CAS Number849217-68-1
SynonymsN'-[4-[(6,7-dimethoxy-4-quinolinyl)oxy]phenyl]-N-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide; Cometriq; N-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide; XL 184; N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide; Cabozantinib; BMS-907351; 1-N-[4-(6,7-dimethoxyquinolin-4-yl)oxyphenyl]-1-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide; N-{4-[(6,7-Dimethoxy-4-quinolinyl)oxy]phenyl}-N'-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide; XL-184; XL184
Molecular FormulaC28H24FN3O5
Molecular Weight501.506
Purity98%%
Density1.4±0.1 g/cm3
Boiling Point758.1±60.0 °C at 760 mmHg
| Chemical & Physical Properties | |
|---|---|
| CAS Number | 849217-68-1 |
| Catalog No. | 2A-0171242 |
| Chinese Name | 卡博替尼 |
| Synonyms | N'-[4-[(6,7-dimethoxy-4-quinolinyl)oxy]phenyl]-N-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide; Cometriq; N-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide; XL 184; N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide; Cabozantinib; BMS-907351; 1-N-[4-(6,7-dimethoxyquinolin-4-yl)oxyphenyl]-1-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide; N-{4-[(6,7-Dimethoxy-4-quinolinyl)oxy]phenyl}-N'-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide; XL-184; XL184 |
| Molecular Formula | C28H24FN3O5 |
| Molecular Weight | 501.506 |
| Purity | 98% |
| Density | 1.4±0.1 g/cm3 |
| Boiling Point | 758.1±60.0 °C at 760 mmHg |
| Storage Condition | room temperature, dry |
| Application | Cabozantinib is a potent multi-receptor tyrosine kinase inhibitor with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM for VEGFR2, c-Met, Kit, Axl and Flt3, respectively. |
| HTC | 2933499090 |
| PubChem ID | 103932275 |
| SMILES | COc1cc2nccc(Oc3ccc(NC(=O)C4(C(=O)Nc5ccc(F)cc5)CC4)cc3)c2cc1OC |
| InChI | InChI=1S/C28H24FN3O5/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/h3-11,14-16H,12-13H2,1-2H3,(H,31,33)(H,32,34) |
| InChI Key | ONIQOQHATWINJY-UHFFFAOYSA-N |
| Use of | Cabozantinib is a potent multiple receptor tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively. Properties Name cabozantinib Synonym More Synonyms Cabozantinib (XL184, BMS-907351) Biological Activity Description Cabozantinib is a potent multiple receptor tyrosine kinases inhibitor that inhibits VEGFR2, c-Met, Kit, Axl and Flt3 with IC50s of 0.035, 1.3, 4.6, 7 and 11.3 nM, respectively. Related Catalog Signaling Pathways >> Protein Tyrosine Kinase/RTK >> c-Kit Signaling Pathways >> Protein Tyrosine Kinase/RTK >> c-Met/HGFR Signaling Pathways >> Protein Tyrosine Kinase/RTK >> FLT3 Signaling Pathways >> Protein Tyrosine Kinase/RTK >> TAM Receptor Signaling Pathways >> Protein Tyrosine Kinase/RTK >> VEGFR Research Areas >> Cancer VEGFR2:0.035 nM (IC50) Flt-1:12 nM (IC50) Flt-4:6 nM (IC50) FLT3:11.3 nM (IC50) c-Met:1.3 nM (IC50) c-Kit:4 nM (IC50) Kinase Assay The inhibition profile of Cabozantinib against a broad panel of 270 human kinases is determined using luciferase-coupled chemiluminescence, 33P-phosphoryl transfer, or AlphaScreen technology. Recombinant human full-length, glutathione S-transferase tag, or histidine tag fusion proteins are used, and IC50 values are determined by measuring phosphorylation of peptide substrate poly(Glu, Tyr) at ATP concentrations at or below the Km for each respective kinase. The mechanism of kinase inhibition is evaluated using the AlphaScreen Assay by determining the IC50 values over a range of ATP concentrations[2]. References [1]. You WK, et al. VEGF and c-Met blockade amplify angiogenesis inhibition in pancreatic islet cancer. Cancer Res, 2011, 71(14), 4758-4768. [2]. Yakes FM, et al. Cabozantinib (XL184), a novel MET and VEGFR2 inhibitor, simultaneously suppresses metastasis, angiogenesis, and tumor growth. Mol Cancer Ther, 2011, 10(12), 2298-2308. [3]. Fuse MA, et al. Combination Therapy With c-Met and Src Inhibitors Induces Caspase-Dependent Apoptosis of Merlin-Deficient Schwann Cells and Suppresses Growth of Schwannoma Cells. Mol Cancer Ther. Mol Cancer Ther. 2017 Nov;16(11):2387-2398. Chemical & Physical Properties Molecular Formula C28H24FN3O5 Exact Mass 501.170013 PSA 98.78000 Index of Refraction 1.688 InChIKey ONIQOQHATWINJY-UHFFFAOYSA-N Safety Information HS Code 2933499090 Synthetic Route Trifluoromethan... CAS#:849217-54-5 N-(4-Fluorophen... CAS#:849217-60-3 Cabozantinib (X... CAS#:849217-68-1 4-Fluoroaniline CAS#:371-40-4 Cabozantinib (X... CAS#:849217-68-1 Cyclopropane-1,... CAS#:598-10-7 Cabozantinib (X... CAS#:849217-68-1 Precursor & DownStream Precursor 8 CAS#:849217-54-5 Trifluoromethan... CAS#:849217-60-3 N-(4-Fluorophen... CAS#:371-40-4 4-Fluoroaniline CAS#:598-10-7 Cyclopropane-1,... DownStream 1 CAS#:1140909-48-3 Cabozantinib ma... |
| Tax Rebate | 13.0% |
| Supervision | None. MFN tariff: 6.5%. Ordinary tariff: 20.0% |
| Transport Info | Product name: Summary 2933499090. other compounds containing in the structure a quinoline or isoquinoline ring-system (whether or not hydrogenated), not further fused. VAT:17.0%. Tax rebate rate:13.0%. . MFN tariff:6.5%. General tariff:20.0% |
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