Details of the Drug

General Information of Drug (ID: DMYLT67)

Drug Name
TKI258
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
Indication
Disease Entry ICD 11 Status REF
Renal cell carcinoma 2C90 Phase 3 [1]
Endometrial cancer 2C76 Phase 2 [2]
Triple negative breast cancer 2C60-2C65 Phase 2 [3]
Therapeutic Class
Anticancer Agents
Drug Type
Small molecular drug
Structure
3D MOL is unavailable 2D MOL
#Ro5 Violations (Lipinski):
2		 Molecular Weight 500.5
Logarithm of the Partition Coefficient Not Available
Rotatable Bond Count 3
Hydrogen Bond Donor Count 6
Hydrogen Bond Acceptor Count 10
Chemical Identifiers
Formula
C24H29FN6O5
IUPAC Name
4-amino-5-fluoro-3-[6-(4-methylpiperazin-1-yl)-1H-benzimidazol-2-yl]-1H-quinolin-2-one;2-hydroxypropanoic acid;hydrate
Canonical SMILES
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
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
Cross-matching ID
PubChem CID
135611162
CAS Number
915769-50-5
UNII
I35H55G906
DrugBank ID
DB05928
TTD ID
D07OZR
INTEDE ID
DR1815
Combinatorial Drugs (CBD) Click to Jump to the Detailed CBD Information of This Drug
Repurposed Drugs (RPD) Click to Jump to the Detailed RPD Information of This Drug

Molecular Interaction Atlas of This Drug


Drug Therapeutic Target (DTT)
DTT Name DTT ID UniProt ID MOA REF
Fibroblast growth factor receptor 3 (FGFR3) TTST7KB FGFR3_HUMAN Inhibitor [4]
Platelet-derived growth factor receptor (PDGFR) TTI2WET NOUNIPROTAC Inhibitor [4]

Drug-Metabolizing Enzyme (DME)
DME Name DME ID UniProt ID MOA REF
Cytochrome P450 1A2 (CYP1A2)
Main DME 		DEJGDUW CP1A2_HUMAN Substrate [5]
Molecular Interaction Atlas (MIA) Jump to Detail Molecular Interaction Atlas of This Drug

Molecular Expression Atlas of This Drug

The Studied Disease Renal cell carcinoma
ICD Disease Classification 2C90
Molecule Name Molecule Type Gene Name p-value Fold-Change Z-score
Fibroblast growth factor receptor 3 (FGFR3) DTT FGFR3 5.83E-03 0.08 0.1
Cytochrome P450 1A2 (CYP1A2) DME CYP1A2 7.36E-01 1.62E-02 1.08E-01
Molecular Expression Atlas (MEA) Jump to Detail Molecular Expression Atlas of This Drug

Experimental Cancer Drug Sensitivity Information

Cancer Drug Sensitivity Data Curated from 10 Cell Line(s) in Autonomic Ganglia Tissue
Cell Line Original Dataset IC50 IC90 EC50 AUC
IMR-32 CCLE 1.3577 2.9581 1.219 14.728
SK-N-SH CCLE 1.7608 3.8813 1.3355 12.6683
KP-N-SI9s CCLE 2.232 4.9259 1.3406 11.1032
SK-N-DZ CCLE 2.3719 3.8604 1.977 7.3335
SiMa CCLE 2.4124 4.0309 1.9393 7.3985
SK-N-BE(2) CCLE 2.5832 3.8014 2.2149 5.4187
CHP-212 CCLE 2.8892 4.5439 2.1339 4.976
SK-N-FI CCLE 2.9045 4.6474 2.0954 5.1442
Kelly CCLE 3.4358 5.6427 2.0219 4.3089
SK-N-AS CCLE 3.5405 5.9174 1.9635 4.4056
⏷ Show the Full List of 10 Cancer Drug Sensitivity Data of This Drug
Cancer Drug Sensitivity Data Curated from 1 Cell Line(s) in Biliary Tract Tissue
Cell Line Original Dataset IC50 IC90 EC50 AUC
HuCC-T1 CCLE 3.4706 6.5792 1.5859 6.566
Cancer Drug Sensitivity Data Curated from 11 Cell Line(s) in Bone Tissue
Cell Line Original Dataset IC50 IC90 EC50 AUC
SK-ES-1 CCLE 1.1502 4.1303 0.5901 18.5297
CAL-78 CCLE 1.4506 4.8021 0.6196 17.3379
SaOS-2 CCLE 1.9115 5.8576 0.5868 16.0194
MG-63 CCLE 2.3569 4.1282 1.8392 8.0969
TC-71 CCLE 2.3843 3.2829 2.2341 5.9913
U2OS CCLE 2.5845 4.8979 1.6859 8.2263
MHH-ES-1 CCLE 2.7557 4.7579 1.91 6.5433
A-673 CCLE 2.9254 5.7851 1.5448 8.0709
SW1353 CCLE 3.3225 6.6264 1.448 7.6362
HOS CCLE 3.8021 5.9678 2.1195 3.1052
SJSA-1 CCLE 3.9321 7.5671 1.4389 6.3952
⏷ Show the Full List of 11 Cancer Drug Sensitivity Data of This Drug
Cancer Drug Sensitivity Data Curated from 29 Cell Line(s) in Breast Tissue
Cell Line Original Dataset IC50 IC90 EC50 AUC
MDA-MB-468 CCLE 1.3976 4.2537 0.8006 16.6124
Hs 739.T CCLE 1.4087 4.8576 0.5523 17.8169
Hs 578T CCLE 1.8218 3.9102 1.3877 12.1936
BT-549 CCLE 1.9009 4.2521 1.323 12.2514
MDA-MB-157 CCLE 1.9833 3.9616 1.5343 10.8974
MDA-MB-415 CCLE 2.1752 3.2244 2.0299 7.7547
ZR-75-1 CCLE 2.2906 4.6502 1.5286 9.9331
MCF-7 CCLE 2.4242 3.5032 2.1875 6.0826
HCC1806 CCLE 2.688 4.0966 2.174 5.3176
MDA-MB-436 CCLE 2.7854 5.7629 1.4359 9.0223
AU565 CCLE 2.8265 6.467 1.1198 10.6139
HMC-1-8 CCLE 2.8328 4.3785 2.1669 4.9479
MDA-MB-453 CCLE 2.9223 5.5147 1.6773 7.3622
HCC1395 CCLE 3.0713 6.9271 1.0955 10.1247
HCC70 CCLE 3.1649 7.2946 0.9885 10.4657
SK-BR-3 CCLE 3.2329 5.1042 2.1351 4.1378
EFM-19 CCLE 3.3054 6.6337 1.4309 7.7672
HCC1187 CCLE 3.3709 5.9486 1.8222 5.5161
T-47D CCLE 3.4426 5.8149 1.9423 4.7196
MDA-MB-175-VII CCLE 3.451 6.0533 1.831 5.2966
CAMA-1 CCLE 3.5212 8.1878 0.8266 10.4829
HCC1954 CCLE 3.5964 5.5756 2.1689 3.2178
ZR-75-30 CCLE 3.8447 13.6489 -1.6379 20.8417
BT-474 CCLE 3.9074 7.0729 1.6612 5.2814
CAL-85-1 CCLE 3.994 7.2604 1.6305 5.2793
HDQ-P1 CCLE 4.0983 7.4524 1.6092 5.1986
HCC1569 CCLE 4.3476 8.562 1.2461 6.6089
BT-20 CCLE 4.6796 6.9974 2.1666 1.678
UACC-812 CCLE 5.4651 7.046 2.4897 0.1977
⏷ Show the Full List of 29 Cancer Drug Sensitivity Data of This Drug
Cancer Drug Sensitivity Data Curated from 30 Cell Line(s) in Central Nervous System Tissue
Cell Line Original Dataset IC50 IC90 EC50 AUC
42-MG-BA CCLE 0.8452 2.4617 0.7705 18.8349
1321N1 CCLE 1.1618 5.1273 0.1807 20.498
8-MG-BA CCLE 1.3394 6.077 -0.0737 21.1271
H4 CCLE 1.3643 4.0065 0.8661 16.4045
T98G CCLE 1.3886 3.9213 0.9257 16.0235
LN-18 CCLE 1.4188 4.4002 0.7611 16.7357
GB-1 CCLE 1.4603 4.0838 0.9364 15.7155
SF126 CCLE 1.5146 3.8699 1.0798 14.8114
SW1088 CCLE 2.0123 5.1401 1.0261 13.43
A-172 CCLE 2.0304 5.7432 0.7553 14.7856
M059J CCLE 2.0414 3.981 1.586 10.4378
SF295 CCLE 2.5557 7.1881 0.5251 14.4696
Hs 683 CCLE 2.6547 4.5393 1.9266 6.7368
KNS-81 CCLE 2.6576 6.5159 0.9491 11.9712
U-118MG CCLE 2.8705 5.7112 1.5351 8.2645
YKG-1 CCLE 2.9003 5.5503 1.6408 7.6159
GaMG CCLE 2.9698 5.0917 1.9289 5.8795
LN-229 CCLE 2.9997 5.6116 1.6939 7.0771
KNS-42 CCLE 3.009 5.4772 1.7689 6.648
DBTRG-05MG CCLE 3.1061 5.1467 2.0137 5.0862
GI-1 CCLE 3.19 6.297 1.5071 7.6263
CAS-1 CCLE 3.3929 6.4818 1.5747 6.7965
U-87MG ATCC CCLE 3.429 5.7001 1.9887 4.5002
KALS-1 CCLE 3.4479 6.3221 1.6958 6.0266
ONS-76 CCLE 3.5305 6.7438 1.5497 6.6301
GMS-10 CCLE 3.596 6.565 1.6865 5.7632
Daoy CCLE 3.6142 7.5047 1.2368 8.1159
KNS-60 CCLE 3.7508 9.3796 0.4123 12.0875
DK-MG CCLE 3.7947 9.1837 0.5429 11.3311
MOG-G-CCM CCLE 4.4861 7.6065 1.7859 3.6698
⏷ Show the Full List of 30 Cancer Drug Sensitivity Data of This Drug
Cancer Drug Sensitivity Data Curated from 19 Cell Line(s) in Endometrium Tissue
Cell Line Original Dataset IC50 IC90 EC50 AUC
ESS-1 CCLE 1.0137 2.6848 0.9095 17.5213
MFE-296 CCLE 1.3092 4.057 0.7877 16.9884
JHUEM-2 CCLE 1.5854 3.7264 1.2112 13.909
HEC-251 CCLE 1.726 5.8703 0.4019 17.5391
MFE-319 CCLE 1.9974 5.4916 0.8445 14.4228
AN3-CA CCLE 2.0015 4.992 1.0854 13.1541
RL95-2 CCLE 2.1138 5.9567 0.7308 14.662
HEC-151 CCLE 2.2195 5.0989 1.2457 11.6417
HEC-265 CCLE 2.6518 4.2569 2.0621 6.0207
HEC-6 CCLE 2.9275 4.2875 2.2949 4.0052
HEC-1-A CCLE 3.0256 7.616 0.7133 12.2602
HEC-59 CCLE 3.0595 4.1689 2.4643 2.758
EN CCLE 3.3566 6.8853 1.346 8.1057
HEC-1-B CCLE 3.5022 6.1983 1.7976 6.2687
MFE-280 CCLE 3.6966 9.5943 0.2638 12.9499
EFE-184 CCLE 4.1756 7.6662 1.5589 5.318
KLE CCLE 4.232 7.6484 1.6049 4.984
TEN CCLE 4.9742 7.0921 2.2716 1.0043
Ishikawa (Heraklio) 02 ER- CCLE 1.6115 4.5074 0.9141 15.3063
⏷ Show the Full List of 19 Cancer Drug Sensitivity Data of This Drug
Cancer Drug Sensitivity Data Curated from 71 Cell Line(s) in Haematopoietic And Lymphoid Tissue Tissue
Cell Line Original Dataset IC50 IC90 EC50 AUC
Mono-Mac-1 CCLE -4.8423 -0.9315 -4.8852 65.83
KG-1 CCLE -0.9028 2.0983 -1.0513 34.1327
697 CCLE -0.294 0.9523 -0.2974 28.3039
F-36P CCLE -0.0373 2.1743 -0.1312 26.4961
JVM-3 CCLE 0.2003 2.6399 0.0348 24.7783
KO52 CCLE 0.3488 3.5123 -0.0479 24.5657
SIG-M5 CCLE 0.3556 2.1235 0.2975 22.9646
OCI-AML-5 CCLE 0.4561 4.9856 -0.4898 26.1581
KE-97 CCLE 0.553 2.6172 0.4235 21.59
Mino CCLE 0.7272 2.2336 0.6791 19.7294
Jurkat CCLE 0.7327 2.5913 0.6241 19.9531
KMS-11 CCLE 0.8499 7.4869 -1.2157 27.7273
MOLT-16 CCLE 1.075 2.4148 1.0252 16.7508
CMK-86 CCLE 1.0978 3.0733 0.9036 17.2151
Ku812 CCLE 1.1457 2.5763 1.0743 16.2403
NCO2 CCLE 1.1957 2.6536 1.1136 15.8591
SU-DHL-4 CCLE 1.2724 3.3752 1.0003 16.0878
ALL-SIL CCLE 1.3124 3.0897 1.133 15.3064
DoHH2 CCLE 1.3571 3.0009 1.2068 14.7871
EM-2 CCLE 1.4012 3.2928 1.1673 14.8031
HD-MY-Z CCLE 1.4177 3.3399 1.1697 14.7293
AMO1 CCLE 1.4617 2.7682 1.3784 13.5813
P12-Ichikawa CCLE 1.464 3.6779 1.0998 14.8956
Pfeiffer CCLE 1.4854 3.7212 1.1063 14.7858
OCI-AML-2 CCLE 1.5188 2.768 1.4404 13.069
RPMI-8402 CCLE 1.5341 3.8052 1.1259 14.5136
Reh CCLE 1.5398 3.2523 1.331 13.4972
SU-DHL-10 CCLE 1.5563 2.5926 1.5141 12.5843
Kasumi-2 CCLE 1.5615 2.7332 1.494 12.6531
BL-70 CCLE 1.5759 3.4017 1.3202 13.4127
MEG-01 CCLE 1.6186 3.9478 1.1586 14.051
L-363 CCLE 1.7536 3.057 1.6238 11.2922
KMS-26 CCLE 1.7699 5.2874 0.7193 15.7822
Granta-519 CCLE 1.7859 4.4475 1.1191 13.6774
DEL CCLE 1.8203 2.9587 1.7236 10.5663
P31/FUJ CCLE 1.8227 6.0349 0.4166 17.1621
BL-41 CCLE 1.9712 4.1216 1.4524 11.355
KCL-22 CCLE 2.0483 3.295 1.8682 9.0079
SU-DHL-8 CCLE 2.0551 2.9667 1.9777 8.4626
MEC-1 CCLE 2.0739 5.2501 1.0335 13.2009
SU-DHL-6 CCLE 2.2222 3.1487 2.1063 7.2117
HuT 78 CCLE 2.3021 4.525 1.5992 9.5257
L-428 CCLE 2.3989 4.8439 1.5392 9.5495
KMS-34 CCLE 2.496 4.5665 1.7653 8.0597
BDCM CCLE 2.6595 6.1603 1.1278 11.0136
SK-MM-2 CCLE 2.6792 6.3763 1.0376 11.4419
Ci-1 CCLE 2.6848 3.2888 2.5496 3.3585
U-937 CCLE 2.7341 5.0658 1.7379 7.5306
MOLP-8 CCLE 2.8609 5.3912 1.6866 7.4703
Karpas-422 CCLE 3.2898 5.222 2.1203 4.0924
KMM-1 CCLE 3.3444 6.0091 1.7719 5.8447
HEL 92.1.7 CCLE 3.3849 5.7922 1.9102 5.0137
Karpas-299 CCLE 3.5402 7.1268 1.3677 7.5802
Raji CCLE 3.652 5.684 2.1548 3.189
Karpas-620 CCLE 3.7798 8.7379 0.7522 10.2933
KHM-1B CCLE 3.7821 5.655 2.2539 2.4606
SUP-M2 CCLE 3.7961 6.2714 1.9708 3.8792
Toledo CCLE 3.8384 6.8969 1.6983 5.2189
P3HR-1 CCLE 4.0442 8.8193 0.9081 8.9322
KMS-12-BM CCLE 4.0463 5.9381 2.2841 1.921
EB2 CCLE 4.369 6.4192 2.2514 1.6627
MC116 CCLE 4.5266 5.6008 2.6505 0.1809
HT CCLE 4.732 5.8893 2.6252 0.1657
SUP-T1 CCLE 4.7633 6.9288 2.2378 1.3079
HH [Human lymphoma] CCLE 5.0236 7.2902 2.2149 1.1656
OPM-2 CCLE 5.3505 6.675 2.5761 0.1038
EB1 CCLE 5.4554 7.5452 2.3054 0.5957
LP-1 CCLE 5.4829 7.0025 2.5111 0.1617
OCI-Ly10 CCLE 5.5628 7.9333 2.2032 0.8237
JM-1 CCLE 5.7795 7.3908 2.4835 0.1407
MJ CCLE 5.864 8.4472 2.1347 0.8471
⏷ Show the Full List of 71 Cancer Drug Sensitivity Data of This Drug
Cancer Drug Sensitivity Data Curated from 9 Cell Line(s) in Kidney Tissue
Cell Line Original Dataset IC50 IC90 EC50 AUC
KMRC-1 CCLE 1.3039 4.8148 0.4636 18.6166
769-P CCLE 1.5492 5.9032 0.2139 19.043
ACHN CCLE 2.4643 6.0768 0.9952 12.2577
BFTC-909 CCLE 2.5564 7.5635 0.3388 15.4199
VMRC-RCW CCLE 2.6466 4.0279 2.1684 5.4702
Caki-2 CCLE 2.8129 5.5619 1.56 8.2802
VMRC-RCZ CCLE 2.9262 4.1357 2.3695 3.6043
786-O CCLE 3.4562 7.4665 1.1346 9.0074
KMRC-2 CCLE 3.4699 5.6238 2.0561 4.0575
⏷ Show the Full List of 9 Cancer Drug Sensitivity Data of This Drug
Cancer Drug Sensitivity Data Curated from 24 Cell Line(s) in Large Intestine Tissue
Cell Line Original Dataset IC50 IC90 EC50 AUC
SW48 CCLE 1.3318 2.8961 1.2068 14.8873
COLO 320 CCLE 1.7622 4.8204 0.9273 14.7387
SW620 CCLE 1.8239 3.6738 1.4855 11.6985
HCT 15 CCLE 1.9087 4.1567 1.3729 11.9705
LS513 CCLE 1.9661 4.8525 1.1158 13.1078
HT-29 CCLE 2.2093 4.4427 1.5469 10.0907
COLO205 CCLE 2.3019 4.3445 1.684 9.0815
RKO CCLE 2.4969 3.9457 2.0624 6.4884
COLO201 CCLE 2.7584 4.4747 2.0527 5.7673
HCT 116 CCLE 2.8371 4.4509 2.1347 5.1106
LS411N CCLE 2.8918 5.3366 1.7404 7.0992
SK-CO-1 CCLE 2.9972 5.4294 1.783 6.6011
SW403 CCLE 3.1172 4.9738 2.109 4.5441
SW1417 CCLE 3.3394 6.8751 1.3375 8.1908
C2BBe1 CCLE 3.3802 5.8488 1.8787 5.1926
HCC-56 CCLE 3.4816 6.0673 1.8469 5.1472
SNU-C2B CCLE 3.4845 6.2085 1.7795 5.5009
CCK-81 CCLE 3.6697 5.9267 2.0502 3.6995
COLO 678 CCLE 3.6915 7.115 1.4865 6.6277
SW480 CCLE 3.7359 6.7702 1.6874 5.4755
SNU-C2A CCLE 4.6347 7.655 1.8524 3.1369
LS123 CCLE 5.0843 6.8536 2.4122 0.501
NCI-H747 CCLE 5.1494 7.3467 2.2502 0.9469
T84 CCLE 5.5658 7.3775 2.4103 0.3085
⏷ Show the Full List of 24 Cancer Drug Sensitivity Data of This Drug
Cancer Drug Sensitivity Data Curated from 19 Cell Line(s) in Liver Tissue
Cell Line Original Dataset IC50 IC90 EC50 AUC
JHH-7 CCLE 0.7396 3.1993 0.4759 20.6095
SK-HEP-1 CCLE 1.1731 3.3967 0.8854 17.0122
HuH-1 CCLE 1.2526 4.2996 0.6295 17.9716
Hep 3B2.1-7 CCLE 1.2587 3.3612 0.9901 16.1886
HLF CCLE 1.7199 3.8333 1.3118 12.9306
HLE CCLE 1.9301 5.8199 0.6226 15.7782
SNU-398 CCLE 2.0802 4.7007 1.2992 11.7915
SNU-475 CCLE 2.4742 6.7183 0.6863 13.8575
Hep-G2 CCLE 2.4935 5.2644 1.4222 9.8978
JHH-2 CCLE 2.8242 5.0223 1.8389 6.7431
PLC/PRF/5 CCLE 3.0371 6.4289 1.3163 9.0244
Hep-G2/C3A CCLE 3.5356 5.3604 2.2308 3.0086
SNU-182 CCLE 3.7447 6.4465 1.851 4.5985
SNU-449 CCLE 3.7556 6.5741 1.7968 4.8618
SNU-423 CCLE 3.7726 7.0773 1.5639 6.0538
JHH-6 CCLE 3.8236 7.3574 1.4637 6.4794
JHH-4 CCLE 3.9306 5.9526 2.2083 2.4521
JHH-5 CCLE 3.9654 8.5007 1.0068 8.583
SNU-387 CCLE 5.0441 7.0975 2.3012 0.8536
⏷ Show the Full List of 19 Cancer Drug Sensitivity Data of This Drug
Cancer Drug Sensitivity Data Curated from 94 Cell Line(s) in Lung Tissue
Cell Line Original Dataset IC50 IC90 EC50 AUC
NCI-H2286 CCLE 0.3164 2.9653 0.0807 24.1026
CAL-12T CCLE 0.7218 4.1586 0.1234 22.3458
Lu-99 CCLE 0.8633 3.3289 0.5707 19.6868
NCI-H1703 CCLE 0.9449 3.3983 0.6371 19.0604
LOU-NH91 CCLE 1.1726 5.8233 -0.122 21.9155
SK-MES-1 CCLE 1.1871 3.6908 0.7977 17.3823
NCI-H520 CCLE 1.5555 4.9837 0.6451 16.8581
NCI-H322 CCLE 1.6429 6.1395 0.1934 18.8441
NCI-H2122 CCLE 1.6645 3.4011 1.4162 12.619
A-549 CCLE 1.6754 3.2224 1.4881 12.2335
NCI-H1048 CCLE 1.7722 5.2996 0.7159 15.7928
PC-14 CCLE 1.8423 4.5349 1.1374 13.3968
NCI-H1155 CCLE 1.8518 4.7036 1.0705 13.7099
COLO 699 CCLE 1.8651 5.1533 0.8758 14.6732
NCI-H1341 CCLE 1.9653 5.2135 0.9456 13.9957
COLO 677 CCLE 2.0128 4.3017 1.4149 11.4087
SBC-5 CCLE 2.0335 3.1186 1.9107 8.8605
SK-LU-1 CCLE 2.0413 5.999 0.6421 15.3393
NCI-H2030 CCLE 2.1154 4.1119 1.604 10.098
NCI-H1792 CCLE 2.1254 3.7263 1.782 9.158
GLC-82 CCLE 2.1471 6.1106 0.6871 14.7907
RERF-LC-A1 CCLE 2.198 5.1813 1.1856 12.0236
DMS 114 CCLE 2.2375 5.2168 1.2061 11.7961
NCI-H1299 CCLE 2.2605 5.6601 1.0126 12.7503
NCI-H1581 CCLE 2.2619 3.8173 1.8841 8.1751
NCI-H23 CCLE 2.2687 4.0914 1.7681 8.7495
NCI-H2023 CCLE 2.3093 4.1359 1.7883 8.514
NCI-H211 CCLE 2.36 3.6376 2.0635 6.9303
NCI-H358 CCLE 2.4763 6.8851 0.6055 14.2722
NCI-H2228 CCLE 2.4913 6.1787 0.9691 12.3208
VMRC-LCD CCLE 2.5749 4.9325 1.6601 8.3921
NCI-H1915 CCLE 2.5865 5.859 1.2128 10.7576
NCI-H1650 CCLE 2.7015 5.3023 1.5915 8.4079
SW1573 CCLE 2.7223 7.7495 0.39 14.7124
NCI-H1975 CCLE 2.7391 5.5454 1.5038 8.7794
Hs 229.T CCLE 2.7468 4.632 1.9644 6.2747
NCI-H1563 CCLE 2.7504 5.34 1.616 8.1438
Calu-6 CCLE 2.7512 5.0683 1.7519 7.4085
NCI-H2009 CCLE 2.7554 5.8084 1.3871 9.3648
NCI-H1651 CCLE 2.772 4.8143 1.8964 6.5724
HCC15 CCLE 2.8207 4.6428 2.0248 5.7483
NCI-H2087 CCLE 2.9484 6.4524 1.2306 9.7072
Calu-1 CCLE 2.9923 4.8941 2.0465 5.1859
NCI-H2172 CCLE 3.0018 7.1582 0.9224 11.219
NCI-H226 CCLE 3.0118 6.8486 1.0855 10.3254
T3M-10 CCLE 3.0429 4.7158 2.1776 4.3504
NCI-H1666 CCLE 3.0486 6.7579 1.1614 9.828
NCI-H1355 CCLE 3.0598 6.2742 1.4125 8.4504
LUDLU-1 CCLE 3.0607 7.3948 0.853 11.4386
NCI-H1092 CCLE 3.0679 6.5096 1.3014 9.0289
HARA [Human squamous cell lung carcinoma] CCLE 3.0758 6.2519 1.4368 8.2799
NCI-H460 CCLE 3.0882 4.6706 2.237 3.9198
NCI-H1373 CCLE 3.1271 4.5112 2.3476 3.2315
MOR/CPR CCLE 3.1681 7.7862 0.7455 11.7391
NCI-H810 CCLE 3.2792 5.7429 1.8537 5.5502
LCLC-103H CCLE 3.301 7.8783 0.807 11.0973
Sq-1 CCLE 3.3071 8.971 0.2664 13.8519
NCI-H441 CCLE 3.3117 6.0714 1.7157 6.2207
Calu-3 CCLE 3.326 5.4783 2.021 4.5471
NCI-H1693 CCLE 3.3264 6.4503 1.5387 7.1398
NCI-H1694 CCLE 3.3626 5.9039 1.8381 5.449
KNS-62 CCLE 3.3829 5.5219 2.0422 4.3113
HCC4006 CCLE 3.4084 6.2891 1.6822 6.1857
COR-L23 CCLE 3.4251 6.7416 1.4706 7.2837
NCI-H1793 CCLE 3.4567 8.0471 0.8462 10.5278
DV-90 CCLE 3.4677 8.6853 0.5371 12.1021
NCI-H1573 CCLE 3.5773 5.5668 2.1601 3.2995
SHP-77 CCLE 3.5865 7.0424 1.4444 7.0721
NCI-H1339 CCLE 3.6403 6.0794 1.9558 4.2498
NCI-H661 CCLE 3.6698 5.7191 2.15 3.1816
HCC44 CCLE 3.6894 6.9298 1.5759 6.1586
COR-L105 CCLE 3.6908 7.6187 1.238 7.9451
RERF-LC-MS CCLE 3.7564 5.6034 2.2617 2.4634
NCI-H1184 CCLE 3.7856 6.0881 2.0514 3.4823
LC-1/sq-SF CCLE 3.8114 7.382 1.4429 6.6132
NCI-H2444 CCLE 3.8219 5.7838 2.2189 2.571
NCI-H1648 CCLE 3.8274 5.8886 2.1733 2.7907
NCI-H1568 CCLE 3.8291 6.9868 1.6481 5.4995
NCI-H1869 CCLE 3.9589 7.5071 1.487 6.0921
NCI-H522 CCLE 4.044 7.5148 1.5423 5.6438
NCI-H1944 CCLE 4.1094 9.765 0.4917 10.9128
NCI-H727 CCLE 4.1754 6.2144 2.2344 1.9786
SW1271 CCLE 4.1769 6.4743 2.118 2.5235
NCI-H650 CCLE 4.1852 10.4531 0.2092 12.1454
HCC827 CCLE 4.1881 6.4478 2.1367 2.4184
NCI-H647 CCLE 4.3154 6.7322 2.0827 2.496
HCC78 CCLE 4.3405 7.6743 1.6633 4.5055
NCI-H2170 CCLE 4.3822 9.5058 0.8146 8.7378
EBC-1 CCLE 4.4035 7.3673 1.8456 3.5039
NCI-H3255 CCLE 4.6097 6.6421 2.2811 1.2842
HCC2935 CCLE 4.649 8.0368 1.6871 3.9044
IA-LM CCLE 5.0008 7.1098 2.2768 0.9662
NCI-H2085 CCLE 5.6333 7.9602 2.2228 0.7268
SW900 CCLE 5.6351 7.7157 2.3148 0.4882
⏷ Show the Full List of 94 Cancer Drug Sensitivity Data of This Drug
Cancer Drug Sensitivity Data Curated from 16 Cell Line(s) in Oesophagus Tissue
Cell Line Original Dataset IC50 IC90 EC50 AUC
TE-15 CCLE 0.6331 3.2578 0.3422 21.6478
TE-11 CCLE 0.6777 3.5142 0.3086 21.6344
KYSE-140 CCLE 1.2771 4.9232 0.3886 19.0806
KYSE-70 CCLE 1.298 4.7602 0.4814 18.5483
OE21 CCLE 2.0211 4.6111 1.2822 12.0681
KYSE-180 CCLE 2.1266 4.1209 1.6114 10.0232
TE-9 CCLE 3.065 6.0352 1.5362 7.7696
TE-1 CCLE 3.1226 6.0277 1.5871 7.3549
KYSE-150 CCLE 3.1655 5.4117 1.9291 5.4036
KYSE-510 CCLE 3.1785 6.5151 1.3889 8.2902
OE33 CCLE 3.3604 5.4426 2.0645 4.24
KYSE-520 CCLE 3.4601 6.287 1.7224 5.858
KYSE-450 CCLE 3.5903 6.8367 1.5486 6.5091
TE-5 CCLE 3.7816 6.9289 1.6427 5.621
KYSE-30 CCLE 3.802 6.9859 1.6294 5.6506
KYSE-410 CCLE 4.1431 6.5492 2.0634 2.8368
⏷ Show the Full List of 16 Cancer Drug Sensitivity Data of This Drug
Cancer Drug Sensitivity Data Curated from 29 Cell Line(s) in Ovary Tissue
Cell Line Original Dataset IC50 IC90 EC50 AUC
A2780 CCLE 0.5512 2.7311 0.3959 21.7228
FU-OV-1 CCLE 1.1877 6.744 -0.5355 23.7608
TOV-21G CCLE 1.2464 3.7079 0.8551 16.885
TOV-112D CCLE 1.8355 4.0122 1.3592 12.2898
SK-OV-3 CCLE 1.9081 5.4801 0.7637 15.118
DOV13 CCLE 2.0892 3.7896 1.7176 9.6074
HEY A8 CCLE 2.4241 6.0305 0.9816 12.4428
OVCAR-8 CCLE 2.5044 3.606 2.2255 5.6182
TYK-nu CCLE 2.5132 4.2445 1.9368 7.0985
IGROV-1 CCLE 2.5847 5.3621 1.4572 9.4522
OC 315 CCLE 2.6186 3.8193 2.2412 5.1705
JHOS-2 CCLE 2.7972 5.5605 1.5471 8.391
MCAS CCLE 2.8053 6.3363 1.1669 10.4171
OC 314 CCLE 2.8482 4.4012 2.1692 4.8941
COV318 CCLE 3.1088 6.4995 1.34 8.7211
OV-90 CCLE 3.1124 6.118 1.5337 7.6678
ONCO-DG-1 CCLE 3.1426 5.6825 1.7757 6.2872
EFO-21 CCLE 3.1757 7.4302 0.9296 10.7518
COV504 CCLE 3.2225 6.9219 1.2212 9.0866
OVTOKO CCLE 3.2441 6.5817 1.4083 8.0311
ES-2 CCLE 3.27 5.6275 1.9039 5.3004
OVCAR-4 CCLE 3.2986 5.8383 1.8213 5.6809
OC 316 CCLE 3.3755 5.7496 1.9242 4.9592
EFO-27 CCLE 3.5571 9.1631 0.3696 12.7432
OVMANA CCLE 3.6523 5.2296 2.3706 2.0879
OVCAR-3 CCLE 3.6638 8.0855 0.987 9.3253
Kuramochi CCLE 3.9127 7.6147 1.402 6.6266
JHOS-4 CCLE 3.9474 10.3183 0.0973 13.2016
OVSAHO CCLE 4.683 9.0843 1.2201 6.1506
⏷ Show the Full List of 29 Cancer Drug Sensitivity Data of This Drug
Cancer Drug Sensitivity Data Curated from 30 Cell Line(s) in Pancreas Tissue
Cell Line Original Dataset IC50 IC90 EC50 AUC
KCI-MOH1 CCLE 1.7181 4.4819 1.0346 14.3349
SUIT-2 CCLE 2.1787 3.8584 1.7807 8.9826
KP-4 CCLE 2.21 4.4175 1.5593 10.0232
MIA PaCa-2 CCLE 2.6083 3.8503 2.2164 5.3328
PK-1 CCLE 2.6147 5.484 1.4239 9.5477
BxPC-3 CCLE 2.6398 5.8541 1.2627 10.3442
SW1990 CCLE 2.7781 5.3058 1.6574 7.8463
PK-45H CCLE 2.839 5.9858 1.3709 9.2323
AsPC-1 CCLE 2.8435 4.9475 1.8929 6.4001
HPAC CCLE 2.8551 6.0581 1.3486 9.311
L3.3 CCLE 2.8792 6.035 1.3807 9.0756
HuP-T3 CCLE 2.9356 7.1931 0.8495 11.7716
HPAF-II CCLE 3.0414 4.8849 2.0919 4.8187
PaTu 8902 CCLE 3.0774 5.7445 1.6917 6.8984
HuP-T4 CCLE 3.107 4.8064 2.1844 4.1604
Panc 10.05 CCLE 3.1153 4.7125 2.2378 3.8518
Hs 766T CCLE 3.2128 6.0203 1.6633 6.7295
KP-3 CCLE 3.3306 5.8039 1.8631 5.3847
KP-1N CCLE 3.3591 6.3249 1.6266 6.5936
KP-2 CCLE 3.3643 6.1525 1.7161 6.1008
QGP-1 CCLE 3.4003 8.643 0.5048 12.4256
Capan-2 CCLE 3.4814 5.1066 2.3159 2.6664
Panc 03.27 CCLE 3.4889 5.3436 2.2064 3.2252
Panc 02.03 CCLE 3.4948 7.6091 1.0937 9.1377
PL45 CCLE 3.5621 5.5153 2.1744 3.2536
PK-59 CCLE 3.584 8.8992 0.5218 11.9116
KP-1NL CCLE 3.7165 7.5932 1.2697 7.7231
Panc 04.03 CCLE 3.9133 6.1942 2.0848 3.0939
SU.86.86 CCLE 4.0588 7.9117 1.3608 6.5572
PSN1 CCLE 4.6277 9.6645 0.9072 7.8121
⏷ Show the Full List of 30 Cancer Drug Sensitivity Data of This Drug
Cancer Drug Sensitivity Data Curated from 7 Cell Line(s) in Pleura Tissue
Cell Line Original Dataset IC50 IC90 EC50 AUC
IST-Mes2 CCLE 1.0931 3.2825 0.8355 17.5539
MSTO-211H CCLE 1.107 3.1103 0.903 17.1821
IST-Mes1 CCLE 2.2403 4.6458 1.4819 10.3334
NCI-H2452 CCLE 2.7631 6.6488 0.9746 11.5547
NCI-H2052 CCLE 3.1301 6.7737 1.2204 9.3125
NCI-H28 CCLE 3.2871 5.0043 2.2259 3.5319
MPP 89 CCLE 3.2903 6.2814 1.5945 6.9214
⏷ Show the Full List of 7 Cancer Drug Sensitivity Data of This Drug
Cancer Drug Sensitivity Data Curated from 3 Cell Line(s) in Prostate Tissue
Cell Line Original Dataset IC50 IC90 EC50 AUC
DU145 CCLE 1.5336 4.3237 0.913 15.5777
22Rv1 CCLE 2.4722 4.0194 2.0037 6.8736
PC-3 CCLE 3.4639 6.4071 1.6659 6.152
Cancer Drug Sensitivity Data Curated from 1 Cell Line(s) in Salivary Gland Tissue
Cell Line Original Dataset IC50 IC90 EC50 AUC
A-253 CCLE 3.7803 7.6075 1.3098 7.3784
Cancer Drug Sensitivity Data Curated from 41 Cell Line(s) in Skin Tissue
Cell Line Original Dataset IC50 IC90 EC50 AUC
HMCB CCLE 0.1289 2.9347 -0.1157 25.7467
IPC-298 CCLE 1.1209 4.5369 0.3929 19.6017
Hs 895.T CCLE 1.1708 5.3991 0.0687 21.0102
G-361 CCLE 1.1925 3.3959 0.9066 16.8376
CHL-1 CCLE 1.7974 4.4276 1.1397 13.5341
A-375 CCLE 1.8408 4.0791 1.3363 12.3869
Hs 944.T CCLE 2.0033 5.4446 0.8726 14.2581
WM793 CCLE 2.1754 5.7702 0.8794 13.7025
Malme-3M CCLE 2.1849 4.9617 1.2781 11.5758
Mel Ho CCLE 2.2336 2.9333 2.1808 6.818
A2058 CCLE 2.2786 3.6786 1.9616 7.7245
COLO 741 CCLE 2.4708 6.1857 0.9471 12.4942
SK-MEL-5 CCLE 2.513 5.631 1.2595 10.7124
WM88 CCLE 2.5656 6.2521 0.9991 11.9556
UACC-62 CCLE 2.6973 5.0103 1.7326 7.6595
HT-144 CCLE 2.7699 7.4832 0.5639 13.6943
SK-MEL-31 CCLE 2.8197 3.8706 2.4066 3.694
WM1799 CCLE 2.8554 7.2732 0.7417 12.5445
WM983B CCLE 2.8867 5.6178 1.5955 7.896
Hs 938.T CCLE 2.8946 4.4811 2.1699 4.7674
K029AX CCLE 2.9008 4.7131 2.0595 5.3485
IGR-37 CCLE 2.9997 4.109 2.4453 3.0067
COLO 679 CCLE 3.0043 5.4164 1.7953 6.5166
RPMI-7951 CCLE 3.0285 5.3204 1.8635 6.0875
LOX-IMVI CCLE 3.0834 5.8767 1.6305 7.2146
MDA-MB-435S CCLE 3.1244 4.387 2.4072 2.9154
Hs 294T CCLE 3.1319 5.6605 1.778 6.3004
IGR-39 CCLE 3.2384 5.4188 1.9831 4.9451
Hs 852.T CCLE 3.2587 6.2015 1.6094 6.9139
UACC-257 CCLE 3.2948 5.418 2.027 4.5828
Hs 936.T CCLE 3.3424 4.544 2.4914 2.0115
MeWo CCLE 3.3443 5.1898 2.1771 3.6718
SK-MEL-30 CCLE 3.4289 6.8607 1.4144 7.5761
RVH-421 CCLE 3.4367 5.6626 2.0128 4.3561
WM115 CCLE 3.4555 6.1103 1.8062 5.4192
SK-MEL-24 CCLE 3.4759 5.8728 1.9384 4.6711
WM266-4 CCLE 3.5916 7.7816 1.0826 8.981
WT2-iPS CCLE 3.7251 8.8383 0.6609 10.8831
Hs 695T CCLE 3.7544 8.3652 0.9173 9.4929
SK-MEL-2 CCLE 4.4124 5.3716 2.6889 0.1447
SF8657 CCLE 5.8532 15.0379 -0.8391 13.5813
⏷ Show the Full List of 41 Cancer Drug Sensitivity Data of This Drug
Cancer Drug Sensitivity Data Curated from 13 Cell Line(s) in Soft Tissue Tissue
Cell Line Original Dataset IC50 IC90 EC50 AUC
A-204 CCLE -0.6126 1.3498 -0.6433 31.1578
G-402 CCLE 1.228 3.1481 1.0238 16.146
SK-LMS-1 CCLE 1.2926 3.9153 0.8259 16.8595
G-401 CCLE 1.2997 2.9247 1.1644 15.2101
TE 617.T CCLE 2.0934 3.1914 1.9524 8.4339
GCT CCLE 2.3128 6.3062 0.7443 14.0101
KYM-1 CCLE 2.485 5.4541 1.3211 10.462
Rh30 CCLE 3.2631 5.9545 1.7359 6.2215
MES-SA CCLE 3.3244 5.5839 1.9674 4.8381
HT-1080 CCLE 3.3258 6.5416 1.4929 7.3876
Hs 729.T CCLE 3.3603 6.6984 1.4418 7.5834
RD CCLE 3.5299 6.0915 1.8705 4.9207
RKN CCLE 3.6886 7.2116 1.4368 6.8969
⏷ Show the Full List of 13 Cancer Drug Sensitivity Data of This Drug
Cancer Drug Sensitivity Data Curated from 20 Cell Line(s) in Stomach Tissue
Cell Line Original Dataset IC50 IC90 EC50 AUC
SNU-16 CCLE -1.2657 0.6657 -1.2794 36.6921
IM95 CCLE 0.0164 30.771 -13.4441 45.0186
Fu97 CCLE 0.6875 2.9195 0.4978 20.7116
AZ-521 CCLE 0.7803 3.974 0.256 21.4979
HGC-27 CCLE 1.0779 3.5757 0.721 18.1579
MKN45 CCLE 1.8586 4.7008 1.0786 13.6464
SNU-1 CCLE 2.2208 4.5057 1.5288 10.1486
BGC-823 CCLE 2.265 5.0331 1.3207 11.108
NCI-N87 CCLE 2.4973 4.3549 1.8686 7.5079
NUGC-4 CCLE 2.6302 4.7684 1.7914 7.5309
NUGC-3 CCLE 2.7845 4.6679 1.9803 6.0862
RERF-GC-1B CCLE 3.0805 6.439 1.3471 8.7519
GCIY CCLE 3.1656 4.8034 2.2324 3.7652
OCUM-1 CCLE 3.2304 5.9568 1.709 6.4423
KE-39 CCLE 3.4581 6.6532 1.5397 6.8406
Hs 746.T CCLE 3.4934 6.2252 1.7778 5.4908
SH-10-TC CCLE 3.8893 7.4512 1.4649 6.3429
MKN74 CCLE 3.8983 10.7344 -0.1464 14.4706
MKN7 CCLE 4.2798 7.2051 1.8443 3.7017
SNG-M CCLE 2.7379 5.4685 1.541 8.5817
⏷ Show the Full List of 20 Cancer Drug Sensitivity Data of This Drug
Cancer Drug Sensitivity Data Curated from 5 Cell Line(s) in Thyroid Tissue
Cell Line Original Dataset IC50 IC90 EC50 AUC
SW579 CCLE 0.5407 3.2464 0.2449 22.4612
TT2609-C02 CCLE 1.0551 3.4764 0.7306 18.1975
8505C CCLE 2.8842 5.0505 1.8768 6.3807
B-CPAP CCLE 2.9552 5.7615 1.5817 7.7962
8305C CCLE 3.014 5.8056 1.6089 7.5017
Cancer Drug Sensitivity Data Curated from 7 Cell Line(s) in Upper Aerodigestive Tract Tissue
Cell Line Original Dataset IC50 IC90 EC50 AUC
Hs 840.T CCLE 1.5154 4.5549 0.7946 16.2362
FaDu CCLE 1.7402 4.6222 0.9947 14.4656
CAL-27 CCLE 2.835 5.5103 1.6048 7.9797
SCC-25 CCLE 2.9287 5.1835 1.8482 6.4205
SCC-9 CCLE 2.9294 4.7196 2.0807 5.1596
Detroit 562 CCLE 3.5827 5.5996 2.1479 3.3529
HSC-2 CCLE 3.92 8.3923 1.0269 8.5724
⏷ Show the Full List of 7 Cancer Drug Sensitivity Data of This Drug
Cancer Drug Sensitivity Data Curated from 14 Cell Line(s) in Urinary Tract Tissue
Cell Line Original Dataset IC50 IC90 EC50 AUC
JMSU-1 CCLE -1.3468 0.7636 -1.3673 37.4157
RT-112 CCLE -0.2029 4.2472 -0.9008 30.4936
T24 CCLE 1.476 4.7822 0.6543 17.0771
HT-1376 CCLE 1.4811 6.4508 -0.1113 20.8424
639V CCLE 1.634 4.103 1.1107 14.2366
RT-4 CCLE 1.7731 7.7091 -0.4416 21.4584
SW780 CCLE 1.9169 5.6039 0.7133 15.3515
SCaBER CCLE 2.0675 5.1073 1.0953 12.8967
5637 CCLE 2.5033 4.9977 1.562 9.122
TCCSUP CCLE 2.6336 5.8908 1.2389 10.4889
J82 CCLE 3.085 6.0077 1.5664 7.5577
KMBC-2 CCLE 3.2418 6.7609 1.3171 8.5265
HT-1197 CCLE 4.0246 8.5429 1.0291 8.3468
UM-UC-3 CCLE 4.3953 8.0195 1.5361 5.053
⏷ Show the Full List of 14 Cancer Drug Sensitivity Data of This Drug

References

1 ClinicalTrials.gov (NCT01223027) Study of Dovitinib Versus Sorafenib in Patients With Metastatic Renal Cell Carcinoma. U.S. National Institutes of Health.
2 Phase 2 study of dovitinib in patients with metastatic or unresectable adenoid cystic carcinoma. Cancer. 2015 Aug 1;121(15):2612-7.
3 ClinicalTrials.gov (NCT01262027) TKI258 for Metastatic Inflammatory Breast Cancer Patients. U.S. National Institutes of Health.
4 A comparison of physicochemical property profiles of marketed oral drugs and orally bioavailable anti-cancer protein kinase inhibitors in clinical development. Curr Top Med Chem. 2007;7(14):1408-22.
5 A drug-drug interaction study to assess the effect of the CYP1A2 inhibitor fluvoxamine on the pharmacokinetics of dovitinib (TKI258) in patients with advanced solid tumors. Cancer Chemother Pharmacol. 2018 Jan;81(1):73-80.