| product Name | cabozantinib (S)-malate |
|---|---|
| Synonyms | Cabozantinib L-(-)-Apple Acid; N1-[4-[(6,7-dimethoxy-4-quinolyl)oxy]phenyl]-N1′-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide; (2S)-2-hydroxybutanedioic acid; Butanedioic acid, 2-hydroxy-, (2S)-, compd. with N-[4-[(6,7-dimethoxy-4- quinolinyl)oxy]phenyl]-N’-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide (1:1); N-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-N’-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide mono[(2S)-2-hydroxybutanedioate]; (2S)-2-Hydroxybutanedioic acid compd.with N-[4-[(6,7-dimethoxy-4-quinolinyl)oxy]phenyl]-N’-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide(1:1); Cabozantinib Malate; Cabozantinib L-Malate; Cabozantinib S-malate |
| Molecular Formula | C28H24FN3O5.C4H6O5 |
| Molecular Weight | 635.60 |
| InChI | InChI=1S/C28H24FN3O5.C4H6O5/c1-35-24-15-21-22(16-25(24)36-2)30-14-11-23(21)37-20-9-7-19(8-10-20)32-27(34)28(12-13-28)26(33)31-18-5-3-17(29)4-6-18;5-2(4(8)9)1-3(6)7/h3-11,14-16H,12-13H2,1-2H3,(H,31,33)(H,32,34);2,5H,1H2,(H,6,7)(H,8,9)/t;2-/m.0/s1 |
| CAS Registry Number | 1140909-48-3 |
| Molecular Structure | 
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| Description | Cabozantinib S-MALATE，formerly known as XL184, trade name Cabometyx, is developed by Exelixis biopharmaceutical company in the United States. The drug is mainly targeted at MET and VEGFR2 tyrosine kinases that associated with the growth and proliferation of prostate cancer, inhibiting tumor metastasis and angiogenesis. Cabozantinib S-MALATE , the malate of Cabozantinib, is an effective VEGFR2 inhibitor, and IC50 is 0.035 nM. It also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2 and AXL, and IC50 is 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM respectively. Cabozantinib(Cometriq) was granted orphan drug status by the U.S. Food and Drug Administration (FDA) in January 2011. Cabozantinib(Cometriq) is approved by the U.S. FDA for medullary thyroid cancer. and advanced renal cell carcinoma in people who have received prior anti-angiogenic therapy. It is currently undergoing clinical trials for the treatment of prostate, bladder, ovarian, brain, melanoma, breast, non-small cell lung, pancreatic, and hepatocellular cancers. |
| Uses | 1.Cabozantinib is a small molecule C-Met modulator. Cabozantinib acts as a potent multitargeted VEGFR2, Met, FLT3, Tie2, Kit and Ret inhibitor with IC50 of 0.035, 1.8, 14.4, 14.3 and 4.6 nM for VEGFR2, Met, FLT3, Tie2 and Kit, respectively. Cabozantinib shows dose-dependent inhibition of tumor growth and tumor regression, associated with disruption of the tumor vasculature and extensive tumor cell a poptosis. 2.Cabozantinib malate is the malate of Cabozantinib, a potent VEGFR2 inhibitor with IC50 of 0.035 nM and also inhibits c-Met, Ret, Kit, Flt-1/3/4, Tie2, and AXL with IC50 of 1.3 nM, 4 nM, 4.6 nM, 12 nM/11.3 nM/6 nM, 14.3 nM and 7 nM, respectively. |
| Biological Activity | cabozantinib malate is a potent inhibitor of met andvegf receptor2 with ic50 values of 1.3nm and 0.035nm [1].cabozantinib is a pan-tyrosine kinase inhibitor and is developed as an oral treatment of various cancers including mtc, gbm, nsclc, pancreatic carcinoma, breast and colon cancer. the targets of cabozantinib are met, vegfr-2, ret, flt3, kit, axl as well as tek. in cellular assays, cabozantinib inhibits the phosphorylation of met, vegfr2, kit, flt3 and axl with ic50 values of 7.8, 1.9, 5.0, 7.5 and 42μm, respectively [1, 2].as a pan-tyrosine kinase inhibitor, cabozantinib can affect many biological processes. cabozantinib inhibits the tubule formation of hmvec cells with ic50 value of 6.7nm. in b16f10 cells, cabozantinib inhibits hgf-inducedmigration and invasion with ic50 values of 31nm and 9nm, respectively. moreover, cabozantinib shows anti-proliferation efficacy in a variety of tumors such as snu-5, hs746t, mda-mb-231 and u87mg. it is also reported that the combination of cabozantinib and gefitinib can cause potent inhibition of the gefitinib-resistant hcc827gr6 cell line [1, 2]. |
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