Drug Information

Drug (ID: DG01599) and It's Reported Resistant Information
Name
Altiratinib
Synonyms
Altiratinib; 1345847-93-9; DCC-2701; DP-5164; Altiratinib [USAN]; UNII-T678746713; Altiratinib (USAN); 1,1-Cyclopropanedicarboxamide, N-[4-[[2-[(cyclopropylcarbonyl)amino]-4-pyridinyl]oxy]-2,5-difluorophenyl]-N'-(4-fluorophenyl)-; T678746713; 1,1-Cyclopropanedicarboxamide, N-(4-((2-((cyclopropylcarbonyl)amino)-4-pyridinyl)oxy)-2,5-difluorophenyl)-N'-(4-fluorophenyl)-; 1-N'-[4-[2-(cyclopropanecarbonylamino)pyridin-4-yl]oxy-2,5-difluorophenyl]-1-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide; N-(4-((2-(cyclopropanecarboxamido)pyridin-4-yl)oxy)-2,5-difluorophenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide.; N-[4-[[2-[(Cyclopropylcarbonyl)amino]-4-pyridinyl]oxy]-2,5-difluorophenyl]-N'-(4-fluorophenyl)-1,1-cyclopropanedicarboxamide; Altiratinib;DCC2701; Altiratinib(DCC-2701); SCHEMBL139906; GTPL9174; CHEMBL3545365; DCC-270; DCC2701; EX-A902; AOB87118; BCP15682; HY-B0791; BDBM50193395; MFCD28900672; NSC784590; s6412; AKOS026750329; ZINC113198271; CS-3944; NSC-784590; SB18876; NCGC00480913-04; N-(4-((2-((Cyclopropylcarbonyl)amino)pyridin-4-yl)oxy)-2,5-difluorophenyi)-N-(4- fluorophenyl)cyclopropane-1,1-dicarboxamide; B5832; FT-0700171; A14387; D10862; F11464; A887875; J-690136; Q27074416; 1,1-CYCLOPROPANEDICARBOXAMIDE, N-[4-[[2-[(CYCLOPROPYLCARBONYL)AMINO]-4-PYRIDINYL]OXY]-2,5-DIFLUOROPHENYL]-N-(4-FLUOROPHENYL)-; 4-{5-[(E)-2-{4-(2-Chlorophenyl)-5-[5-(methylsulfonyl)-2-pyridinyl]-4H-1,2,4-triazol-3-yl}vinyl]-1,3,4-oxadiazol-2-yl}benzonitrile; N-(4-(2-(cyclopropanecarboxamido)pyridin-4-yloxy)-2,5-difluorophenyl)-N'-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide
    Click to Show/Hide
Indication
In total 2 Indication(s)
Solid tumour/cancer [ICD-11: 2A00-2F9Z]
Phase 1
[1]
Solid tumour/cancer [ICD-11: 2A00-2F9Z]
Investigative
[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
8
IsoSMILES
C1CC1C(=O)NC2=NC=CC(=C2)OC3=C(C=C(C(=C3)F)NC(=O)C4(CC4)C(=O)NC5=CC=C(C=C5)F)F
InChI
InChI=1S/C26H21F3N4O4/c27-15-3-5-16(6-4-15)31-24(35)26(8-9-26)25(36)32-20-12-19(29)21(13-18(20)28)37-17-7-10-30-22(11-17)33-23(34)14-1-2-14/h3-7,10-14H,1-2,8-9H2,(H,31,35)(H,32,36)(H,30,33,34)
InChIKey
GNNDEPIMDAZHRQ-UHFFFAOYSA-N
PubChem CID
54576299
Type(s) of Resistant Mechanism of This Drug
  ADTT: Aberration of the Drug's Therapeutic Target
  RTDM: Regulation by the Disease Microenvironment
Drug Resistance Data Categorized by Their Corresponding Diseases
ICD-01: Infectious/parasitic diseases
Click to Show/Hide the Resistance Disease of This Class
Toxoplasmosis [ICD-11: 1F57]
Click to Show/Hide
Drug Resistance Data Categorized by Their Corresponding Mechanisms
  Aberration of the Drug's Therapeutic Target (ADTT) Click to Show/Hide
Key Molecule: Pre-mRNA processing factor 4 kinase (PRP4K) [2]
Resistant Disease Toxoplasmosis [ICD-11: 1F57.Z]
 Disease Info 
Molecule Alteration Mutation
F647S
 Molecule Info 
Experiment for
Molecule Alteration		 DNA sequencing assay
Experiment for
Drug Resistance		 Fluorescence microscopy assay
Mechanism Description Mutant strains edited for?TgPRP4K significantly decreased sensitivity to altiratinib
Key Molecule: Pre-mRNA processing factor 4 kinase (PRP4K) [2]
Resistant Disease Toxoplasmosis [ICD-11: 1F57.Z]
 Disease Info 
Molecule Alteration Mutation
L686F
 Molecule Info 
Experiment for
Molecule Alteration		 DNA sequencing assay
Experiment for
Drug Resistance		 Fluorescence microscopy assay
Mechanism Description Mutant strains edited for?TgPRP4K significantly decreased sensitivity to altiratinib
Key Molecule: Pre-mRNA processing factor 4 kinase (PRP4K) [2]
Resistant Disease Toxoplasmosis [ICD-11: 1F57.Z]
 Disease Info 
Molecule Alteration Mutation
F647S
 Molecule Info 
Experiment for
Molecule Alteration		 DNA sequencing assay
Experiment for
Drug Resistance		 Plaque assay
Mechanism Description Mutant strains edited for?TgPRP4K significantly decreased sensitivity to altiratinib
Key Molecule: Pre-mRNA processing factor 4 kinase (PRP4K) [2]
Resistant Disease Toxoplasmosis [ICD-11: 1F57.Z]
 Disease Info 
Molecule Alteration Mutation
L393S, L393F, F397L, and F397I
 Molecule Info 
Experiment for
Molecule Alteration		 DNA sequencing assay
Experiment for
Drug Resistance		 Plaque assay
Mechanism Description Mutant strains edited for?TgPRP4K significantly decreased sensitivity to altiratinib
Key Molecule: Pre-mRNA processing factor 4 kinase (PRP4K) [2]
Resistant Disease Toxoplasmosis [ICD-11: 1F57.Z]
 Disease Info 
Molecule Alteration Mutation
L715F
 Molecule Info 
Experiment for
Molecule Alteration		 DNA sequencing assay
Experiment for
Drug Resistance		 Plaque assay
Mechanism Description Mutant strains edited for?TgPRP4K significantly decreased sensitivity to altiratinib
ICD-02: Benign/in-situ/malignant neoplasm
Click to Show/Hide the Resistance Disease of This Class
Solid tumour/cancer [ICD-11: 2A00-2F9Z]
Click to Show/Hide
Drug Sensitivity Data Categorized by Their Corresponding Mechanisms
  Regulation by the Disease Microenvironment (RTDM) Click to Show/Hide
Key Molecule: Hepatocyte growth factor receptor (MET) [1]
Sensitive Disease Solid tumour/cancer [ICD-11: 2A00-2F9Z]
 Disease Info 
Molecule Alteration Missense mutation
p.Y1230H (c.3688T>C)
 Molecule Info 
Wild Type Structure Method: X-ray diffraction Resolution: 1.71  Å
PDB: 5HNI
Mutant Type Structure Method: X-ray diffraction Resolution: 1.97  Å
PDB: 5HLW
   Download The Information of Sequence       Download The Structure File   
RMSD: 0.65
TM score: 0.96625
Amino acid change:
Y1230H
 : Wild Type Structure
 : Mutant Type Structure
  Mutation site(s) have been marked in red
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N
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1050
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T
-
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I
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1060
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A
A
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H
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1070
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I
G
G
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P
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L
I
I
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1080
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F
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E
E
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I
G
G
R
R
G
G
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H
F
F
1090
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G
G
C
C
V
V
Y
Y
H
H
G
G
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T
L
L
L
L
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D
1100
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N
D
D
G
G
K
K
K
K
I
I
H
H
C
C
A
A
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1110
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K
K
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L
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1120
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I
1130
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I
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M
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F
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1140
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L
G
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C
L
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1160
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L
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F
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1170
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E
E
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T
H
H
N
N
P
P
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1180
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D
D
L
L
I
I
G
G
F
F
G
G
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L
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A
A
1190
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K
K
G
G
M
M
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L
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A
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K
K
K
1200
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F
F
V
V
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H
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R
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D
L
L
A
A
A
A
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R
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1210
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C
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M
L
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D
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E
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F
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1220
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V
A
A
D
D
F
F
G
G
L
L
A
A
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R
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D
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M
1230
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H
D
D
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E
F
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D
Y
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S
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H
H
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N
1240
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G
G
A
A
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L
L
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1260
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1270
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1280
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1290
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1300
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1320
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1330
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A
A
1340
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I
I
F
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E
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1350
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H
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A
A
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1360
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-
Click to Show/Hide the Structure
Experimental Note Revealed Based on the Cell Line Data
In Vitro Model A549 cells Lung Homo sapiens (Human) CVCL_0023
A375 cells Skin Homo sapiens (Human) CVCL_0132
THP-1 cells Blood Homo sapiens (Human) CVCL_0006
K562 cells Blood Homo sapiens (Human) CVCL_0004
MkN-45 cells Gastric Homo sapiens (Human) CVCL_0434
Sk-N-SH cells Adrenal Homo sapiens (Human) CVCL_0531
HCT-116 cells Colon Homo sapiens (Human) CVCL_0291
EBC-1 cells Lung Homo sapiens (Human) CVCL_2891
MRC-5 cells Lung Homo sapiens (Human) CVCL_0440
PC-3 cells Prostate Homo sapiens (Human) CVCL_0035
HUVEC cells Endothelium Homo sapiens (Human) N.A.
HUVEC cells Endothelium Homo sapiens (Human) N.A.
U87-MG cells Brain Homo sapiens (Human) CVCL_0022
SkMEL5 cells Skin Homo sapiens (Human) CVCL_0527
SkMEL28 cells Skin Homo sapiens (Human) CVCL_0526
MV-4-11 cells Peripheral blood Homo sapiens (Human) CVCL_0064
M-NFS-60 cells Blood Mus musculus (Mouse) CVCL_3543
KM-12 cells Colon Homo sapiens (Human) CVCL_1331
HMVEC cells Blood vessel Homo sapiens (Human) N.A.
EAhy926 cells N.A. Homo sapiens (Human) CVCL_3901
CHO-K cells Ovary Cricetulus griseus (Chinese hamster) (Cricetulus barabensis griseus) CVCL_0213
BT-474 cells Breast Homo sapiens (Human) CVCL_0179
B16/F10 cells Skin Mus musculus (Mouse) CVCL_0159
In Vivo Model Mouse xenograft efficacy model; MKN-45 xenograft mouse pharmacokinetic/pharmacodynamic model; Orthotopic U87-MG xenograft efficacy model; Orthotopic U87-MG xenograft survival model; PyMT syngeneic breast cancer model Mus musculus
Experiment for
Molecule Alteration		 Enzyme-linked immunosorbent assay; Western blot analysis
Experiment for
Drug Resistance		 Resazurin cell viability assay
Key Molecule: Hepatocyte growth factor receptor (MET) [1]
Sensitive Disease Solid tumour/cancer [ICD-11: 2A00-2F9Z]
 Disease Info 
Molecule Alteration Missense mutation
p.M1250T (c.3749T>C)
 Molecule Info 
Wild Type Structure Method: X-ray diffraction Resolution: 1.71  Å
PDB: 5HNI
Mutant Type Structure Method: X-ray diffraction Resolution: 2.20  Å
PDB: 5HOR
   Download The Information of Sequence       Download The Structure File   
RMSD: 0.55
TM score: 0.98376
Amino acid change:
M1250T
 : Wild Type Structure
 : Mutant Type Structure
  Mutation site(s) have been marked in red
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H
1080
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F
F
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N
E
E
V
V
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I
G
G
R
R
G
G
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H
F
F
1090
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G
G
C
C
V
V
Y
Y
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H
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G
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T
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L
L
L
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D
1100
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N
N
D
D
G
G
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K
K
K
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I
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H
C
C
A
A
V
V
1110
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K
K
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S
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L
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D
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1120
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E
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F
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L
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S
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L
L
L
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G
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C
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1160
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T
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1190
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M
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A
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1200
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F
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A
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1220
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A
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D
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Y
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D
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E
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H
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N
1240
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M
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A
A
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E
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Q
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T
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Q
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K
1260
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F
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K
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D
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1270
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L
L
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E
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L
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1280
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N
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T
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F
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1300
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L
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E
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C
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C
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M
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1330
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F
F
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A
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1350
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1360
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Click to Show/Hide the Structure
Experimental Note Revealed Based on the Cell Line Data
In Vitro Model A549 cells Lung Homo sapiens (Human) CVCL_0023
A375 cells Skin Homo sapiens (Human) CVCL_0132
THP-1 cells Blood Homo sapiens (Human) CVCL_0006
K562 cells Blood Homo sapiens (Human) CVCL_0004
MkN-45 cells Gastric Homo sapiens (Human) CVCL_0434
Sk-N-SH cells Adrenal Homo sapiens (Human) CVCL_0531
HCT-116 cells Colon Homo sapiens (Human) CVCL_0291
EBC-1 cells Lung Homo sapiens (Human) CVCL_2891
MRC-5 cells Lung Homo sapiens (Human) CVCL_0440
PC-3 cells Prostate Homo sapiens (Human) CVCL_0035
HUVEC cells Endothelium Homo sapiens (Human) N.A.
HUVEC cells Endothelium Homo sapiens (Human) N.A.
U87-MG cells Brain Homo sapiens (Human) CVCL_0022
SkMEL5 cells Skin Homo sapiens (Human) CVCL_0527
SkMEL28 cells Skin Homo sapiens (Human) CVCL_0526
MV-4-11 cells Peripheral blood Homo sapiens (Human) CVCL_0064
M-NFS-60 cells Blood Mus musculus (Mouse) CVCL_3543
KM-12 cells Colon Homo sapiens (Human) CVCL_1331
HMVEC cells Blood vessel Homo sapiens (Human) N.A.
EAhy926 cells N.A. Homo sapiens (Human) CVCL_3901
CHO-K cells Ovary Cricetulus griseus (Chinese hamster) (Cricetulus barabensis griseus) CVCL_0213
BT-474 cells Breast Homo sapiens (Human) CVCL_0179
B16/F10 cells Skin Mus musculus (Mouse) CVCL_0159
In Vivo Model Mouse xenograft efficacy model; MKN-45 xenograft mouse pharmacokinetic/pharmacodynamic model; Orthotopic U87-MG xenograft efficacy model; Orthotopic U87-MG xenograft survival model; PyMT syngeneic breast cancer model Mus musculus
Experiment for
Molecule Alteration		 Enzyme-linked immunosorbent assay; Western blot analysis
Experiment for
Drug Resistance		 Resazurin cell viability assay
Key Molecule: Hepatocyte growth factor receptor (MET) [1]
Sensitive Disease Solid tumour/cancer [ICD-11: 2A00-2F9Z]
 Disease Info 
Molecule Alteration Missense mutation
p.D1228N (c.3682G>A)
 Molecule Info 
Experimental Note Revealed Based on the Cell Line Data
In Vitro Model A549 cells Lung Homo sapiens (Human) CVCL_0023
A375 cells Skin Homo sapiens (Human) CVCL_0132
THP-1 cells Blood Homo sapiens (Human) CVCL_0006
K562 cells Blood Homo sapiens (Human) CVCL_0004
MkN-45 cells Gastric Homo sapiens (Human) CVCL_0434
Sk-N-SH cells Adrenal Homo sapiens (Human) CVCL_0531
HCT-116 cells Colon Homo sapiens (Human) CVCL_0291
EBC-1 cells Lung Homo sapiens (Human) CVCL_2891
MRC-5 cells Lung Homo sapiens (Human) CVCL_0440
PC-3 cells Prostate Homo sapiens (Human) CVCL_0035
HUVEC cells Endothelium Homo sapiens (Human) N.A.
HUVEC cells Endothelium Homo sapiens (Human) N.A.
U87-MG cells Brain Homo sapiens (Human) CVCL_0022
SkMEL5 cells Skin Homo sapiens (Human) CVCL_0527
SkMEL28 cells Skin Homo sapiens (Human) CVCL_0526
MV-4-11 cells Peripheral blood Homo sapiens (Human) CVCL_0064
M-NFS-60 cells Blood Mus musculus (Mouse) CVCL_3543
KM-12 cells Colon Homo sapiens (Human) CVCL_1331
HMVEC cells Blood vessel Homo sapiens (Human) N.A.
EAhy926 cells N.A. Homo sapiens (Human) CVCL_3901
CHO-K cells Ovary Cricetulus griseus (Chinese hamster) (Cricetulus barabensis griseus) CVCL_0213
BT-474 cells Breast Homo sapiens (Human) CVCL_0179
B16/F10 cells Skin Mus musculus (Mouse) CVCL_0159
In Vivo Model Mouse xenograft efficacy model; MKN-45 xenograft mouse pharmacokinetic/pharmacodynamic model; Orthotopic U87-MG xenograft efficacy model; Orthotopic U87-MG xenograft survival model; PyMT syngeneic breast cancer model Mus musculus
Experiment for
Molecule Alteration		 Enzyme-linked immunosorbent assay; Western blot analysis
Experiment for
Drug Resistance		 Resazurin cell viability assay
Key Molecule: Hepatocyte growth factor receptor (MET) [1]
Sensitive Disease Solid tumour/cancer [ICD-11: 2A00-2F9Z]
 Disease Info 
Molecule Alteration Missense mutation
p.Y1230D (c.3688T>G)
 Molecule Info 
Experimental Note Revealed Based on the Cell Line Data
In Vitro Model A549 cells Lung Homo sapiens (Human) CVCL_0023
A375 cells Skin Homo sapiens (Human) CVCL_0132
THP-1 cells Blood Homo sapiens (Human) CVCL_0006
K562 cells Blood Homo sapiens (Human) CVCL_0004
MkN-45 cells Gastric Homo sapiens (Human) CVCL_0434
Sk-N-SH cells Adrenal Homo sapiens (Human) CVCL_0531
HCT-116 cells Colon Homo sapiens (Human) CVCL_0291
EBC-1 cells Lung Homo sapiens (Human) CVCL_2891
MRC-5 cells Lung Homo sapiens (Human) CVCL_0440
PC-3 cells Prostate Homo sapiens (Human) CVCL_0035
HUVEC cells Endothelium Homo sapiens (Human) N.A.
HUVEC cells Endothelium Homo sapiens (Human) N.A.
U87-MG cells Brain Homo sapiens (Human) CVCL_0022
SkMEL5 cells Skin Homo sapiens (Human) CVCL_0527
SkMEL28 cells Skin Homo sapiens (Human) CVCL_0526
MV-4-11 cells Peripheral blood Homo sapiens (Human) CVCL_0064
M-NFS-60 cells Blood Mus musculus (Mouse) CVCL_3543
KM-12 cells Colon Homo sapiens (Human) CVCL_1331
HMVEC cells Blood vessel Homo sapiens (Human) N.A.
EAhy926 cells N.A. Homo sapiens (Human) CVCL_3901
CHO-K cells Ovary Cricetulus griseus (Chinese hamster) (Cricetulus barabensis griseus) CVCL_0213
BT-474 cells Breast Homo sapiens (Human) CVCL_0179
B16/F10 cells Skin Mus musculus (Mouse) CVCL_0159
In Vivo Model Mouse xenograft efficacy model; MKN-45 xenograft mouse pharmacokinetic/pharmacodynamic model; Orthotopic U87-MG xenograft efficacy model; Orthotopic U87-MG xenograft survival model; PyMT syngeneic breast cancer model Mus musculus
Experiment for
Molecule Alteration		 Enzyme-linked immunosorbent assay; Western blot analysis
Experiment for
Drug Resistance		 Resazurin cell viability assay
Key Molecule: Hepatocyte growth factor receptor (MET) [1]
Sensitive Disease Solid tumour/cancer [ICD-11: 2A00-2F9Z]
 Disease Info 
Molecule Alteration Missense mutation
p.Y1230C (c.3689A>G)
 Molecule Info 
Experimental Note Revealed Based on the Cell Line Data
In Vitro Model A549 cells Lung Homo sapiens (Human) CVCL_0023
A375 cells Skin Homo sapiens (Human) CVCL_0132
THP-1 cells Blood Homo sapiens (Human) CVCL_0006
K562 cells Blood Homo sapiens (Human) CVCL_0004
MkN-45 cells Gastric Homo sapiens (Human) CVCL_0434
Sk-N-SH cells Adrenal Homo sapiens (Human) CVCL_0531
HCT-116 cells Colon Homo sapiens (Human) CVCL_0291
EBC-1 cells Lung Homo sapiens (Human) CVCL_2891
MRC-5 cells Lung Homo sapiens (Human) CVCL_0440
PC-3 cells Prostate Homo sapiens (Human) CVCL_0035
HUVEC cells Endothelium Homo sapiens (Human) N.A.
HUVEC cells Endothelium Homo sapiens (Human) N.A.
U87-MG cells Brain Homo sapiens (Human) CVCL_0022
SkMEL5 cells Skin Homo sapiens (Human) CVCL_0527
SkMEL28 cells Skin Homo sapiens (Human) CVCL_0526
MV-4-11 cells Peripheral blood Homo sapiens (Human) CVCL_0064
M-NFS-60 cells Blood Mus musculus (Mouse) CVCL_3543
KM-12 cells Colon Homo sapiens (Human) CVCL_1331
HMVEC cells Blood vessel Homo sapiens (Human) N.A.
EAhy926 cells N.A. Homo sapiens (Human) CVCL_3901
CHO-K cells Ovary Cricetulus griseus (Chinese hamster) (Cricetulus barabensis griseus) CVCL_0213
BT-474 cells Breast Homo sapiens (Human) CVCL_0179
B16/F10 cells Skin Mus musculus (Mouse) CVCL_0159
In Vivo Model Mouse xenograft efficacy model; MKN-45 xenograft mouse pharmacokinetic/pharmacodynamic model; Orthotopic U87-MG xenograft efficacy model; Orthotopic U87-MG xenograft survival model; PyMT syngeneic breast cancer model Mus musculus
Experiment for
Molecule Alteration		 Enzyme-linked immunosorbent assay; Western blot analysis
Experiment for
Drug Resistance		 Resazurin cell viability assay
References
Ref 1 Altiratinib Inhibits Tumor Growth, Invasion, Angiogenesis, and Microenvironment-Mediated Drug Resistance via Balanced Inhibition of MET, TIE2, and VEGFR2Mol Cancer Ther. 2015 Sep;14(9):2023-34. doi: 10.1158/1535-7163.MCT-14-1105. Epub 2015 Aug 18.
Ref 2 Altiratinib blocks Toxoplasma gondii and Plasmodium falciparum development by selectively targeting a spliceosome kinase. Sci Transl Med. 2022 Aug 3;14(656):eabn3231.

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