|---|---|---|---|
| 0.1 mM | 15.81 mL | 79.03 mL | 158.05 mL |
| 0.5 mM | 3.16 mL | 15.81 mL | 31.61 mL |
| 1 mM | 1.58 mL | 7.9 mL | 15.81 mL |
| 5 mM | 0.32 mL | 1.58 mL | 3.16 mL |
*The above data is based on the productmolecular weight 632.7. Batch specific molecular weights may vary from batch to batch due to solvent of hydration, which will affect the solvent volumes required to prepare stock solutions.
| Catalog Num | A10998 |
|---|---|
| Actions | Inhibitor |
| CAS No. | 849217-64-7 |
| Formula | C34H34F2N4O6 |
| M. Wt | 632.7 |
| Purity | >98% |
| Synonyms | GSK089, EXEL-2880 |
| SMILES | COC1=CC2=C(C=CN=C2C=C1OCCCN3CCOCC3)OC4=C(C=C(C=C4)NC(=O)C5(CC5)C(=O)NC6=CC=C(C=C6)F)F |
| Storage | Store lyophilized at -20ºC, keep desiccated. |
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