Description
TSU-68 (SU6668, Orantinib) can potently inhibit FGFR1, PDGFRbeta, and Flk-1/KDR with Ki of 8 nM, 1200 nM and 2100 nM.
Storage
2 years at -20 centigrade
Targets
FGFR1, PDGFRbeta, Flk-1
Molecular Formula
C18H18N2O3
Chemical Name
(Z)-3-(2,4-dimethyl-5-((2-oxoindolin-3-ylidene)methyl)-1H-pyrrol-3-yl)propanoic acid
Solubility
DSMO 62 mg/mL Water
In vitro
TSU-68 (SU6668, Orantinib) can potently inhibit FGFR1, PDGFRbeta, and Flk-1/KDR with Ki of 8 nM, 1200 nM and 2100 nM. TSU-68 in combination with docetaxel showed a promising antitumor response with manageable toxicity in patients with anthracycline-resistant metastatic breast cancer.
In vivo
(1) In mouse model of ovarian cancer The oral administration of SU6668 inhibited angiogenesis and peritoneal dissemination and prolonged survival in mice with peritoneally disseminated ovarian cancer. These effects were observed with both the VEGF- and PDGF-hypersecretory cell lines.
(2) Human colon cancer xenograft TSU-68 significantly inhibited tumor growth and liver metastasis formation of human colon cancer xenografts.
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