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Cevipabulin (TTI-237) is a novel, potent, oral, microtubule-active antitumor small molecule, inhibits the binding of [3H] vinblastine to tubulin, with an IC50 of 18-40 nM for cytotoxicity in human tumor cell line. Cevipabulin (TTI-237) inhibited the binding of [(3)H]vinblastine to tubulin, but it caused a marked increase in turbidity development that more closely resembled the effect observed with docetaxel than that observed with vincristine. Cevipabulin (TTI-237) was active in vivo in several nude mouse xenograft models of human cancer, including LoVo human colon carcinoma and U87-MG human glioblastoma, when dosed i.v. or p.o.
| Molecular Weight | 464.82 |
| Formula | C18H18ClF5N6O |
| CAS Number | 849550-05-6 |
| Solubility (25°C) | DMSO 15 mg/mL |
| Storage |
Powder -20°C 3 years ; 4°C 2 years In solvent -80°C 6 months ; -20°C 1 month |
| Related Microtubule Products |
|---|
| ABT-751
ABT-751 is an orally bioavailable tubulin inhibitor with IC50 of about 1.5 and 3.4 µM in neuroblastoma and non-neuroblastoma cell lines, respectively. |
| Vincristine sulfate
Vincristine, formally known as leurocristine, is a mitotic inhibitor used in cancer chemotherapy. |
| Docetaxel
Docetaxel (Taxotere), a semi-synthetic analog of paclitaxel (Taxol), is a promoter of microtubule polymerization leading to cell cycle arrest at G2/M, apoptosis and cytotoxicity. |
| Paclitaxel
Paclitaxel is a diterpenoid derived from the bark of the plant Picea abies, and is also a microtubule polymer stabilizer, which promotes polymerization of microtubule proteins to inhibit depolymerization, maintains the stability of microtubule proteins, and inhibits cellular mitosis, and acts on human endothelial cells with an IC50 of 0.1 pM. |
| Fosbretabulin disodium
Fosbretabulin disodium (Combretastatin A-4 phosphate) is a microtubule-targeting agent that binds β-tubulin with Kd of 0.4 μM. |
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