RRX-001 (RRX001) is a novel NO and hypoxia mediated anticancer agent with with epigenetic and immunologic activity; targets CD133 + /CD44 + cancer stem cells from colon cancer cell-lines, HT-29, Caco-2, and HCT116, and inhibits Wnt pathway signalling with downregulation of c-Myc; inhibits HCT 116 and decreases levels of the DNA methyltransferases DNMT1 and DNMT3a in a time and dose-dependent manner; RRX-001 (RRX001) is a chemosensitizer in multiple tumor types and disease states including malaria, hemorrhagic shock and sickle cell anemia.

Avitinib (AC-0010, AC0010) is an orally available, irreversible, and mutant-selective EGFR inhibitor with IC50 of 0.18 nM against EGFR L858R/T790M; displays 43-fold greater potency over wild-type EGFR (IC50=7.68 nM); selectively inhibits mutant EGFR phosphorylation (IC50 =7.3 nM and 2.8 nM) in NCI-H1975 and NIH/3T3_TC32T8 cells, 115- and 298-fold more sensitive than that of the inhibition of wild type EGFR in A431; overcomes T790M-induced resistance in animal models and lung cancer patients without hyperglycemia or other severe adverse effects.

CK-101 (RX-518) is a novel potent, mutant-selective, irreversible, orally available EGFR inhibitor, overcomes T790M-mediated resistance in NSCLC; specifically targets the mutant forms of EGFR, including T790M, while exhibiting minimal activity toward WT EGFR; selectively inhibits cell proliferation of cell lines expressing both the activating (HCC827, IC50 <15 nM) and resistance mutations (NCI-H1975, IC50 <5 nM); significantly inhibits tumor growth in EGFR-mutated NSCLC tumor xenograft models, with no activity in WT EGFR tumor xenograft model.

A potent, selective, orally active EGFR inhibitor with IC50 of 23 nM; inhibits EGF-stimulated proliferation of KB cells with IC50 of 80 nM; blocks the growth of GEO colon cancer, ZR-75-1 and MCF-10A Ha-ras breast cancer, and OVCAR-3 ovarian cancer cell lines with IC50 of 0.2-0.4 uM; significantly decreases EGFRvIII phosphotyrosine load, EGFRvIII-mediated proliferation and anchorage-independent growth; has been used to treat advanced (or recurrent) non-small cell lung cancer.

A potent, oral active, BBB-penetrating EGFR inhibitor (IC50=7.2 nM, L858R pEGFR); fully penetrate the blood-brain barrier (BBB), with equal free concentrations in the blood, cerebrospinal fluid, and brain tissue; causes tumor regression in subcutaneous xenograft, leptomeningeal metastasis (LM), and brain metastasis (BM) lung cancer models and prevents the development of BM in nude mice.

Avitinib maleate (AC-0010MA, AC0010 maleate) is an orally available, irreversible, and mutant-selective EGFR inhibitor with IC50 of 0.18 nM against EGFR L858R/T790M; displays 43-fold greater potency over wild-type EGFR (IC50=7.68 nM); selectively inhibits mutant EGFR phosphorylation (IC50 =7.3 nM and 2.8 nM) in NCI-H1975 and NIH/3T3_TC32T8 cells, 115- and 298-fold more sensitive than that of the inhibition of wild type EGFR in A431; overcomes T790M-induced resistance in animal models and lung cancer patients without hyperglycemia or other severe adverse effects.

EGF816 (Nazartinib) is a potent, irreversible, mutant-selective EGFR inhibitor with Ki and Kinact of 31 nM and 0.222 min-1, respectively; shows potent inhibition of pEGFR levels in H3255, HCC827, and H1975 with EC50 of 5, 1, and 3 nM, which harbor the L858R, Ex19del, and L858R/T790M mutations, respectively, inhibitscell proliferation with EC50 of 9, 11, and 25 nM, but not the WT EGFR-containing patient-derived cell lines; potently inhibits the most common EGFR mutations L858R, Ex19del, and T790M in vitro; causes tumor regressions in vivo in several patient-derived xenograft models, also demonstrates antitumor activity in exon 20 insertion mutant model.

Naquotinib (ASP-8273) is a potent, irreversible, mutant-selective inhibitor of EGFR (IC50=8-33 nM for (L858R, exon 19 deletion, L858R/T790M, and del19/T790M)); more potently than that of WT EGFR (IC50= 230 nM); shows activity in mutant EGFR cell line which is resistant to other EGFR TKIs including AZD9291 and CO-1686.

Naquotinib (ASP-8273) is a potent, irreversible, mutant-selective inhibitor of EGFR (IC50=8-33 nM for (L858R, exon 19 deletion, L858R/T790M, and del19/T790M)); more potently than that of WT EGFR (IC50= 230 nM); shows activity in mutant EGFR cell line which is resistant to other EGFR TKIs including AZD9291 and CO-1686.

A potent, selective, third-generation irreversible inhibitor of mutant EGFR with IC50s of 1/12/5 nM for L858R-T790M/L858R/L861Q respectively; weak activity against wt EGFR (IC50=184 nM); inhibits signaling pathways and cellular growth in both EGFRm(+) and EGFRm(+)/T790M(+) mutant cell lines in vitro; exhibits tumor regression in EGFR-mutant tumor xenograft and transgenic models; orally active.