Table 2. Small molecule inhibitors and their identified targets under current investigation for the treatment of pancreatic cancer.
| Compound | IC50 (μM) | Target |
| PD173074 (42) | 2.5 to 15 (AsPC-1, Capan-1, HPAF-II, MiaPaCa-2, and Panc 1) | FGFR1 tyrosine kinase; VEGFR2 |
| PKC412 (43) | 0.25 to 20 (16 pancreatic cancer cell lines) | Ser/Thr and tyrosine kinases |
| BGB324 (44) + gemcitabine (1) | 0.016, 0.0069 (AsPC-1, MiaPaCa-2) | Receptor tyrosine kinase Axl |
| GSK2256098 (45) | 25, 29 (L3.6P1, Panc-1) | Focal adhesion kinase |
| PF573228 (46) | NA a | |
| Binimetinib (MEK162) (47) | 0.092, 0.28 and 0.316 (MiaPaCa-2, AsPC-1, and CAPAN-2 | Mitogen-activated protein kinase kinase |
| Cobimetinib (48) | NA | |
| GSK2656157 (49) | NA a | Protein kinase R (PKR)-like endoplasmic reticulum kinase |
| 3-(2,5-dimethoxyphenyl)-N-((4-(5-(4-fluorophenyl)-2-(methylthio)-1H-imidazol-4-yl)pyridin-2-yl)carbamoyl)-propanamide (50) | EC50: 3.5, 1.5 (Colo357, Panc89) | Protein kinase CK1δ |
| SCH727965 (dinaciclib) (51) | GI50: 0.01, 0.02 (MiaPaCa-2,Pa20C) | Cyclin-dependent kinase (CDK; CDK1,2,5,9) |
| AZD6738 (52) | GR50: 0.9 μM, 1.57, 1.98, 3.2, 4.8, 9.8, 32.3 (SW1990, Capan-1, AsPC-1, HPAF-II, Capan-2, MiaPaCa-2, and Panc-1) | Ataxia telangiectasia and Rad3-related protein |
| L61H46 (53) | 0.86, 2.83 (BXPC-3, Panc-1) | Signal transducer and activator of transcription3 |
| PG-S3-001 (54) | ED50: 2.4 (Panc10.05) | |
| HJC0416 (55) | 0.04, 1.88 (AsPC-1, Panc-1) | |
| XZH-5 (56) | 24.7, 17.4 and 17.9 (Panc-1, HPAC, and SW1990) | |
| Methyl Nα-(((3,5-bis(trifluoromethyl)phenyl)-carbamoyl)isoleucyl)-Nτ-methyl-l-histidinate (57) | 10.1, 7.6, 8.3 (Panc-1, HPAC, and SW1990) | |
| Cryptotanshinone (58) | NA a | |
| JQ1 (59) | 0.037, 0.72 and 0.19 (AsPC-1, Panc-1, and CAPAN-1) | Bromodomain and extra terminal proteins: BRD2, BRD3 and BRD4 |
| I-BET 762 (60) | 0.231, 2.55 and 0.99 (AsPC-1, Panc-1, and CAPAN-1) | |
| ST-3595 (61) | NA a | Histone deacetylases |
| CG200745 (62) | 2.4, 10.7 and 7.4 (BxPC3, CFPAC1 and HPAC) | |
| MGCD0103 (63) | 3.9, 1.1, 0.6 and 1.8 (AsPC-1, BxPC-3, MiaPaca-2, and Panc-1) | |
| Belinostat (64) | EC50: 0.3, 0.7, 0.5, 1.1, 1.1 and 0.7 (AsPC1, BxPC3, Panc0327, Panc0403, and Panc1005, MiaPaCa-2) | |
| Panobinostat (65) | 0.284, 0.00046, 0.0077, 0.261, 0.013 (BxPC3, Panc0327, Panc0403, Panc1005, and MiaPaCa-2) | |
| UMI-77 (66) | 3.4, 4.4 and 5.5 (AsPC-1, BxPC-3, and Capan-2) | Bcl-2 family proteins |
| 4-((6-nitroquinolin-4-yl)amino)-N-(4-(pyridin-4-ylamino) phenyl benzamide (67) | 15.1 (BxPC-3) | |
| 2,3,4,6-tetrahydroxy-5H-benzo[7]annulen-5-one (68) | 17.6 (MiaPaCa-2) | |
| TW-37 (69) | NA a | |
| ABT737 (70) | NA a | |
| BMS-754807 (71) + gemcitabine (1) | 0.075, 0.070, 0.016, 0.016 (AsPC, Panc-1, MiaPaCa-2, and BxPC-3) | IGF-1R and insulin receptor (IR) family kinases |
| P1608K04 (72) | 8.5, 14, and 20 (Panc-1, MiaPaCa-2, and AsPC1) | Protein arginine methyltransferases |
| MI-319 (73) | NA a | Murine double minute 2 protein |
| NPC-26 (74) | NA a | Mitochondrion interfering |
| Spongiatriol (75) | 13, 8, 6 and 13 (AsPC-1, BxPC-3, MiaPaCa-2 and Panc-1) | Nuclear factor kappa B |
| SW IV-134 (76) | 7.4, 6.8, 6.3 and 7.8 (CFPAC-1, BxPC-3, AsPC-1, Panc-1 and MiaPaCa-2) | Sigma-2 receptor |
| BAY ACC002 (77) | NA a | Acetyl-CoA carboxylase 1 and 2; Hedgehog signalling pathway |
| ICG-001 (78) | 5.48, 14.07, 3.43 and 3.31 (AsPC-1, L3.6pl, Panc-1 and MiaPaCa-2) | CREB-binding protein |
| IPI-269609 (79) | NA a | Hedgehog signalling pathway |
| MRK-003 (80) | NA a | Gamma secretase |
| MDC-1016 (81) | NA a | RAS inhibitor |
| TIC10/ONC201 (82) | NA a | Tumour necrosis (TNF)-related apoptosis-inducing ligand |
aNo IC50 value was reported in the primary literature.