Foretinib (GSK1363089, XL880)

Catalog No. A10998

Foretinib (GSK1363089,XL880)是c-Met和VEGFR-2的多激酶抑制剂，可抑制增殖，诱导Anoikis并损害卵巢癌转移。

Product Citations

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

Technical details

Catalog Num	A10998
M. Wt	632.7
Formula	C34H34F2N4O6
Purity	>98%
Storage	at -20°C 3 years Powder
CAS No.	849217-64-7
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

Biological Activity

Foretinib (GSK1363089,XL880)是c-Met和VEGFR-2的多激酶抑制剂，可抑制增殖，诱导Anoikis并损害卵巢癌转移。

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

Solubility *

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.

Preparing Stock Solutions

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.