BMS-599626 (AC480) is a selective and efficacious inhibitor of HER1 and HER2 with IC50 of 20 nM and 30 nM, respectively.

NVP-BGT226 is a novel dual PI3K/mTOR inhibitor with IC50 of 1 nM.

Cediranib (AZD2171) is a highly potent VEGFR2 inhibitor with IC50 of 0.5 nM, also inhibits Flt1/4 with IC50 of 5 nM/≤3 nM.

NVP-AEW541 is a potent inhibitor of IGF-1R with IC50 of 86 nM.

BMS-911543 is a potent and selective inhibitor of JAK2 with IC50 of 1.1 nM, approximately 350-, 75- and 65-fold selective to JAK1, JAK3 and TYK2, respectively.

Methazolastone (Temozolomide, Temodar, Temodal) is a DNA damage inducer.

Bleomycin sulfate (Blenoxane) is a glycopeptide antibiotic and an anticancer agent for squamous cell carcinomas (SCC) with IC50 of 4 nM in UT-SCC-19A cells.

Vismodegib (formerly GDC-0449) is a hedgehog antagonist, is also an orally bioavailable small molecule with potential antineoplastic activity.

AZD1480 is a novel ATP-competitive JAK2 inhibitor with IC50 of 0.26 nM, selectivity against JAK3 and Tyk2, and to a smaller extent against JAK1. Phase 1/2.

RAF265 (CHIR-265) is a highly selective B-Raf and VEGFR2 inhibitor with IC50 of 3-60 nM and EC50 of 30 nM, including B-Raf, C-Raf and mutant B-Raf.

MLN2238 inhibits the chymotrypsin-like proteolytic (β5) site of the 20S proteasome with IC50 and Ki of 3.4 nM and 0.93 nM, respectively, also inhibits the caspase-like (β1) and trypsin-like (β2) proteolytic sites, with IC50 of 31 and 3500 nM.

Crenolanib (CP-868596) is a potent and selective inhibitor of PDGFRα/β with Kd of 2.1 nM/3.2 nM, also potently inhibits FLT3, sensitive to D842V mutation not V561D mutation, >100-fold more selective for PDGFR than c-Kit, VEGFR-2, TIE-2, FGFR-2, EGFR, erbB

Fosbretabulin disodium(CA 4DP; CA 4P) is a microtubule destabilizing drug, a type of vascular-targeting agent, a drug designed to damage the vasculature (blood vessels) of cancer tumors causing central necrosis.

Entinostat (MS-275) strongly inhibits HDAC1 and HDAC3 with IC50 of 0.51 μM and 1.7 μM, compared with HDACs 4, 6, 8, and 10. Phase 1/2.

AMG-208 is a potent small molecular c-Met inhibitor with an IC50 of 9.3 nM.

Daunorubicin HCl inhibits both DNA and RNA synthesis and inhibits DNA synthesis with Ki of 0.02 μM.

PF-04217903 is a selective ATP-competitive c-Met inhibitor with IC50 of 4.8 nM, susceptible to oncogenic mutations (no activity to Y1230C mutant).

Dinaciclib (SCH727965) is a novel and potent CDK inhibitor for CDK2, CDK5, CDK1 and CDK9 with IC50 of 1 nM, 1 nM, 3 nM and 4 nM, respectively.

JNJ-38877605 is an ATP-competitive inhibitor of c-Met with IC50 of 4 nM, 600-fold selective for c-Met than 200 other tyrosine and serine-threonine kinases.

LGK-974 is a potent and specific PORCN inhibitor, and inhibits Wnt signaling with IC50 of 0.4 nM.

LY2940680 binds to the Smoothened (Smo) receptor and potently inhibits Hedgehog (Hh) signaling.

SGX-523 is a selective Met inhibitor with IC50 of 4 nM, no activity to BRAFV599E, c-Raf, Abl and p38α.