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  1. General Info
  2. Effects Info
  3. Reference
Drug Details
01. General Information
Name Cabozantinib
PubChem CID 25102847
Molecular Weight 501.5g/mol
Synonyms

Cabozantinib, 849217-68-1, XL184, Cometriq, XL-184, XL 184, BMS-907351, XL-184 free base, BMS 907351, Cabozantinib (XL184, BMS-907351), CHEBI:72317, XL184 cpd, UNII-1C39JW444G, Cabozantinib [USAN], 1C39JW444G, BMS-907351 FREE BASE, N'-[4-[(6,7-DIMETHOXY-4-QUINOLINYL)OXY]PHENYL]-N-(4-FLUOROPHENYL)-1,1-CYCLOPROPANEDICARBOXAMIDE, DTXSID10233968, MFCD20926324, n-(4-((6,7-dimethoxy-4-quinolinyl)oxy)phenyl)-n'-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide, Cabozantinib (USAN), XL-184 (Cabozantinib,BMS907351), Cabometyx (TN), Cometriq (TN), 1-N-[4-(6,7-dimethoxyquinolin-4-yl)oxyphenyl]-1-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, 1,1-CYCLOPROPANEDICARBOXAMIDE, N'-(4-((6,7-DIMETHOXY-4-QUINOLINYL)OXY)PHENYL)-N-(4-FLUOROPHENYL)-, 1,1-CYCLOPROPANEDICARBOXAMIDE, N-(4-((6,7-DIMETHOXY-4-QUINOLINYL)OXY)PHENYL)-N'-(4-FLUOROPHENYL)-, N-[4-[(6,7-Dimethoxy-4-quinolinyl)oxy]phenyl]-N'-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide, N-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, Cabozantinib [USAN:INN], cabozantinibum, Carbozantinib, Cabozantinib; N'-?[4-?[(6,?7-?Dimethoxy-?4-?quinolinyl)?oxy]?phenyl]?-?N-?(4-?fluorophenyl)?-1,?1-cyclopropanedicarbox?amide; N'-[4-[(6,7-Dimethoxy-4-quinolinyl)oxy]phenyl]-N-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide; BMS 907351; N-[4-[(6,7-Dimethoxy-4-quinolinyl)oxy]phenyl]-N'-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide, N-(4-((6,7-dimethoxyquinolin-4-yl)oxy)phenyl)-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, Cabozantinib (free base), CABOZANTINIB [MI], Cabozantinib (XL-184), CABOZANTINIB [INN], CABOZANTINIB [VANDF], CABOZANTINIB [WHO-DD], SCHEMBL360795, GTPL5887, Cabozantinib (BMS-907351), CHEMBL2105717, DTXCID40156459, EX-A075, L01XE26, BCPP000308, HMS3654G06, XL-184 free base (Cabozantinib), BCP02591, 849217-68-1 (free base), BDBM50021574, NSC761068, NSC800066, s1119, AKOS025142112, BCP9000470, CCG-264678, CS-0278, DB08875, NSC-761068, NSC-800066, SB20062, XL-184,Cabozantinib, BMS-907351, NCGC00263164-01, NCGC00263164-14, NCGC00263164-17, AC-25082, AS-16277, HY-13016, N-{4-[(6,7-dimethoxyquinolin-4-yl)oxy]phenyl}-N'-(4-fluorophenyl)cyclopropane-1,1- dicarboxamide, SY097158, DB-023624, FT-0664184, NS00020240, SW218093-3, D10062, AB01565831_02, Q795057, SR-01000941569, J-523016, SR-01000941569-1, BRD-K51544265-001-01-8, XL184 , BMS-907351, 1,1-Cyclopropanedicarboxamide, N'-(4-((6,7-dimethoxy-4-quinolinyl)oxy]phenyl]-N-(4- fluorophenyl)-, cyclopropane-1,1-dicarboxylic acid [4-(6,7-dimethoxy-quinoline-4-yloxy)-phenyl]-amide(4-fluoro-phenyl)-amide, cyclopropane-1,1-dicarboxylic acid[4-(6,7-dimethoxy-quinoline-4-yloxy)-phenyl]-amide (4-fluoro-phenyl)-amide, N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N'-(4 fluorophenyl)cyclopropane-1,1-dicarboxamide, N-(4-{[6,7-bis(methyloxy)quinolin-4-yl]oxy}phenyl)-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, N-[4-[(6,7-Dimethoxyquinolin-4-yl)oxy]phenyl]-N inverted exclamation mark -(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, N1-[4-[(6,7-dimethoxy-4-quinolyl)oxy]phenyl]-N1'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide

Drug Type Small molecule
Formula C₂₈H₂₄FN₃O₅
SMILES COC1=CC2=C(C=CN=C2C=C1OC)OC3=CC=C(C=C3)NC(=O)C4(CC4)C(=O)NC5=CC=C(C=C5)F
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)
InChIKey ONIQOQHATWINJY-UHFFFAOYSA-N
CAS Number 849217-68-1
ChEMBL ID CHEMBL2105717
ChEBI ID CHEBI:72317
TTD ID D0IQ6P
Drug Bank ID DB08875
KEGG ID D10062
Toxicity Organism Test Type Route(Dose)
rat LD50 intraperitoneal(165 mg/kg)
mouse LD50 intraperitoneal(254 mg/kg)
rat LD50 oral(322 mg/kg)
Structure 2D-img
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2D MOL 3D MOL
02. Combinatorial Therapeutic Effect(s)
Synergistic Effect
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Enhancing Drug Efficacy
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Combination Pair ID: 772
Pair Name Honokiol, Cabozantinib
Partner Name Honokiol
Disease Info [ICD-11: 2C90.0] Renal cell carcinoma Investigative
Biological Phenomena Induction-->Oxidative Stress
Gene Regulation Down-regulation Expression BCL2 hsa596
Down-regulation Expression BCL-xL hsa598
Down-regulation Expression NFE2L2 hsa4780
Down-regulation Expression RUBCN hsa9711
Down-regulation Expression SQSTM1 hsa8878
In Vitro Model 786-O Renal cell carcinoma Homo sapiens (Human) CVCL_1051
Caki-1 Clear cell renal cell carcinoma Homo sapiens (Human) CVCL_0234
Caki-2 Papillary renal cell carcinoma Homo sapiens (Human) CVCL_0235
ACHN Papillary renal cell carcinoma Homo sapiens (Human) CVCL_1067
In Vivo Model 786-0 cells were subcutaneously injected into dorsal flank of 8-week-old male athymic nude mice and observed for the formation of tumors. The mice were then divided into four treatment groups (n = 5 mice per group): vehicle, XL-184, HNK, and XL-184 + HNK. Once the palpable tumor growth was observed, mice were treated with XL-184 (15 mg/kg), HNK (2 mg/kg) and XL-14 + HNK every alternate day for three weeks via intraperitoneal injection.
Result Cabozantinib + Honokiol combination can significantly inhibit c-Met-induced and Nrf2-mediated anti-oxidant pathway in renal cancer cells to promote increased oxidative stress and tumor cell death.
Combination Pair ID: 1031
Pair Name Atractylenolide I, Cabozantinib
Partner Name Atractylenolide I
Disease Info [ICD-11: 2C82] Prostate cancer Investigative
Biological Phenomena Induction-->Apoptosis
Gene Regulation Up-regulation Expression BAX hsa581
Down-regulation Expression BCL2 hsa596
Up-regulation Expression CASP3 hsa836
Up-regulation Expression CDH1 hsa999
Up-regulation Expression PARP1 hsa142
Down-regulation Expression VIM hsa7431
In Vitro Model DU145 Prostate carcinoma Homo sapiens (Human) CVCL_0105
PC-3 Prostate carcinoma Homo sapiens (Human) CVCL_0035
Result Silencing Hsp27 inhibits EMT. ATL-1 can inhibit the malignant evolution of prostate cancer cells by inhibiting Hsp27/eIF4E. ATL-1 also enhanced chemosensitization of cabozantinib in prostate cancer.
03. Reference
No. Title Href
1 A novel combination therapy with Cabozantinib and Honokiol effectively inhibits c-Met-Nrf2-induced renal tumor growth through increased oxidative stress. Redox Biol. 2023 Dec;68:102945. doi: 10.1016/j.redox.2023.102945. Click
2 Atractylenolide I inhibits EMT and enhances the antitumor effect of cabozantinib in prostate cancer via targeting Hsp27. Front Oncol. 2023 Jan 6;12:1084884. doi: 10.3389/fonc.2022.1084884. Click
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