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  1. General Info
  2. Effects Info
  3. Reference
Drug Details
01. General Information
Name Apatinib
PubChem CID 11315474
Molecular Weight 397.5g/mol
Synonyms

Apatinib, 811803-05-1, rivoceranib, Apatinib free base, N-(4-(1-Cyanocyclopentyl)phenyl)-2-((pyridin-4-ylmethyl)amino)nicotinamide, Apatinib (free base), YN968D1, N-[4-(1-cyanocyclopentyl)phenyl]-2-(pyridin-4-ylmethylamino)pyridine-3-carboxamide, 5S371K6132, N-(4-(1-cyanocyclopentyl)phenyl)-2-(pyridin-4-ylmethylamino)nicotinamide, 3-Pyridinecarboxamide, N-(4-(1-cyanocyclopentyl)phenyl)-2-((4-pyridinylmethyl)amino)-, UNII-5S371K6132, apatinib (in China), RIVOCERANIB [INN], Rivoceranib (USAN/INN), RIVOCERANIB [USAN], RIVOCERANIB [WHO-DD], GTPL7648, SCHEMBL1814966, CHEMBL3186534, Apatinib free base; YN-968D1, DTXSID601024366, AMY21302, BCP02840, EX-A1794, HY-13342A, MFCD21648511, NSC772886, NSC799333, s5248, AKOS024464453, CCG-268625, DB14765, DS-7455, NSC-772886, NSC-799333, SB16590, N-[4-(1-Cyanocyclopentyl)phenyl]-2-[(4-pyridinylmethyl)amino]-3-pyridinecarboxamide, NCGC00249393-01, NCGC00249393-08, AC-27461, BA175030, DA-35324, CS-0003200, C76598, D11288, AB01274807-01, AB01274807_02, Q27262801, N-[4-(1-Cyanocyclopentyl)phenyl]-2-[(4-pyridinylmethyl)amino]nicotinamide, N-[4-(1-Cyanocyclopentyl)phenyl]-2-[(pyridin-4-ylmethyl)amino]pyridine-3-carboxamide

Drug Type Small molecule
Formula C₂₄H₂₃N₅O
SMILES C1CCC(C1)(C#N)C2=CC=C(C=C2)NC(=O)C3=C(N=CC=C3)NCC4=CC=NC=C4
InChI 1S/C24H23N5O/c25-17-24(11-1-2-12-24)19-5-7-20(8-6-19)29-23(30)21-4-3-13-27-22(21)28-16-18-9-14-26-15-10-18/h3-10,13-15H,1-2,11-12,16H2,(H,27,28)(H,29,30)
InChIKey WPEWQEMJFLWMLV-UHFFFAOYSA-N
CAS Number 811803-05-1
ChEMBL ID CHEMBL3186534
TTD ID D0SZ6E
Drug Bank ID DB14765
KEGG ID D11289
Toxicity Organism Test Type Route(Dose)
Structure 2D-img
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2D MOL 3D MOL
03. Combinatorial Therapeutic Effect(s)
Synergistic Effect
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Enhancing Drug Efficacy
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Combination Pair ID: 215
Pair Name Ginsenoside Rb1, Apatinib
Partner Name Ginsenoside Rb1
Disease Info [ICD-11: 2B6E] Hypopharyngeal carcinoma Investigative
Biological Phenomena Induction-->Immunomodulatory
Gene Regulation Up-regulation Expression CD4 hsa920
Down-regulation Expression CD8A hsa925
Down-regulation Expression HK2 hsa3099
Down-regulation Expression KDR hsa3791
Down-regulation Expression PECAM1 hsa5175
Down-regulation Expression SLC2A4 hsa6517
Down-regulation Expression SOX5 hsa6660
In Vitro Model FaDu Hypopharyngeal squamous cell carcinoma Homo sapiens (Human) CVCL_1218
Rca-B Squamous cell carcinoma Rattus norvegicus (Rat) CVCL_5U48
Result A combination of apatinib and G-Rb1 induced more tumor cell apoptosis and reduced cell proliferation than the individual drug treatment and promote antitumor immunity by enhancing immunomodulatory molecules. Thus, we believe that this study could serve as a valuable platform to assess the synergetic anticancer effects of the herbal as well as synthetic medicines.
Combination Pair ID: 388
Pair Name Curcumin, Apatinib
Partner Name Curcumin
Disease Info [ICD-11: 2C60] Breast cancer Investigative
Biological Phenomena Induction-->Apoptosis
Gene Regulation Up-regulation Expression BAX hsa581
Down-regulation Expression BCL2 hsa596
Up-regulation Expression BIRC5 hsa332
Up-regulation Expression DIABLO hsa56616
In Vitro Model MCF-7 Invasive breast carcinoma of no special type Homo sapiens (Human) CVCL_0031
Result Apa-Cur combination therapy exerts more profound anti-proliferation effects on breast cancer cell than Apatinib or Curcumin monotherapy. However, further studies are required to identify other possible signaling pathways and mechanisms involved in the anticancer effects of Apatinib, Curcumin, and Apa-Cur.
Combination Pair ID: 935
Pair Name Cordycepin, Apatinib
Partner Name Cordycepin
Disease Info [ICD-11: 2C25] Lung cancer Investigative
Biological Phenomena Induction-->Apoptosis
Gene Regulation Down-regulation Phosphorylation AKT1 hsa207
Up-regulation Expression BAX hsa581
Down-regulation Expression BCL2 hsa596
Up-regulation Cleavage CASP3 hsa836
Down-regulation Phosphorylation PIK3CA hsa5290
Down-regulation Expression VEGFA hsa7422
In Vitro Model A-549 Lung adenocarcinoma Homo sapiens (Human) CVCL_0023
PC-9 Lung adenocarcinoma Homo sapiens (Human) CVCL_B260
Result Our findings demonstrated that the combination of cordycepin and apatinib has synergistically anticancer effect on NSCLC cells by down-regulating VEGF/PI3K/Akt signaling pathway. This result indicated that cordycepin and apatinib could be a promising drug combination against NSCLC.
Decreasing Drug Toxicity
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Combination Pair ID: 1014
Pair Name Oleanolic Acid, Apatinib
Partner Name Oleanolic Acid
Disease Info [ICD-11: 2C12] Hepatocellular carcinoma Investigative
Biological Phenomena Induction-->Oxidative Stress
In Vitro Model H22 Hepatocellular carcinoma Mus musculus (Mouse) CVCL_H613
In Vivo Model H22 tumor-burdened mice model was established in vivo.
Result OA can treat apatinib induced liver injury in H22 Tumor-burdened mice by enhancing the suppresssive effect of apatinib on the growth of tumor.
04. Reference
No. Title Href
1 A Synergistic Combination of Oleanolic Acid and Apatinib to Enhance Antitumor Effect on Liver Cancer Cells and Protect against Hepatic Injury. Recent Pat Anticancer Drug Discov. 2024;19(2):199-208. doi: 10.2174/1574892818666230417093208. Click
2 Apatinib and Ginsenoside-Rb1 Synergetically Control the Growth of Hypopharyngeal Carcinoma Cells. Dis Markers. 2022 Jan 13;2022:3833489. doi: 10.1155/2022/3833489. Click
3 Anti-proliferation effects of Apatinib in combination with Curcumin in breast cancer cells. Horm Mol Biol Clin Investig. 2022 Sep 5;44(1):27-32. doi: 10.1515/hmbci-2022-0036. Click
4 Combination of Cordycepin and Apatinib Synergistically Inhibits NSCLC Cells by Down-Regulating VEGF/PI3K/Akt Signaling Pathway. Front Oncol. 2020 Sep 7;10:1732. doi: 10.3389/fonc.2020.01732. Click
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