Drug Information

Drug (ID: DG01636) and It's Reported Resistant Information
Name
E7090
Synonyms
E-7090; E7090; 1622204-21-0; tasurgratinib; TN7CUD1NGA; UNII-TN7CUD1NGA; 5-((2-(4-(1-(2-hydroxyethyl)piperidin-4-yl)benzamido)pyridin-4-yl)oxy)-6-(2-methoxyethoxy)-N-methyl-1H-indole-1-carboxamide; 5-[2-[[4-[1-(2-hydroxyethyl)piperidin-4-yl]benzoyl]amino]pyridin-4-yl]oxy-6-(2-methoxyethoxy)-N-methylindole-1-carboxamide; CHEMBL3686884; SCHEMBL15955142; GTPL11414; BDBM142256; Fgf/fgfr pathway inhibitor E7090; BCP29727; EX-A2908; NSC806388; NSC-806388; SB18854; Example 22 [WO2014129477A1]; HY-101466; CS-0021430; E 7090; E7090; US8933099, 22; Q27896113; 1H-Indole-1-carboxamide, 5-((2-((4-(1-(2-hydroxyethyl)-4-piperidinyl)benzoyl)amino)-4-pyridinyl)oxy)-6-(2-methoxyethoxy)-N-methyl-; 5-((2-(((4-(1-(2-Hydroxyethyl)piperidin-4-yl)phenyl)carbonyl)amino)pyridin-4-yl)oxy)-6-(2-methoxyethoxy)-N-methyl-1H-indole-1-carboxamide
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Structure
Click to Show/Hide the Molecular Information and External Link(s) of This Drug
Formula
11
IsoSMILES
CNC(=O)N1C=CC2=CC(=C(C=C21)OCCOC)OC3=CC(=NC=C3)NC(=O)C4=CC=C(C=C4)C5CCN(CC5)CCO
InChI
InChI=1S/C32H37N5O6/c1-33-32(40)37-14-10-25-19-29(28(21-27(25)37)42-18-17-41-2)43-26-7-11-34-30(20-26)35-31(39)24-5-3-22(4-6-24)23-8-12-36(13-9-23)15-16-38/h3-7,10-11,14,19-21,23,38H,8-9,12-13,15-18H2,1-2H3,(H,33,40)(H,34,35,39)
InChIKey
IBHOLSBDZMIPPT-UHFFFAOYSA-N
PubChem CID
78323434
Type(s) of Resistant Mechanism of This Drug
  ADTT: Aberration of the Drug's Therapeutic Target
Drug Resistance Data Categorized by Their Corresponding Diseases
ICD-02: Benign/in-situ/malignant neoplasm
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Multiple myeloma [ICD-11: 2A83]
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Drug Sensitivity Data Categorized by Their Corresponding Mechanisms
  Aberration of the Drug's Therapeutic Target (ADTT) Click to Show/Hide
Key Molecule: Fibroblast growth factor receptor 3 (FGFR3) [1]
Sensitive Disease Multiple myeloma [ICD-11: 2A83.0]
 Disease Info 
Molecule Alteration Missense mutation
p.Y373C (c.1118A>G)
 Molecule Info 
Experimental Note Identified from the Human Clinical Data
Endometrial cancer [ICD-11: 2C76]
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Drug Sensitivity Data Categorized by Their Corresponding Mechanisms
  Aberration of the Drug's Therapeutic Target (ADTT) Click to Show/Hide
Key Molecule: Fibroblast growth factor receptor 2 (FGFR2) [1]
Sensitive Disease Endometrial adenocarcinoma [ICD-11: 2C76.0]
 Disease Info 
Molecule Alteration Missense mutation
p.S252W (c.755C>G)
 Molecule Info 
Wild Type Structure Method: X-ray diffraction Resolution: 3.88  Å
PDB: 4J23
Mutant Type Structure Method: X-ray diffraction Resolution: 2.70  Å
PDB: 1II4
   Download The Information of Sequence       Download The Structure File   
RMSD: 1.81
TM score: 0.89346
Amino acid change:
S252W
 : Wild Type Structure
 : Mutant Type Structure
  Mutation site(s) have been marked in red
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270
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Click to Show/Hide the Structure
Experimental Note Identified from the Human Clinical Data
References
Ref 1 E7090, a Novel Selective Inhibitor of Fibroblast Growth Factor Receptors, Displays Potent Antitumor Activity and Prolongs Survival in Preclinical ModelsMol Cancer Ther. 2016 Nov;15(11):2630-2639. doi: 10.1158/1535-7163.MCT-16-0261. Epub 2016 Aug 17.

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