Drug Information

Drug (ID: DG01640) and It's Reported Resistant Information
Name
Lifirafenib
Synonyms
Lifirafenib; BGB-283; Beigene-283; 1446090-77-2; 1446090-79-4; 5-(((1R,1aS,6bR)-1-(6-(trifluoromethyl)-1H-benzo[d]imidazol-2-yl)-1a,6b-dihydro-1H-cyclopropa[b]benzofuran-5-yl)oxy)-3,4-dihydro-1,8-naphthyridin-2(1H)-one; Bgb 283; UNII-8762XZS5ZF; 8762XZS5ZF; 5-(((1R,1aS,6bR)-1-(6-(Trifluoromethyl)-1H-benzimidazol-2-yl)-1a,6b-dihydro-1H-cyclopropa(b)benzofuran-5-yl)oxy)-3,4-dihydro-1H-1,8-naphthyridin-2-one; BGB283; 5-({(1r,1as,6br)-1-[5-(Trifluoromethyl)-1h-Benzimidazol-2-Yl]-1a,6b-Dihydro-1h-Cyclopropa[b][1]benzofuran-5-Yl}oxy)-3,4-Dihydro-1,8-Naphthyridin-2(1h)-One; 5-[[(1R,1aS,6bR)-1-[6-(trifluoromethyl)-1H-benzimidazol-2-yl]-1a,6b-dihydro-1H-cyclopropa[b][1]benzofuran-5-yl]oxy]-3,4-dihydro-1H-1,8-naphthyridin-2-one; compound 2.2b; 5-{{(1r,1as,6br)-1-[5-(trifluoromethyl)-1h-benzimidazol-2-yl]-1a,6b-dihydro-1h-cyclopropa[b][1]benzofuran-5-yl}oxy}-3,4-dihydro-1,8-naphthyridin-2(1h)-one; Lifirafenib [USAN]; Lifirafenib (USAN/INN); BGB-283;Beigene-283; GTPL8958; CHEMBL4209157; SCHEMBL15085288; BDBM372968; EX-A1473; US9895376, Compound 2.2b; WHC09077; WHC09079; Lifirafenib;BGB-283;Beigene-283; BDBM50453816; WHO 10554; ZINC68764621; CS-6308; DB14773; HY-18957; D11410; A900647; Q27075193; 1,8-Naphthyridin-2(1H)-one, 5-(((1R,1aS,6bR)-1a,6b-dihydro-1-(6-(trifluoromethyl)-1H-benzimidazol-2-yl)-1H-cyclopropa(b)benzofuran-5-yl)oxy)-3,4-dihydro-; 3K3
    Click to Show/Hide
Indication
In total 1 Indication(s)
Solid tumour/cancer [ICD-11: 2A00-2F9Z]
Phase 1/2
[1]
Structure
Target Fms-like tyrosine kinase 3 (FLT-3) FLT3_HUMAN [1]
Tyrosine-protein kinase Mer (MERTK) MERTK_HUMAN [1]
Click to Show/Hide the Molecular Information and External Link(s) of This Drug
Formula
3
IsoSMILES
C1CC(=O)NC2=NC=CC(=C21)OC3=CC4=C(C=C3)O[C@H]5[C@@H]4[C@@H]5C6=NC7=C(N6)C=C(C=C7)C(F)(F)F
InChI
InChI=1S/C25H17F3N4O3/c26-25(27,28)11-1-4-15-16(9-11)31-24(30-15)21-20-14-10-12(2-5-17(14)35-22(20)21)34-18-7-8-29-23-13(18)3-6-19(33)32-23/h1-2,4-5,7-10,20-22H,3,6H2,(H,30,31)(H,29,32,33)/t20-,21-,22-/m0/s1
InChIKey
NGFFVZQXSRKHBM-FKBYEOEOSA-N
PubChem CID
89670174
TTD Drug ID
D10LNV
DrugBank ID
DB14773
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]
Click to Show/Hide
Drug Sensitivity Data Categorized by Their Corresponding Mechanisms
  Unusual Activation of Pro-survival Pathway (UAPP) Click to Show/Hide
Key Molecule: Epidermal growth factor receptor (EGFR) [1]
Sensitive Disease Solid tumour/cancer [ICD-11: 2A00-2F9Z]
 Disease Info 
Molecule Alteration Missense mutation
p.L858R (c.2573T>G)
 Molecule Info 
Wild Type Structure Method: X-ray diffraction Resolution: 2.64  Å
PDB: 4LI5
Mutant Type Structure Method: X-ray diffraction Resolution: 2.47  Å
PDB: 2ITV
   Download The Information of Sequence       Download The Structure File   
RMSD: 1.34
TM score: 0.90001
Amino acid change:
L858R
 : Wild Type Structure
 : Mutant Type Structure
  Mutation site(s) have been marked in red
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G
-
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-
M
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G
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E
E
A
A
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700
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N
N
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A
A
L
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L
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I
I
L
L
K
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E
E
710
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T
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E
E
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V
L
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G
G
720
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G
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V
Y
Y
K
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G
G
730
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L
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W
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I
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P
E
E
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G
E
E
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740
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I
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V
A
A
I
I
K
K
E
E
L
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R
E
E
750
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A
A
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S
P
P
K
K
A
A
N
N
K
K
E
E
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I
760
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L
L
D
D
E
E
A
A
Y
Y
V
V
M
M
A
A
S
S
V
V
770
|
D
D
N
N
P
P
H
H
V
V
C
C
R
R
L
L
L
L
G
G
780
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I
I
C
C
L
L
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T
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V
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Q
L
L
I
I
790
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T
T
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Q
L
L
M
M
P
P
F
F
G
G
C
C
L
L
L
L
800
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D
D
Y
Y
V
V
R
R
E
E
H
H
K
K
D
D
N
N
I
I
810
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G
G
S
S
Q
Q
Y
Y
L
L
L
L
N
N
W
W
C
C
V
V
820
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Q
Q
I
I
A
A
K
K
G
G
M
M
N
N
Y
Y
L
L
E
E
830
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D
D
R
R
R
R
L
L
V
V
H
H
R
R
D
D
L
L
A
A
840
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A
A
R
R
N
N
V
V
L
L
V
V
K
K
T
T
P
P
Q
Q
850
|
H
H
V
V
K
K
I
I
T
T
D
D
F
F
G
G
L
R
A
A
860
|
K
K
L
L
L
L
G
G
A
A
E
E
E
E
K
K
E
E
Y
Y
870
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H
H
A
A
E
E
G
G
G
G
K
K
V
V
P
P
I
I
K
K
880
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W
W
M
M
A
A
L
L
E
E
S
S
I
I
L
L
H
H
R
R
890
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I
I
Y
Y
T
T
H
H
Q
Q
S
S
D
D
V
V
W
W
S
S
900
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Y
Y
G
G
V
V
T
T
V
V
W
W
E
E
L
L
M
M
T
T
910
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F
F
G
G
S
S
K
K
P
P
Y
Y
D
D
G
G
I
I
P
P
920
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A
A
S
S
E
E
I
I
S
S
S
S
I
I
L
L
E
E
K
K
930
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G
G
E
E
R
R
L
L
P
P
Q
Q
P
P
P
P
I
I
C
C
940
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T
T
I
I
D
D
V
V
Y
Y
M
M
I
I
M
M
V
V
K
K
950
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C
C
W
W
M
M
I
I
D
D
A
A
D
D
S
S
R
R
P
P
960
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K
K
F
F
R
R
E
E
L
L
I
I
I
I
E
E
F
F
S
S
970
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K
K
M
M
A
A
R
R
D
D
P
P
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Q
R
R
Y
Y
L
L
980
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V
V
I
I
Q
Q
G
G
D
D
E
E
R
R
M
M
H
H
L
L
990
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P
P
S
S
P
P
T
T
D
D
S
S
N
N
F
F
Y
Y
R
R
1000
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A
A
L
L
M
M
D
D
E
E
E
E
D
D
M
M
D
D
D
D
1010
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V
V
V
V
D
D
A
A
D
D
E
E
Y
Y
L
L
I
I
P
P
1020
|
Q
Q
-
Q
-
G
Click to Show/Hide the Structure
Experimental Note Revealed Based on the Cell Line Data
In Vitro Model HT29 Cells Colon Homo sapiens (Human) CVCL_A8EZ
SW620 cells Colon Homo sapiens (Human) CVCL_0547
HCT116 cells Colon Homo sapiens (Human) CVCL_0291
A375 cells Skin Homo sapiens (Human) CVCL_0132
HCC827 cells Lung Homo sapiens (Human) CVCL_2063
A431 cells Skin Homo sapiens (Human) CVCL_0037
COLO205 cells Colon Homo sapiens (Human) CVCL_F402
WiDR cells Colon Homo sapiens (Human) CVCL_2760
Ba/F3 cells Colon Homo sapiens (Human) CVCL_0161
SkMEL28 cells Skin Homo sapiens (Human) CVCL_0526
In Vivo Model Female NOD/SCID and BALB/c nude mouse xenograft model Mus musculus
Experiment for
Molecule Alteration		 Western blot analysis
Experiment for
Drug Resistance		 CellTiter-Glo assay; Tumor volume measurement assay
Key Molecule: Serine/threonine-protein kinase B-raf (BRAF) [1]
Sensitive Disease Solid tumour/cancer [ICD-11: 2A00-2F9Z]
 Disease Info 
Molecule Alteration Missense mutation
p.V600E (c.1799T>A)
 Molecule Info 
Wild Type Structure Method: X-ray diffraction Resolution: 2.55  Å
PDB: 4E26
Mutant Type Structure Method: X-ray diffraction Resolution: 3.20  Å
PDB: 4G9R
   Download The Information of Sequence       Download The Structure File   
RMSD: 1.53
TM score: 0.95765
Amino acid change:
V600E
 : Wild Type Structure
 : Mutant Type Structure
  Mutation site(s) have been marked in red
-
420
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M
M
D
D
R
R
G
G
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H
H
H
H
H
H
430
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H
H
G
G
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S
E
E
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D
R
R
N
N
R
R
M
M
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K
440
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T
T
L
L
G
G
R
R
R
R
D
D
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S
D
D
D
D
450
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W
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460
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G
G
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I
I
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G
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S
F
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G
470
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T
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Y
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G
K
K
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H
G
G
D
D
480
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V
V
A
A
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V
K
K
M
M
L
L
N
N
V
V
T
T
A
A
490
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P
P
T
T
P
P
Q
Q
Q
Q
L
L
Q
Q
A
A
F
F
K
K
500
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N
N
E
E
V
V
G
G
V
V
L
L
R
R
K
K
T
T
R
R
510
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H
H
V
V
N
N
I
I
L
L
L
L
F
F
M
M
G
G
Y
Y
520
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S
S
T
T
K
K
P
P
Q
Q
L
L
A
A
I
I
V
V
T
T
530
|
Q
Q
W
W
C
C
E
E
G
G
S
S
S
S
L
L
Y
Y
H
H
540
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H
H
L
L
H
H
I
I
I
I
E
E
T
T
K
K
F
F
E
E
550
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M
M
I
I
K
K
L
L
I
I
D
D
I
I
A
A
R
R
Q
Q
560
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T
T
A
A
Q
Q
G
G
M
M
D
D
Y
Y
L
L
H
H
A
A
570
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K
K
S
S
I
I
I
I
H
H
R
R
D
D
L
L
K
K
S
S
580
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N
N
N
N
I
I
F
F
L
L
H
H
E
E
D
D
L
L
T
T
590
|
V
V
K
K
I
I
G
G
D
D
F
F
G
G
L
L
A
A
T
T
600
|
V
E
K
K
S
S
R
R
W
W
S
S
G
G
S
S
H
H
Q
Q
610
|
F
F
E
E
Q
Q
L
L
S
S
G
G
S
S
I
I
L
L
W
W
620
|
M
M
A
A
P
P
E
E
V
V
I
I
R
R
M
M
Q
Q
D
D
630
|
K
K
N
N
P
P
Y
Y
S
S
F
F
Q
Q
S
S
D
D
V
V
640
|
Y
Y
A
A
F
F
G
G
I
I
V
V
L
L
Y
Y
E
E
L
L
650
|
M
M
T
T
G
G
Q
Q
L
L
P
P
Y
Y
S
S
N
N
I
I
660
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N
N
N
N
R
R
D
D
Q
Q
I
I
I
I
F
F
M
M
V
V
670
|
G
G
R
R
G
G
Y
Y
L
L
S
S
P
P
D
D
L
L
S
S
680
|
K
K
V
V
R
R
S
S
N
N
C
C
P
P
K
K
A
A
M
M
690
|
K
K
R
R
L
L
M
M
A
A
E
E
C
C
L
L
K
K
K
K
700
|
K
K
R
R
D
D
E
E
R
R
P
P
L
L
F
F
P
P
Q
Q
710
|
I
I
L
L
A
A
S
S
I
I
E
E
L
L
L
L
A
A
R
R
720
|
S
S
L
L
P
P
K
K
I
I
H
H
R
R
Click to Show/Hide the Structure
Experimental Note Revealed Based on the Cell Line Data
In Vitro Model HT29 Cells Colon Homo sapiens (Human) CVCL_A8EZ
SW620 cells Colon Homo sapiens (Human) CVCL_0547
HCT116 cells Colon Homo sapiens (Human) CVCL_0291
A375 cells Skin Homo sapiens (Human) CVCL_0132
HCC827 cells Lung Homo sapiens (Human) CVCL_2063
A431 cells Skin Homo sapiens (Human) CVCL_0037
COLO205 cells Colon Homo sapiens (Human) CVCL_F402
WiDR cells Colon Homo sapiens (Human) CVCL_2760
Ba/F3 cells Colon Homo sapiens (Human) CVCL_0161
SkMEL28 cells Skin Homo sapiens (Human) CVCL_0526
In Vivo Model Female NOD/SCID and BALB/c nude mouse xenograft model Mus musculus
Experiment for
Molecule Alteration		 Western blot analysis
Experiment for
Drug Resistance		 CellTiter-Glo assay; Tumor volume measurement assay
Colorectal cancer [ICD-11: 2B91]
Click to Show/Hide
Drug Sensitivity Data Categorized by Their Corresponding Mechanisms
  Unusual Activation of Pro-survival Pathway (UAPP) Click to Show/Hide
Key Molecule: Serine/threonine-protein kinase B-raf (BRAF) [1]
Sensitive Disease Colorectal cancer [ICD-11: 2B91.1]
 Disease Info 
Molecule Alteration Missense mutation
p.V600E (c.1799T>A)
 Molecule Info 
Wild Type Structure Method: X-ray diffraction Resolution: 2.55  Å
PDB: 4E26
Mutant Type Structure Method: X-ray diffraction Resolution: 3.20  Å
PDB: 4G9R
   Download The Information of Sequence       Download The Structure File   
RMSD: 1.53
TM score: 0.95765
Amino acid change:
V600E
 : Wild Type Structure
 : Mutant Type Structure
  Mutation site(s) have been marked in red
-
420
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M
M
D
D
R
R
G
G
S
S
H
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H
H
H
H
H
H
H
H
430
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H
H
G
G
S
S
E
E
D
D
R
R
N
N
R
R
M
M
K
K
440
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T
T
L
L
G
G
R
R
R
R
D
D
S
S
S
S
D
D
D
D
450
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W
W
E
E
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I
P
P
D
D
G
G
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I
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T
V
V
460
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G
G
Q
Q
R
R
I
I
G
G
S
S
G
G
S
S
F
F
G
G
470
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T
T
V
V
Y
Y
K
K
G
G
K
K
W
W
H
H
G
G
D
D
480
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V
V
A
A
V
V
K
K
M
M
L
L
N
N
V
V
T
T
A
A
490
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P
P
T
T
P
P
Q
Q
Q
Q
L
L
Q
Q
A
A
F
F
K
K
500
|
N
N
E
E
V
V
G
G
V
V
L
L
R
R
K
K
T
T
R
R
510
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H
H
V
V
N
N
I
I
L
L
L
L
F
F
M
M
G
G
Y
Y
520
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S
S
T
T
K
K
P
P
Q
Q
L
L
A
A
I
I
V
V
T
T
530
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Q
Q
W
W
C
C
E
E
G
G
S
S
S
S
L
L
Y
Y
H
H
540
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H
H
L
L
H
H
I
I
I
I
E
E
T
T
K
K
F
F
E
E
550
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M
M
I
I
K
K
L
L
I
I
D
D
I
I
A
A
R
R
Q
Q
560
|
T
T
A
A
Q
Q
G
G
M
M
D
D
Y
Y
L
L
H
H
A
A
570
|
K
K
S
S
I
I
I
I
H
H
R
R
D
D
L
L
K
K
S
S
580
|
N
N
N
N
I
I
F
F
L
L
H
H
E
E
D
D
L
L
T
T
590
|
V
V
K
K
I
I
G
G
D
D
F
F
G
G
L
L
A
A
T
T
600
|
V
E
K
K
S
S
R
R
W
W
S
S
G
G
S
S
H
H
Q
Q
610
|
F
F
E
E
Q
Q
L
L
S
S
G
G
S
S
I
I
L
L
W
W
620
|
M
M
A
A
P
P
E
E
V
V
I
I
R
R
M
M
Q
Q
D
D
630
|
K
K
N
N
P
P
Y
Y
S
S
F
F
Q
Q
S
S
D
D
V
V
640
|
Y
Y
A
A
F
F
G
G
I
I
V
V
L
L
Y
Y
E
E
L
L
650
|
M
M
T
T
G
G
Q
Q
L
L
P
P
Y
Y
S
S
N
N
I
I
660
|
N
N
N
N
R
R
D
D
Q
Q
I
I
I
I
F
F
M
M
V
V
670
|
G
G
R
R
G
G
Y
Y
L
L
S
S
P
P
D
D
L
L
S
S
680
|
K
K
V
V
R
R
S
S
N
N
C
C
P
P
K
K
A
A
M
M
690
|
K
K
R
R
L
L
M
M
A
A
E
E
C
C
L
L
K
K
K
K
700
|
K
K
R
R
D
D
E
E
R
R
P
P
L
L
F
F
P
P
Q
Q
710
|
I
I
L
L
A
A
S
S
I
I
E
E
L
L
L
L
A
A
R
R
720
|
S
S
L
L
P
P
K
K
I
I
H
H
R
R
Click to Show/Hide the Structure
Experimental Note Revealed Based on the Cell Line Data
In Vitro Model HT29 Cells Colon Homo sapiens (Human) CVCL_A8EZ
SW620 cells Colon Homo sapiens (Human) CVCL_0547
HCT116 cells Colon Homo sapiens (Human) CVCL_0291
A375 cells Skin Homo sapiens (Human) CVCL_0132
HCC827 cells Lung Homo sapiens (Human) CVCL_2063
A431 cells Skin Homo sapiens (Human) CVCL_0037
COLO205 cells Colon Homo sapiens (Human) CVCL_F402
WiDR cells Colon Homo sapiens (Human) CVCL_2760
Ba/F3 cells Colon Homo sapiens (Human) CVCL_0161
SkMEL28 cells Skin Homo sapiens (Human) CVCL_0526
In Vivo Model Female NOD/SCID and BALB/c nude mouse xenograft model Mus musculus
Experiment for
Molecule Alteration		 Western blot analysis
Experiment for
Drug Resistance		 CellTiter-Glo assay; Tumor volume measurement assay
Lung cancer [ICD-11: 2C25]
Click to Show/Hide
Drug Sensitivity Data Categorized by Their Corresponding Mechanisms
  Unusual Activation of Pro-survival Pathway (UAPP) Click to Show/Hide
Key Molecule: Epidermal growth factor receptor (EGFR) [1]
Sensitive Disease Lung adenocarcinoma [ICD-11: 2C25.0]
 Disease Info 
Molecule Alteration IF-deletion
p.E746_A750delELREA (c.2236_2250del15)
 Molecule Info 
Experimental Note Revealed Based on the Cell Line Data
In Vitro Model HT29 Cells Colon Homo sapiens (Human) CVCL_A8EZ
SW620 cells Colon Homo sapiens (Human) CVCL_0547
HCT116 cells Colon Homo sapiens (Human) CVCL_0291
A375 cells Skin Homo sapiens (Human) CVCL_0132
HCC827 cells Lung Homo sapiens (Human) CVCL_2063
A431 cells Skin Homo sapiens (Human) CVCL_0037
COLO205 cells Colon Homo sapiens (Human) CVCL_F402
WiDR cells Colon Homo sapiens (Human) CVCL_2760
Ba/F3 cells Colon Homo sapiens (Human) CVCL_0161
SkMEL28 cells Skin Homo sapiens (Human) CVCL_0526
In Vivo Model Female NOD/SCID and BALB/c nude mouse xenograft model Mus musculus
Experiment for
Molecule Alteration		 Western blot analysis
Experiment for
Drug Resistance		 CellTiter-Glo assay; Tumor volume measurement assay
Melanoma [ICD-11: 2C30]
Click to Show/Hide
Drug Sensitivity Data Categorized by Their Corresponding Mechanisms
  Unusual Activation of Pro-survival Pathway (UAPP) Click to Show/Hide
Key Molecule: Serine/threonine-protein kinase B-raf (BRAF) [1]
Sensitive Disease Melanoma [ICD-11: 2C30.0]
 Disease Info 
Molecule Alteration Missense mutation
p.V600E (c.1799T>A)
 Molecule Info 
Wild Type Structure Method: X-ray diffraction Resolution: 2.55  Å
PDB: 4E26
Mutant Type Structure Method: X-ray diffraction Resolution: 3.20  Å
PDB: 4G9R
   Download The Information of Sequence       Download The Structure File   
RMSD: 1.53
TM score: 0.95765
Amino acid change:
V600E
 : Wild Type Structure
 : Mutant Type Structure
  Mutation site(s) have been marked in red
-
420
|
M
M
D
D
R
R
G
G
S
S
H
H
H
H
H
H
H
H
H
H
430
|
H
H
G
G
S
S
E
E
D
D
R
R
N
N
R
R
M
M
K
K
440
|
T
T
L
L
G
G
R
R
R
R
D
D
S
S
S
S
D
D
D
D
450
|
W
W
E
E
I
I
P
P
D
D
G
G
Q
Q
I
I
T
T
V
V
460
|
G
G
Q
Q
R
R
I
I
G
G
S
S
G
G
S
S
F
F
G
G
470
|
T
T
V
V
Y
Y
K
K
G
G
K
K
W
W
H
H
G
G
D
D
480
|
V
V
A
A
V
V
K
K
M
M
L
L
N
N
V
V
T
T
A
A
490
|
P
P
T
T
P
P
Q
Q
Q
Q
L
L
Q
Q
A
A
F
F
K
K
500
|
N
N
E
E
V
V
G
G
V
V
L
L
R
R
K
K
T
T
R
R
510
|
H
H
V
V
N
N
I
I
L
L
L
L
F
F
M
M
G
G
Y
Y
520
|
S
S
T
T
K
K
P
P
Q
Q
L
L
A
A
I
I
V
V
T
T
530
|
Q
Q
W
W
C
C
E
E
G
G
S
S
S
S
L
L
Y
Y
H
H
540
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H
H
L
L
H
H
I
I
I
I
E
E
T
T
K
K
F
F
E
E
550
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M
M
I
I
K
K
L
L
I
I
D
D
I
I
A
A
R
R
Q
Q
560
|
T
T
A
A
Q
Q
G
G
M
M
D
D
Y
Y
L
L
H
H
A
A
570
|
K
K
S
S
I
I
I
I
H
H
R
R
D
D
L
L
K
K
S
S
580
|
N
N
N
N
I
I
F
F
L
L
H
H
E
E
D
D
L
L
T
T
590
|
V
V
K
K
I
I
G
G
D
D
F
F
G
G
L
L
A
A
T
T
600
|
V
E
K
K
S
S
R
R
W
W
S
S
G
G
S
S
H
H
Q
Q
610
|
F
F
E
E
Q
Q
L
L
S
S
G
G
S
S
I
I
L
L
W
W
620
|
M
M
A
A
P
P
E
E
V
V
I
I
R
R
M
M
Q
Q
D
D
630
|
K
K
N
N
P
P
Y
Y
S
S
F
F
Q
Q
S
S
D
D
V
V
640
|
Y
Y
A
A
F
F
G
G
I
I
V
V
L
L
Y
Y
E
E
L
L
650
|
M
M
T
T
G
G
Q
Q
L
L
P
P
Y
Y
S
S
N
N
I
I
660
|
N
N
N
N
R
R
D
D
Q
Q
I
I
I
I
F
F
M
M
V
V
670
|
G
G
R
R
G
G
Y
Y
L
L
S
S
P
P
D
D
L
L
S
S
680
|
K
K
V
V
R
R
S
S
N
N
C
C
P
P
K
K
A
A
M
M
690
|
K
K
R
R
L
L
M
M
A
A
E
E
C
C
L
L
K
K
K
K
700
|
K
K
R
R
D
D
E
E
R
R
P
P
L
L
F
F
P
P
Q
Q
710
|
I
I
L
L
A
A
S
S
I
I
E
E
L
L
L
L
A
A
R
R
720
|
S
S
L
L
P
P
K
K
I
I
H
H
R
R
Click to Show/Hide the Structure
Experimental Note Revealed Based on the Cell Line Data
In Vitro Model HT29 Cells Colon Homo sapiens (Human) CVCL_A8EZ
SW620 cells Colon Homo sapiens (Human) CVCL_0547
HCT116 cells Colon Homo sapiens (Human) CVCL_0291
A375 cells Skin Homo sapiens (Human) CVCL_0132
HCC827 cells Lung Homo sapiens (Human) CVCL_2063
A431 cells Skin Homo sapiens (Human) CVCL_0037
COLO205 cells Colon Homo sapiens (Human) CVCL_F402
WiDR cells Colon Homo sapiens (Human) CVCL_2760
Ba/F3 cells Colon Homo sapiens (Human) CVCL_0161
SkMEL28 cells Skin Homo sapiens (Human) CVCL_0526
In Vivo Model Female NOD/SCID and BALB/c nude mouse xenograft model Mus musculus
Experiment for
Molecule Alteration		 Western blot analysis
Experiment for
Drug Resistance		 CellTiter-Glo assay; Tumor volume measurement assay
References
Ref 1 BGB-283, a Novel RAF Kinase and EGFR Inhibitor, Displays Potent Antitumor Activity in BRAF-Mutated Colorectal CancersMol Cancer Ther. 2015 Oct;14(10):2187-97. doi: 10.1158/1535-7163.MCT-15-0262. Epub 2015 Jul 24.

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