Details
Stereochemistry | ACHIRAL |
Molecular Formula | C24H23N5O |
Molecular Weight | 397.4723 |
Optical Activity | NONE |
Defined Stereocenters | 0 / 0 |
E/Z Centers | 0 |
Charge | 0 |
SHOW SMILES / InChI
SMILES
O=C(NC1=CC=C(C=C1)C2(CCCC2)C#N)C3=CC=CN=C3NCC4=CC=NC=C4
InChI
InChIKey=WPEWQEMJFLWMLV-UHFFFAOYSA-N
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)
Apatinib is an orally bioavailable, small molecule tyrosine kinase inhibitor that selectively inhibits the vascular endothelial growth factor receptor-2 and used for the treatment of metastatic gastric cancer or gastroesophageal junction cancer that has progressed or relapsed after chemotherapy. To date, second-line ramucirumab and third-line Apatinib are the only anti-angiogenic approaches that have significantly improved the survival of patients with metastatic gastric cancer. Apatinib exhibited potent, highly-selective inhibition of VEGFR-2, c-kit, c-src, and RET tyrosine kinases. The efficacy of Apatinib monotherapy in patients with metastatic gastric cancer or gastroesophageal junction cancer for whom at least two prior chemotherapy regimens had failed was demonstrated in randomized open-label or double-blind phase II trials and a pivotal placebo-controlled phase III trial, all of which were conducted in China. Further clinical experience and long-term pharmacovigilance are required to definitively establish the efficacy and safety profile of Apatinib, including its use in combination with other chemotherapeutic agents.
Approval Year
Targets
Primary Target | Pharmacology | Condition | Potency |
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Target ID: P35968 Gene ID: 3791.0 Gene Symbol: KDR Target Organism: Homo sapiens (Human) Sources: https://www.ncbi.nlm.nih.gov/pubmed/21443688 |
1.0 nM [IC50] |
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Classification Tree | Code System | Code | ||
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NCI_THESAURUS |
C129825
Created by
admin on Sat Dec 16 02:11:04 GMT 2023 , Edited by admin on Sat Dec 16 02:11:04 GMT 2023
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FDA ORPHAN DRUG |
798720
Created by
admin on Sat Dec 16 02:11:04 GMT 2023 , Edited by admin on Sat Dec 16 02:11:04 GMT 2023
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FDA ORPHAN DRUG |
682618
Created by
admin on Sat Dec 16 02:11:04 GMT 2023 , Edited by admin on Sat Dec 16 02:11:04 GMT 2023
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NCI_THESAURUS |
C1742
Created by
admin on Sat Dec 16 02:11:04 GMT 2023 , Edited by admin on Sat Dec 16 02:11:04 GMT 2023
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NCI_THESAURUS |
C1967
Created by
admin on Sat Dec 16 02:11:04 GMT 2023 , Edited by admin on Sat Dec 16 02:11:04 GMT 2023
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Code System | Code | Type | Description | ||
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5211
Created by
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PRIMARY | |||
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DB14765
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FG-23
Created by
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PRIMARY | |||
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10596
Created by
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PRIMARY | |||
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811803-05-1
Created by
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PRIMARY | |||
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SUB183841
Created by
admin on Sat Dec 16 02:11:04 GMT 2023 , Edited by admin on Sat Dec 16 02:11:04 GMT 2023
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PRIMARY | |||
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11315474
Created by
admin on Sat Dec 16 02:11:04 GMT 2023 , Edited by admin on Sat Dec 16 02:11:04 GMT 2023
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PRIMARY | |||
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5S371K6132
Created by
admin on Sat Dec 16 02:11:04 GMT 2023 , Edited by admin on Sat Dec 16 02:11:04 GMT 2023
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PRIMARY | |||
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100000170007
Created by
admin on Sat Dec 16 02:11:04 GMT 2023 , Edited by admin on Sat Dec 16 02:11:04 GMT 2023
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PRIMARY | |||
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DTXSID601024366
Created by
admin on Sat Dec 16 02:11:04 GMT 2023 , Edited by admin on Sat Dec 16 02:11:04 GMT 2023
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PRIMARY | |||
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C152237
Created by
admin on Sat Dec 16 02:11:04 GMT 2023 , Edited by admin on Sat Dec 16 02:11:04 GMT 2023
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PRIMARY |
ACTIVE MOIETY
METABOLITE (PARENT)
METABOLITE (PARENT)
METABOLITE (PARENT)
METABOLITE (PARENT)
METABOLITE (PARENT)
METABOLITE (PARENT)
SALT/SOLVATE (PARENT)