AEE788 is a potent inhibitor of EGFR and HER2/ErbB2 with IC50 of 2 nM and 6 nM, less potent to VEGFR2/KDR, c-Abl, c-Src, and Flt-1, does not inhibit Ins-R, IGF-1R, PKCα and CDK1. Phase 1/2.

An orally available thioxanthone-based DNA intercalator and inhibitor of the DNA repair enzyme apurinic-apyrimidinic endonuclease 1 (APE1) potential antineoplastic activity, also inhibits autophagy.

CBL0137 is a metabolically stable curaxin that activates p53 with an EC50 value of 0.37 µM and inhibits NF-κB with an EC50 of 0.47 µM.

CYC065 is an orally bioavailable inhibitor of cyclin dependent kinases 2, 5 and 9 (CDK2/5/9) with potential antineoplastic and chemoprotective activities.

GDC-0084 （RG7666）, is a phosphatidylinositol 3-kinase (PI3K) inhibitor with potential antineoplastic activity.

IDH305 is an inhibitor of the citric acid cycle enzyme isocitrate dehydrogenase [NADP] cytoplasmic (isocitrate dehydrogenase 1; IDH1) with mutations at residue R132 (IDH1(R132)), with potential antineoplastic activity.

INK 128 is a potent and selective mTOR inhibitor with IC50 of 1 nM; >200-fold less potent to class I PI3K isoforms.

LB-100 is a small-molecular protein phosphatase 2A(PP2A)inhibitor with IC50 of 0.85 μM and 3.87 μM in BxPc-3 and Panc-1 cells.

MK-4101 is a potent SMO Inhibitor of the Hedgehog Pathway, highly active against Medulloblastoma and Basal Cell Carcinoma.

PD0325901 (PD325901) is selective and non ATP-competitive MEK inhibitor with IC50 of 0.33 nM.

Perifosine (KRX-0401) is a novel Akt inhibitor with IC50 of 4.7 μM.

PF-06840003 is an orally available hydroxyamidine and inhibitor of indoleamine 2,3-dioxygenase 1 (IDO1),with potential immunomodulating and antineoplastic activities.

PI3K-IN-2 is a PI3K inhibitor, inhibits pPKB and pS6 with "++++/+++(+)" in A2058 melanoma cell.

S49076 is a novel kinase inhibitor of MET, AXL, and FGFR with strong preclinical activity alone and in association with bevacizumab.

S49076 is a novel, potent inhibitor of MET, AXL/MER, and FGFR1/2/3 with IC50 values below 20 nM.

Tandutinib (MLN518, CT53518) is a potent FLT3 antagonist with IC50 of 0.22 μM, also inhibits PDGFR and c-Kit, 15 to 20-fold higher potency for FLT3 versus CSF-1R and >100-fold selectivity for the same target versus FGFR, EGFR and KDR. Phase 2.

TIC10 isomer(ONC201 isomer) is an isomer of TIC10; TIC10 is a potent, orally active, and stable small molecule that transcriptionally induces TRAIL in a p53-independent manner and crosses the blood-brain barrier.