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Table 2 MCL-1 targeted anti-tumor drugs in the preclinical stage

From: Targeting MCL-1 in cancer: current status and perspectives

Compound   Efficacy towards malignant cells In vitro potency drug discovery method References
MIM1 MCL-1 dependent leukemia cells IC50: < 4.2 μM HTS (2013) [81]
UMI-59/77 BxPC-3 xenograft model Ki: 490 nM HTS (2014) [84]
Complex 39 NCI-H460 cell line and xenograft model IC50: 12–18 μM   [102]
Complex 14 NCI-H460 xenograft model Ki: 1.4 nM   [101]
Pyridoclax/Compound12 Ovarian cancer cell line (2014/2018) [77, 78]
ML311/EU-5346 Active MCL-1 cell line IC50: 0.31 μM HTS (2013) [82, 83]
A-1210477 MCL-1-dependent cell lines Ki: 4–5 nM HTS (2015) [62]
BIM SAHBA NA DLBCL cell lines EC50: 2–18 μM   [79]
MS1 PREIWMTQGLRRLGDEINAYYAR MCL-1 dependent cell lines Kd:1.9 ± 1.0 nM   [80]
VU661013 AML, MM, triple negative breast cancer cell lines Ki: 97 ± 30 pM Structure-based design (2018) [90, 124]
Wang.Compound12 NCI-H345 cell line IC50: 2.2 μM Fragment-based approach (2016) [107]
Compound8 A2780, MCF-7, SMMC-7721 and DLD1 cell lines IC50: 38–47 μM Virtual screening (2017) [108]
Compound24 Lymphoma cell lines Ki: 100 nM HTS and virtual screening (2020) [109]
Compound M08 Hematological and solid cancer cell lines Ki: 0.53 ± 0.07 μM Structure-based virtual screening (2020) [110]
Compound5 L-363, LP-1, NCI-H929 and MOLP-8 IC50: 3.4 nM   [92]
C3 HeLa, K562, NCI-H23 cell line IC50: 0.78 ± 0.12 μM (2019) [105]
dMCL1-2 MM cell line OPM2 Kd: 30 nM (2019) [104]
MI-223 H1299 cell Kd: 193 ± 4.3 nM Virtual screening (2018) [91]
APG-3526 NA MM cell line IC50: 7 nM (2020) [106]
  1. EC50 Half-maximal concentration of drug, IC50 Concentration inhibitory to 50% of cells, Ki Inhibition constant, Kd Dissociation constant