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. 2016 Jul 20;7(49):81926–81968. doi: 10.18632/oncotarget.10745

Table 5. Cell Cycle Control S/TK Inhibitors With Anti-MM Activity.

Compound Route Structure Kinase(s) Inhibited (IC50 in nM)a References/ Clinical Trials
Alisertib (MLN8237)* Oral graphic file with name oncotarget-07-81926-i092.jpg AURKA/B (1.2/396.5) [350-353]; NCT01034553
AT9283* IV graphic file with name oncotarget-07-81926-i093.jpg AURKA/B(3.0/3.0); JAK2/3 (1.2/1.1) [354, 355]; NCT01145989
Barasertib (AZD1152)* Oral graphic file with name oncotarget-07-81926-i094.jpg AURKA/B (1368/ 0.37) [356, 357]
Danusertib (PHA739358)* IV graphic file with name oncotarget-07-81926-i095.jpg AURKA/B (13/79); ABL (25); FGFR1 (47) [358, 359]; NCT00872300
ENMD-2076 Oral graphic file with name oncotarget-07-81926-i096.jpg AURKA/B (15/290); FLT3 (1.86); VEGFR2 (58.2) [360-363]; NCT00806065
Tozasertib (VE-465, VX-680, MK 0457)* IV graphic file with name oncotarget-07-81926-i097.jpg AURKA/B (0.6/18)b; BCR-ABL (30)b; FLT3 (30)b [364, 365]
Alvocidib (Flavopiridol)* IV graphic file with name oncotarget-07-81926-i098.jpg CDK1/2/4/6 (40/40/ 40/40) [366, 367]
AT7519* Oral graphic file with name oncotarget-07-81926-i099.jpg CDK1/2/4/5/6/9 (210/47/100/13/170/<10) [368, 369]
Dinaciclib* IV graphic file with name oncotarget-07-81926-i100.jpg CDK1/2/5/9 (3/1/1/4) [370, 371]; NCT01711528
LCQ195/ AT9311 NA graphic file with name oncotarget-07-81926-i101.jpg CDK1/2/3/5/9 (2/2/ 42/1/15) [372]
P276-00* IV graphic file with name oncotarget-07-81926-i102.jpg CDK1/4/9 (79/63/20) [373, 374]
Palbociclib* Oral graphic file with name oncotarget-07-81926-i103.jpg CDK4/6 (11/16) [375, 376]; NCT02030483; NCT00555906
PHA-767491* NA graphic file with name oncotarget-07-81926-i104.jpg CDK9 (34); CDC7 (10) [152, 377]
RGB-286638 IV graphic file with name oncotarget-07-81926-i105.jpg CDK1/2/3/4/5/6/7/9 (2/3/5/4/5/55/44/1); JAK2 (50); AMPK (41); GSK3beta (3) [378]
Seliciclib (CYC202, R-roscovitine)* Oral graphic file with name oncotarget-07-81926-i106.jpg CDK2/5 (700/160) [379, 380]
SNS-032 IV graphic file with name oncotarget-07-81926-i107.jpg CDK2/7/9 (38/62/4) [381, 382]
TG02 (SB1317) Oral graphic file with name oncotarget-07-81926-i108.jpg CDK2 (13); JAK2 (73); FLT3 (56); ERK5 (NA) [383, 384]; NCT01204164
89S Oral graphic file with name oncotarget-07-81926-i109.jpg CDC7 (2) [153]
BI 2536 NA graphic file with name oncotarget-07-81926-i110.jpg PLK1/2/3 (0.83/3.5/ 9.0) [157, 158, 385]
Scytonemin NA graphic file with name oncotarget-07-81926-i111.jpg PLK1 (2000) [159, 386]
KU55933* NA graphic file with name oncotarget-07-81926-i112.jpg ATM (12.9) [165, 387]
AZD7762* IV graphic file with name oncotarget-07-81926-i113.jpg CHK1/2 (5/<10) [162, 388]
NU7026* NA graphic file with name oncotarget-07-81926-i114.jpg DNA-PKcs (230) [165, 389, 390]

NA = Information not available;

*

ATP-competitive inhibitor;

a

as determined in cell-free assays;

b

Ki in nM