PP121 is a multitargeted dual receptor tyrosine kinases inhibitor. PP121 blocks the proliferation of tumor cells by direct inhibition of oncogenic tyrosine kinases and phosphatidylinositol-3-OH kinases. PP-121 is a multi-targeted inhibitor of PDGFR, Hck, mTOR, VEGFR2, Src and Abl with IC50 of 2 nM, 8 nM, 10 nM, 12 nM, 14 nM and 18 nM, also inhibits DNA-PK with IC50 of 60 nM. PP121 blocks the proliferation of tumor cells by direct inhibition of oncogenic tyrosine kinases and phosphatidylinositol-3-OH kinases.

KRN633 is a selective inhibitor of Vascular endothelial growth factor receptors VEGFR-1, -2, and -3. KRN633 also blocked the activation of mitogen-activated protein kinases by VEGF, along with human umbilical vein endothelial cell proliferation and tube formation. KRN633 inhibited tumor growth in several in vivo tumor xenograft models with diverse tissue origins, including lung, colon, and prostate, in athymic mice and rats. Kirin Brewery developed angiogenesis inhibitor KRN 633 as a treatment for solid tumours. It is in phase I clinical trials.

AZD2932 is an oral inhibitor of VEGFR-2 and PDGFR tyrosine kinases, which was developed by AstraZeneca as a potential anti-cancer medicine. The drug was tested in vivo in preclinical model of mice bearing C6 rat glial tumors and AZD2932 demonstrated good potency: growth of Calu-6 tumor was inhibited by 81% and 72% at 50 and 12.5 mg/kg b.i.d. and LoVo tumors by 67% at 50 mg/kg b.i.d.

Pristimerin, the methyl ester of celasterol, is a triterpenoid quinone methide isolated from Pristimerae indica. Pristimerin shows anticancer activity in vitro towards myeloma, prostate, breast, ovarian cancer cell lines and inhibits xenografted plasmacytoma tumors in mice. In a rat model of adjuvant arthritis, pristimerin effectively inhibited both arthritic inflammation and cartilage and bone damage in the joints. Pristimerin acts by inhibiting NF-kB signaling pathway and the 26S proteasome.

Gamabufotalin belongs to bufadienolides was first isolated from B. formosus Boulenger and described by Kotake in 1928. Gamabufotalin is a component of traditional Chinese medicinal preparations containing ChanSu, also known as toad venom, a dried product of the skin and parotid venom glands from the Asiatic toad (Bufo gargarizans). Gamabufotalin inhibits sodium/potassium-transporting ATPase activity and exhibited positive inotropic action in the papillary muscle preparations. Gamabufotalin demonstrates significant anti-tumor activity in vitro on cancer cells and in vivo on mouse tumor xenografts. Gamabufotalin, a major derivative of bufadienolide, inhibits VEGF-induced angiogenesis.

ACTB-1003 is an oral kinase inhibitor targeting cancer mutations (FGFR inhibition), angiogenesis (inhibition of VEGFR2 and Tie-2) and induces apoptosis (targeting RSK and p70S6K, downstream of PI3 kinase). The multi-activity of ACTB- 1003 translates to in vivo efficacy with dose-dependent tumor growth inhibition in a variety of histological cancers including lung, breast and colorectal. Eddingpharm acquired worldwide rights to small molecule drug assets including ACTB1003 from ACT Biotech. Eddingpharm plans a phase I trial for Cancer in USA.

Corosolic acid is a pentacyclic triterpene acid isolated from Lagerstroemia speciosa. It inhibits STAT3 and VEGFR2 signaling and has cytotoxic effect on a number of tumor cell lines. Corosolic acid has demonstrated anti-diabetic effect in vivo, probably due to facilitation of GLUT4 translocation or AMPK activation.

N-Desethyl Sunitinib is a major and pharmacologically active metabolite of sunitinib, which is potent, ATP-competitive VEGFR, PDGFRβ, and KIT inhibitor.