Drug Information

Drug (ID: DG00331) and It's Reported Resistant Information
Name
Dovitinib lactate
Synonyms
Dovitinib; 405169-16-6; CHIR-258; TKI-258; Chir 258; 4-Amino-5-fluoro-3-[5-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]quinolin-2(1H)-one; CHIR258; Dovitinib (TKI-258, CHIR-258); UNII-I35H55G906; CHEMBL522892; 804551-71-1; I35H55G906; TKI 258; 1027263-12-2; (3Z)-4-Amino-5-fluoro-3-[5-(4-methyl-1-piperazinyl)-1,3-dihydro-2H-benzimidazol-2-ylidene]-2(3H)-quinolinone; C21H21FN6O; 4-Amino-5-fluoro-3-(5-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl)quinolin-2(1H)-one
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Indication
In total 3 Indication(s)
Renal cell carcinoma [ICD-11: 2C90]
Phase 3
[1]
Breast cancer [ICD-11: 2C60]
Phase 2
[1]
Endometrial cancer [ICD-11: 2C76]
Phase 2
[1]
Structure
Target Fibroblast growth factor receptor 3 (FGFR3) FGFR3_HUMAN [1]
Platelet-derived growth factor receptor (PDGFR) NOUNIPROTAC [1]
Click to Show/Hide the Molecular Information and External Link(s) of This Drug
Formula
C24H29FN6O5
IsoSMILES
CC(C(=O)O)O.CN1CCN(CC1)C2=CC3=C(C=C2)N=C(N3)C4=C(C5=C(C=CC=C5F)NC4=O)N.O
InChI
1S/C21H21FN6O.C3H6O3.H2O/c1-27-7-9-28(10-8-27)12-5-6-14-16(11-12)25-20(24-14)18-19(23)17-13(22)3-2-4-15(17)26-21(18)29;1-2(4)3(5)6;/h2-6,11H,7-10H2,1H3,(H,24,25)(H3,23,26,29);2,4H,1H3,(H,5,6);1H2
InChIKey
QDPVYZNVVQQULH-UHFFFAOYSA-N
PubChem CID
135611162
TTD Drug ID
D07OZR
INTEDE ID
DR1815
DrugBank ID
DB05928
Type(s) of Resistant Mechanism of This Drug
  EADR: Epigenetic Alteration of DNA, RNA or Protein
  UAPP: Unusual Activation of Pro-survival Pathway
Drug Resistance Data Categorized by Their Corresponding Diseases
ICD-02: Benign/in-situ/malignant neoplasm
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Kidney cancer [ICD-11: 2C90]
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Drug Sensitivity Data Categorized by Their Corresponding Mechanisms
       Epigenetic Alteration of DNA, RNA or Protein (EADR) Click to Show/Hide
Key Molecule: hsa-mir-21 [1]
Molecule Alteration Expression
Down-regulation
 Molecule Info 
Sensitive Disease Renal carcinoma [ICD-11: 2C90.2]
 Disease Info 
Experimental Note Revealed Based on the Cell Line Data
Cell Pathway Regulation PI3K/AKT signaling pathway Inhibition hsa04151
In Vitro Model 786-O cells Kidney Homo sapiens (Human) CVCL_1051
ACHN cells Pleural effusion Homo sapiens (Human) CVCL_1067
HK-2 cells Kidney Homo sapiens (Human) CVCL_0302
RCC10 cells Kidney Homo sapiens (Human) CVCL_6265
RCC4 cells Kidney Homo sapiens (Human) CVCL_0498
Experiment for
Molecule Alteration		 qPCR
Experiment for
Drug Resistance		 Celltiter96 Aqueous Non Radioactive Cell Proliferation Assay
Mechanism Description Tumor suppressor genes like PTEN, PDCD4 and TIMP3, are target genes of miR21. PTEN is a potent inhibitor of PI3k/Akt pathway, as well as a direct target of miR21.
       Unusual Activation of Pro-survival Pathway (UAPP) Click to Show/Hide
Key Molecule: Programmed cell death protein 4 (PDCD4) [1]
Molecule Alteration Expression
Up-regulation
 Molecule Info 
Sensitive Disease Renal carcinoma [ICD-11: 2C90.2]
 Disease Info 
Experimental Note Revealed Based on the Cell Line Data
Cell Pathway Regulation PI3K/AKT signaling pathway Inhibition hsa04151
In Vitro Model 786-O cells Kidney Homo sapiens (Human) CVCL_1051
ACHN cells Pleural effusion Homo sapiens (Human) CVCL_1067
HK-2 cells Kidney Homo sapiens (Human) CVCL_0302
RCC10 cells Kidney Homo sapiens (Human) CVCL_6265
RCC4 cells Kidney Homo sapiens (Human) CVCL_0498
Experiment for
Molecule Alteration		 Western blot analysis
Experiment for
Drug Resistance		 Celltiter96 Aqueous Non Radioactive Cell Proliferation Assay
Mechanism Description Tumor suppressor genes like PTEN, PDCD4 and TIMP3, are target genes of miR21. PTEN is a potent inhibitor of PI3k/Akt pathway, as well as a direct target of miR21.
Key Molecule: Phosphatase and tensin homolog (PTEN) [1]
Molecule Alteration Expression
Up-regulation
 Molecule Info 
Sensitive Disease Renal carcinoma [ICD-11: 2C90.2]
 Disease Info 
Experimental Note Revealed Based on the Cell Line Data
Cell Pathway Regulation PI3K/AKT signaling pathway Inhibition hsa04151
In Vitro Model 786-O cells Kidney Homo sapiens (Human) CVCL_1051
ACHN cells Pleural effusion Homo sapiens (Human) CVCL_1067
HK-2 cells Kidney Homo sapiens (Human) CVCL_0302
RCC10 cells Kidney Homo sapiens (Human) CVCL_6265
RCC4 cells Kidney Homo sapiens (Human) CVCL_0498
Experiment for
Molecule Alteration		 Western blot analysis
Experiment for
Drug Resistance		 Celltiter96 Aqueous Non Radioactive Cell Proliferation Assay
Mechanism Description Tumor suppressor genes like PTEN, PDCD4 and TIMP3, are target genes of miR21. PTEN is a potent inhibitor of PI3k/Akt pathway, as well as a direct target of miR21.
Key Molecule: Metalloproteinase inhibitor 3 (TIMP3) [1]
Molecule Alteration Expression
Up-regulation
 Molecule Info 
Sensitive Disease Renal carcinoma [ICD-11: 2C90.2]
 Disease Info 
Experimental Note Revealed Based on the Cell Line Data
Cell Pathway Regulation PI3K/AKT signaling pathway Inhibition hsa04151
In Vitro Model 786-O cells Kidney Homo sapiens (Human) CVCL_1051
ACHN cells Pleural effusion Homo sapiens (Human) CVCL_1067
HK-2 cells Kidney Homo sapiens (Human) CVCL_0302
RCC10 cells Kidney Homo sapiens (Human) CVCL_6265
RCC4 cells Kidney Homo sapiens (Human) CVCL_0498
Experiment for
Molecule Alteration		 Western blot analysis
Experiment for
Drug Resistance		 Celltiter96 Aqueous Non Radioactive Cell Proliferation Assay
Mechanism Description Tumor suppressor genes like PTEN, PDCD4 and TIMP3, are target genes of miR21. PTEN is a potent inhibitor of PI3k/Akt pathway, as well as a direct target of miR21.
References
Ref 1 Targeting miR-21 decreases expression of multi-drug resistant genes and promotes chemosensitivity of renal carcinoma. Tumour Biol. 2017 Jul;39(7):1010428317707372. doi: 10.1177/1010428317707372.

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