Drug Information
Drug (ID: DG01595) and It's Reported Resistant Information
| Name |
Uprosertib
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| Synonyms |
Uprosertib; 1047634-65-0; GSK2141795; UNII-ZXM835LQ5E; GSK795; GSK2141795C; GSK-2141795; ZXM835LQ5E; Uprosertib (GSK2141795); N-((S)-1-Amino-3-(3,4-difluorophenyl)propan-2-yl)-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)furan-2-carboxamide; N-[(2S)-1-amino-3-(3,4-difluorophenyl)propan-2-yl]-5-chloro-4-(4-chloro-2-methylpyrazol-3-yl)furan-2-carboxamide; Uprosertib [USAN:INN]; Uprosertib (USAN/INN); Akt inhibitor gsk2141795; SCHEMBL168584; Uprosertib, GSK2141795; Akt inhibitor gsk-2141795; GTPL7902; CHEMBL3137336; BCP28204; EX-A1593; BDBM50170284; GSK-2141795C; MFCD28144686; NSC778368; NSC800960; s7492; ZINC43197676; AKOS027323909; CCG-268992; DB11969; NSC-778368; NSC-800960; NCGC00390653-01; AC-30940; HY-15965; D10674; F20800; Q27089099; GSK-2141795; GSK2141795; GSK 2141795; GSK795; GSK-795; GSK 795.; 2-Furancarboxamide, N-((1S)-2-amino-1-((3,4-difluorophenyl)methyl)ethyl)-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-; N-((1S)-1-(Aminomethyl)-2-(3,4-difluorophenyl)ethyl)-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)furan-2-carboxamide; N-{(1S)-2-amino-1-[(3,4-difluorophenyl)methyl]ethyl}-5-chloro-4-(4-chloro-1-methyl-1H-pyrazol-5-yl)-2-furancarboxamide
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| Indication |
In total 2 Indication(s)
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| Structure |
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| Target | Fibroblast growth factor receptor (FGFR) | NOUNIPROTAC | [2] | ||
| Fibroblast growth factor receptor 1 (FGFR1) | FGFR1_HUMAN | [2] | |||
| Click to Show/Hide the Molecular Information and External Link(s) of This Drug | |||||
| Formula |
6
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| IsoSMILES |
CN1C(=C(C=N1)Cl)C2=C(OC(=C2)C(=O)N[C@@H](CC3=CC(=C(C=C3)F)F)CN)Cl
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| InChI |
InChI=1S/C18H16Cl2F2N4O2/c1-26-16(12(19)8-24-26)11-6-15(28-17(11)20)18(27)25-10(7-23)4-9-2-3-13(21)14(22)5-9/h2-3,5-6,8,10H,4,7,23H2,1H3,(H,25,27)/t10-/m0/s1
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| InChIKey |
AXTAPYRUEKNRBA-JTQLQIEISA-N
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| PubChem CID | |||||
| TTD Drug ID | |||||
| DrugBank ID | |||||
Type(s) of Resistant Mechanism of This Drug
ADTT: Aberration of the Drug's Therapeutic Target
UAPP: Unusual Activation of Pro-survival Pathway
Drug Resistance Data Categorized by Their Corresponding Diseases
ICD-02: Benign/in-situ/malignant neoplasm
Solid tumour/cancer [ICD-11: 2A00-2F9Z]
| Drug Sensitivity Data Categorized by Their Corresponding Mechanisms | |||||||||||||
|
Aberration of the Drug's Therapeutic Target (ADTT)
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| Key Molecule: RAC-alpha serine/threonine-protein kinase (AKT1) | [2] | ||||||||||||
| Sensitive Disease | Solid tumour/cancer [ICD-11: 2A00-2F9Z] | ||||||||||||
| Molecule Alteration | Missense mutation | p.E17K (c.49G>A) |
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| Wild Type Structure | Method: X-ray diffraction | Resolution: 1.65 Å | |||||||||||
| Mutant Type Structure | Method: X-ray diffraction | Resolution: 1.94 Å | |||||||||||
| Download The Information of Sequence | Download The Structure File | ||||||||||||
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0
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-
S
M
M
S
S
D
D
V
V
A
A
I
I
V
V
K
K
E
E
10
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G
G
W
W
L
L
H
H
K
K
R
R
G
G
E
K
Y
Y
I
I
20
|
K
K
T
T
W
W
R
R
P
P
R
R
Y
Y
F
F
L
L
L
L
30
|
K
K
N
N
D
D
G
G
T
T
F
F
I
I
G
G
Y
Y
K
K
40
|
E
E
R
R
P
P
Q
Q
D
D
V
V
D
D
Q
Q
R
R
E
E
50
|
A
A
P
P
L
L
N
N
N
N
F
F
S
S
V
V
A
A
Q
Q
60
|
C
C
Q
Q
L
L
M
M
K
K
T
T
E
E
R
R
P
P
R
R
70
|
P
P
N
N
T
T
F
F
I
I
I
I
R
R
C
C
L
L
Q
Q
80
|
W
W
T
T
T
T
V
V
I
I
E
E
R
R
T
T
F
F
H
H
90
|
V
V
E
E
T
T
P
P
E
E
E
E
R
R
E
E
E
E
W
W
100
|
T
T
T
T
A
A
I
I
Q
Q
T
T
V
V
A
A
D
D
G
G
110
|
L
L
K
K
K
K
Q
Q
E
E
E
E
E
E
E
E
M
M
D
D
120
|
F
F
R
R
-
S
-
G
|
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| Experimental Note | Revealed Based on the Cell Line Data | ||||||||||||
| In Vitro Model | SkOV3 cells | Ovary | Homo sapiens (Human) | CVCL_0532 | |||||||||
| BT474 cells | Breast | Homo sapiens (Human) | CVCL_0179 | ||||||||||
| In Vivo Model | Female nu/nu CD-1 mouse xenograft model | Mus musculus | |||||||||||
| Mechanism Description | The missense mutation p.E17K (c.49G>A) in gene AKT1 cause the sensitivity of Uprosertib by aberration of the drug's therapeutic target | ||||||||||||
Melanoma [ICD-11: 2C30]
| Drug Sensitivity Data Categorized by Their Corresponding Mechanisms | |||||||||||||
|
Unusual Activation of Pro-survival Pathway (UAPP)
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| Key Molecule: RAC-alpha serine/threonine-protein kinase (AKT1) | [1] | ||||||||||||
| Sensitive Disease | Melanoma [ICD-11: 2C30.0] | ||||||||||||
| Molecule Alteration | Missense mutation | p.E17K (c.49G>A) |
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| Wild Type Structure | Method: X-ray diffraction | Resolution: 1.65 Å | |||||||||||
| Mutant Type Structure | Method: X-ray diffraction | Resolution: 1.94 Å | |||||||||||
| Download The Information of Sequence | Download The Structure File | ||||||||||||
-
0
|
-
S
M
M
S
S
D
D
V
V
A
A
I
I
V
V
K
K
E
E
10
|
G
G
W
W
L
L
H
H
K
K
R
R
G
G
E
K
Y
Y
I
I
20
|
K
K
T
T
W
W
R
R
P
P
R
R
Y
Y
F
F
L
L
L
L
30
|
K
K
N
N
D
D
G
G
T
T
F
F
I
I
G
G
Y
Y
K
K
40
|
E
E
R
R
P
P
Q
Q
D
D
V
V
D
D
Q
Q
R
R
E
E
50
|
A
A
P
P
L
L
N
N
N
N
F
F
S
S
V
V
A
A
Q
Q
60
|
C
C
Q
Q
L
L
M
M
K
K
T
T
E
E
R
R
P
P
R
R
70
|
P
P
N
N
T
T
F
F
I
I
I
I
R
R
C
C
L
L
Q
Q
80
|
W
W
T
T
T
T
V
V
I
I
E
E
R
R
T
T
F
F
H
H
90
|
V
V
E
E
T
T
P
P
E
E
E
E
R
R
E
E
E
E
W
W
100
|
T
T
T
T
A
A
I
I
Q
Q
T
T
V
V
A
A
D
D
G
G
110
|
L
L
K
K
K
K
Q
Q
E
E
E
E
E
E
E
E
M
M
D
D
120
|
F
F
R
R
-
S
-
G
|
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| Experimental Note | Revealed Based on the Cell Line Data | ||||||||||||
| In Vitro Model | 19 drug na?ve cell lines and four sub-lines | N.A. | N.A. | N.A. | |||||||||
| Experiment for Molecule Alteration |
Western blot analysis | ||||||||||||
| Experiment for Drug Resistance |
ATP-based luminescent assay; Flow cytometry assay | ||||||||||||
References
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