Drug Information

Drug (ID: DG01166) and It's Reported Resistant Information
Name
Axitinib
Synonyms
Axitinib; 319460-85-0; AG-013736; Inlyta; AG 013736; (E)-N-Methyl-2-((3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-yl)thio)benzamide; UNII-C9LVQ0YUXG; AG-13736; AG013736; C9LVQ0YUXG; N-methyl-2-((3-((1E)-2-(pyridin-2-yl)ethenyl)-1H-indazol-6-yl)sulfanyl)benzamide; CHEBI:66910; (E)-N-methyl-2-(3-(2-(pyridin-2-yl)vinyl)-1H-indazol-6-ylthio)benzamide; N-methyl-2-[[3-[(E)-2-pyridin-2-ylethenyl]-1H-indazol-6-yl]sulfanyl]benzamide; MFCD09837898; NSC757441; N-methyl-2-({3-[(E)-2-(pyridin-2-yl)ethenyl]-1H-indazol-6-yl}sulfanyl)benzamide; NSC-757441; NCGC00241108-01; S1005; DSSTox_CID_28975; DSSTox_RID_83240; DSSTox_GSID_49049; Axitinib (AG 013736); C22H18N4OS; N-methyl-2-({3-[(E)-2-(pyridin-2-yl)vinyl]-1H-indazol-6-yl}sulfanyl)benzamide; CAS-319460-85-0; axitinibum; Axitinib [USAN:INN:JAN]; 4agc; Inlyta (TN); AG13736; 4ag8; Axitinib (JAN/USAN); AG-013736;Axitinib; Axitinib,AG-013736; MLS006010164; SCHEMBL172918; GTPL5659; Axitinib, >=98% (HPLC); CHEMBL1289926; DTXSID3049049; N-methyl-2-[[3-[2-(2-pyridinyl)ethenyl]-1H-indazol-6-yl]thio]benzamide; SCHEMBL22930506; BDBM25117; CHEBI:94568; EX-A337; QCR-109; SYN1014; BCPP000372; AOB87786; BCP01371; ZINC3816287; Tox21_113597; NSC799341; AKOS015902898; Tox21_113597_1; AC-1539; BCP9000345; CCG-264772; CS-0116; DB06626; KS-1448; NSC 757441; NSC-799341; Benzamide, N-methyl-2-((3-((E)-2-(2-pyridinyl)ethenyl)-1H-indazol-6-yl)thio)-; NCGC00241108-04; NCGC00241108-06; HY-10065; SMR002530046; AM20090673; SW219464-1; D03218; AB01274739-01; AB01274739_02; 460A850; SR-01000941566; J-502064; Q-200662; Q4830631; SR-01000941566-1; BRD-K29905972-001-01-4; BRD-K29905972-001-02-2; Benzamide, N-methyl-2-((3-((1E)-2-(2-pyridinyl)ethenyl)-1H-indazo)-6-yl)thio)-; Benzamide, N-methyl-2-[[3-[(1E)-2-(2-pyridinyl)ethenyl]-1H-indazol-6-yl]thio]-; N-Methyl-[[3[(1E)-2-(2-pyridinyl)ethenyl]-1H-indazol-6-yl]thio]-benzamide; N-methyl-2-({3-[(E)-2-pyridin-2-ylethenyl]-2H-indazol-6-yl}sulfanyl)benzamide; N-METHYL-2-(3-((E)-2-PYRIDIN-2-YL-VINYL)-1H-INDAZOL-6-YLSULFANYL)-BENZAMIDE
    Click to Show/Hide
Indication
In total 1 Indication(s)
Renal cell carcinoma [ICD-11: 2C90]
Approved
[1]
Structure
Target Vascular endothelial growth factor receptor 2 (KDR) VGFR2_HUMAN [1]
Click to Show/Hide the Molecular Information and External Link(s) of This Drug
Formula
C22H18N4OS
IsoSMILES
CNC(=O)C1=CC=CC=C1SC2=CC3=C(C=C2)C(=NN3)/C=C/C4=CC=CC=N4
InChI
1S/C22H18N4OS/c1-23-22(27)18-7-2-3-8-21(18)28-16-10-11-17-19(25-26-20(17)14-16)12-9-15-6-4-5-13-24-15/h2-14H,1H3,(H,23,27)(H,25,26)/b12-9+
InChIKey
RITAVMQDGBJQJZ-FMIVXFBMSA-N
PubChem CID
6450551
ChEBI ID
CHEBI:66910
TTD Drug ID
D01ZRI
VARIDT ID
DR00035
INTEDE ID
DR0162
DrugBank ID
DB06626
Type(s) of Resistant Mechanism of This Drug
  UAPP: Unusual Activation of Pro-survival Pathway
Drug Resistance Data Categorized by Their Corresponding Diseases
ICD-02: Benign/in-situ/malignant neoplasm
Click to Show/Hide the Resistance Disease of This Class
Solid tumour/cancer [ICD-11: 2A00-2F9Z]
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Drug Sensitivity Data Categorized by Their Corresponding Mechanisms
  Unusual Activation of Pro-survival Pathway (UAPP) Click to Show/Hide
Key Molecule: Tyrosine-protein kinase ABL1 (ABL1) [2]
Sensitive Disease Solid tumour/cancer [ICD-11: 2A00-2F9Z]
 Disease Info 
Molecule Alteration Missense mutation
p.T315I (c.944C>T)
 Molecule Info 
Wild Type Structure Method: X-ray diffraction Resolution: 2.89  Å
PDB: 4XEY
Mutant Type Structure Method: X-ray diffraction Resolution: 2.17  Å
PDB: 5MO4
   Download The Information of Sequence       Download The Structure File   
RMSD: 1.69
TM score: 0.88225
Amino acid change:
T315I
 : Wild Type Structure
 : Mutant Type Structure
  Mutation site(s) have been marked in red
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190
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270
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Click to Show/Hide the Structure
Experimental Note Identified from the Human Clinical Data
In Vitro Model Bone marrow N.A.
Mechanism Description The missense mutation p.T315I (c.944C>T) in gene ABL1 cause the sensitivity of Axitinib by aberration of the drug's therapeutic target
Key Molecule: Mast/stem cell growth factor receptor Kit (KIT) [3]
Sensitive Disease Solid tumour/cancer [ICD-11: 2A00-2F9Z]
 Disease Info 
Molecule Alteration Missense mutation
p.T670I (c.2009C>T)
 Molecule Info 
Wild Type Structure Method: X-ray diffraction Resolution: 2.25  Å
PDB: 6HH1
Mutant Type Structure Method: X-ray diffraction Resolution: 2.40  Å
PDB: 8PQG
   Download The Information of Sequence       Download The Structure File   
RMSD: 1.88
TM score: 0.9084
Amino acid change:
T670I
 : Wild Type Structure
 : Mutant Type Structure
  Mutation site(s) have been marked in red
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770
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G
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N
N
C
C
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I
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A
A
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R
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N
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800
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L
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C
810
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A
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D
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N
820
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830
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E
840
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850
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860
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870
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880
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890
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930
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Click to Show/Hide the Structure
Experimental Note Identified from the Human Clinical Data
In Vitro Model GIST-T1 cells Gastric Homo sapiens (Human) CVCL_4976
Ba/F3 cells Colon Homo sapiens (Human) CVCL_0161
GIST-882 cells Gastric Homo sapiens (Human) CVCL_7044
GIST-5R cells Gastric Homo sapiens (Human) CVCL_A9M9
GIST-48B cells Gastric Homo sapiens (Human) CVCL_M441
In Vivo Model Female BALB/c-nu/nu mouse xenograft model Mus musculus
Experiment for
Molecule Alteration		 Whole transcriptome shotgun sequencing assay
Experiment for
Drug Resistance		 CellTiter-Glo assay; IC50 assay
Key Molecule: Mast/stem cell growth factor receptor Kit (KIT) [3]
Sensitive Disease Solid tumour/cancer [ICD-11: 2A00-2F9Z]
 Disease Info 
Molecule Alteration Missense mutation
p.V559D (c.1676T>A)
 Molecule Info 
Experimental Note Identified from the Human Clinical Data
In Vitro Model GIST-T1 cells Gastric Homo sapiens (Human) CVCL_4976
Ba/F3 cells Colon Homo sapiens (Human) CVCL_0161
GIST-882 cells Gastric Homo sapiens (Human) CVCL_7044
GIST-5R cells Gastric Homo sapiens (Human) CVCL_A9M9
GIST-48B cells Gastric Homo sapiens (Human) CVCL_M441
In Vivo Model Female BALB/c-nu/nu mouse xenograft model Mus musculus
Experiment for
Molecule Alteration		 Whole transcriptome shotgun sequencing assay
Experiment for
Drug Resistance		 CellTiter-Glo assay; IC50 assay
Key Molecule: Mast/stem cell growth factor receptor Kit (KIT) [3]
Sensitive Disease Solid tumour/cancer [ICD-11: 2A00-2F9Z]
 Disease Info 
Molecule Alteration Missense mutation
p.V559A (c.1676T>C)
 Molecule Info 
Experimental Note Identified from the Human Clinical Data
In Vitro Model GIST-T1 cells Gastric Homo sapiens (Human) CVCL_4976
Ba/F3 cells Colon Homo sapiens (Human) CVCL_0161
GIST-882 cells Gastric Homo sapiens (Human) CVCL_7044
GIST-5R cells Gastric Homo sapiens (Human) CVCL_A9M9
GIST-48B cells Gastric Homo sapiens (Human) CVCL_M441
In Vivo Model Female BALB/c-nu/nu mouse xenograft model Mus musculus
Experiment for
Molecule Alteration		 Whole transcriptome shotgun sequencing assay
Experiment for
Drug Resistance		 CellTiter-Glo assay; IC50 assay
Key Molecule: Mast/stem cell growth factor receptor Kit (KIT) [3]
Sensitive Disease Solid tumour/cancer [ICD-11: 2A00-2F9Z]
 Disease Info 
Molecule Alteration Missense mutation
p.V559G (c.1676T>G)
 Molecule Info 
Experimental Note Identified from the Human Clinical Data
In Vitro Model GIST-T1 cells Gastric Homo sapiens (Human) CVCL_4976
Ba/F3 cells Colon Homo sapiens (Human) CVCL_0161
GIST-882 cells Gastric Homo sapiens (Human) CVCL_7044
GIST-5R cells Gastric Homo sapiens (Human) CVCL_A9M9
GIST-48B cells Gastric Homo sapiens (Human) CVCL_M441
In Vivo Model Female BALB/c-nu/nu mouse xenograft model Mus musculus
Experiment for
Molecule Alteration		 Whole transcriptome shotgun sequencing assay
Experiment for
Drug Resistance		 CellTiter-Glo assay; IC50 assay
Key Molecule: Mast/stem cell growth factor receptor Kit (KIT) [3]
Sensitive Disease Solid tumour/cancer [ICD-11: 2A00-2F9Z]
 Disease Info 
Molecule Alteration Missense mutation
p.L576P (c.1727T>C)
 Molecule Info 
Experimental Note Identified from the Human Clinical Data
In Vitro Model GIST-T1 cells Gastric Homo sapiens (Human) CVCL_4976
Ba/F3 cells Colon Homo sapiens (Human) CVCL_0161
GIST-882 cells Gastric Homo sapiens (Human) CVCL_7044
GIST-5R cells Gastric Homo sapiens (Human) CVCL_A9M9
GIST-48B cells Gastric Homo sapiens (Human) CVCL_M441
In Vivo Model Female BALB/c-nu/nu mouse xenograft model Mus musculus
Experiment for
Molecule Alteration		 Whole transcriptome shotgun sequencing assay
Experiment for
Drug Resistance		 CellTiter-Glo assay; IC50 assay
Key Molecule: Mast/stem cell growth factor receptor Kit (KIT) [3]
Sensitive Disease Solid tumour/cancer [ICD-11: 2A00-2F9Z]
 Disease Info 
Molecule Alteration Missense mutation
p.V654A (c.1961T>C)
 Molecule Info 
Experimental Note Identified from the Human Clinical Data
In Vitro Model GIST-T1 cells Gastric Homo sapiens (Human) CVCL_4976
Ba/F3 cells Colon Homo sapiens (Human) CVCL_0161
GIST-882 cells Gastric Homo sapiens (Human) CVCL_7044
GIST-5R cells Gastric Homo sapiens (Human) CVCL_A9M9
GIST-48B cells Gastric Homo sapiens (Human) CVCL_M441
In Vivo Model Female BALB/c-nu/nu mouse xenograft model Mus musculus
Experiment for
Molecule Alteration		 Whole transcriptome shotgun sequencing assay
Experiment for
Drug Resistance		 CellTiter-Glo assay; IC50 assay
Key Molecule: Mast/stem cell growth factor receptor Kit (KIT) [3]
Sensitive Disease Solid tumour/cancer [ICD-11: 2A00-2F9Z]
 Disease Info 
Molecule Alteration Missense mutation
p.A829P (c.2485G>C)
 Molecule Info 
Experimental Note Identified from the Human Clinical Data
In Vitro Model GIST-T1 cells Gastric Homo sapiens (Human) CVCL_4976
Ba/F3 cells Colon Homo sapiens (Human) CVCL_0161
GIST-882 cells Gastric Homo sapiens (Human) CVCL_7044
GIST-5R cells Gastric Homo sapiens (Human) CVCL_A9M9
GIST-48B cells Gastric Homo sapiens (Human) CVCL_M441
In Vivo Model Female BALB/c-nu/nu mouse xenograft model Mus musculus
Experiment for
Molecule Alteration		 Whole transcriptome shotgun sequencing assay
Experiment for
Drug Resistance		 CellTiter-Glo assay; IC50 assay
Gastrointestinal cancer [ICD-11: 2B5B]
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Drug Sensitivity Data Categorized by Their Corresponding Mechanisms
  Unusual Activation of Pro-survival Pathway (UAPP) Click to Show/Hide
Key Molecule: Mast/stem cell growth factor receptor Kit (KIT) [3]
Sensitive Disease Gastrointestinal stromal tumor [ICD-11: 2B5B.0]
 Disease Info 
Molecule Alteration Missense mutation
p.V559D (c.1676T>A)
 Molecule Info 
Experimental Note Identified from the Human Clinical Data
In Vitro Model GIST-T1 cells Gastric Homo sapiens (Human) CVCL_4976
Ba/F3 cells Colon Homo sapiens (Human) CVCL_0161
GIST-882 cells Gastric Homo sapiens (Human) CVCL_7044
GIST-5R cells Gastric Homo sapiens (Human) CVCL_A9M9
GIST-48B cells Gastric Homo sapiens (Human) CVCL_M441
In Vivo Model Female BALB/c-nu/nu mouse xenograft model Mus musculus
Experiment for
Molecule Alteration		 Whole transcriptome shotgun sequencing assay
Experiment for
Drug Resistance		 CellTiter-Glo assay; IC50 assay
Key Molecule: Mast/stem cell growth factor receptor Kit (KIT) [3]
Sensitive Disease Gastrointestinal stromal tumor [ICD-11: 2B5B.0]
 Disease Info 
Molecule Alteration IF-deletion
p.V560_Y578del19 (c.1679_1735del57)
 Molecule Info 
Experimental Note Identified from the Human Clinical Data
In Vitro Model GIST-T1 cells Gastric Homo sapiens (Human) CVCL_4976
Ba/F3 cells Colon Homo sapiens (Human) CVCL_0161
GIST-882 cells Gastric Homo sapiens (Human) CVCL_7044
GIST-5R cells Gastric Homo sapiens (Human) CVCL_A9M9
GIST-48B cells Gastric Homo sapiens (Human) CVCL_M441
In Vivo Model Female BALB/c-nu/nu mouse xenograft model Mus musculus
Experiment for
Molecule Alteration		 Whole transcriptome shotgun sequencing assay
Experiment for
Drug Resistance		 CellTiter-Glo assay; IC50 assay
Key Molecule: Mast/stem cell growth factor receptor Kit (KIT) [3]
Sensitive Disease Gastrointestinal stromal tumor [ICD-11: 2B5B.0]
 Disease Info 
Molecule Alteration Missense mutation
p.K642E (c.1924A>G)
 Molecule Info 
Experimental Note Identified from the Human Clinical Data
In Vitro Model GIST-T1 cells Gastric Homo sapiens (Human) CVCL_4976
Ba/F3 cells Colon Homo sapiens (Human) CVCL_0161
GIST-882 cells Gastric Homo sapiens (Human) CVCL_7044
GIST-5R cells Gastric Homo sapiens (Human) CVCL_A9M9
GIST-48B cells Gastric Homo sapiens (Human) CVCL_M441
In Vivo Model Female BALB/c-nu/nu mouse xenograft model Mus musculus
Experiment for
Molecule Alteration		 Whole transcriptome shotgun sequencing assay
Experiment for
Drug Resistance		 CellTiter-Glo assay; IC50 assay
References
Ref 1 Axitinib Reverses Resistance to Anti-Programmed Cell Death-1 Therapy in a Patient With Renal Cell Carcinoma .Front Immunol. 2021 Oct 26;12:728750. doi: 10.3389/fimmu.2021.728750. eCollection 2021. 10.3389/fimmu.2021.728750
Ref 2 Axitinib effectively inhibits BCR-ABL1(T315I) with a distinct binding conformationNature. 2015 Mar 5;519(7541):102-5. doi: 10.1038/nature14119. Epub 2015 Feb 9.
Ref 3 Axitinib overcomes multiple imatinib resistant cKIT mutations including the gatekeeper mutation T670I in gastrointestinal stromal tumorsTher Adv Med Oncol. 2019 May 17;11:1758835919849757. doi: 10.1177/1758835919849757. eCollection 2019.

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