Ansamitocin p-3 (Maytansinol isobutyrate, NSC292222) (C007B-020703)

InformationAnsamitocin p-3 (Maytansinol isobutyrate, NSC292222, Antibiotic C 15003P3) is a potent inhibitor of tubulin polymerization with IC50 of 3.4 μM.In vitroAnsamitocin p-3 at 5 μM completely inhibits the polymerization of tubulin isolated from bovine brains, but in contrast to VCR, Ansamitocin p-3 at a high concentration of 80 μM does not leads to the aggregation of tubulin. Ansamitocin p-3 at 16 μM also potently depolymerizes the polymerized tubulin (IC50 = 3.8 μM). The addition of Ansamitocin p-3 to culture cells blocks the morphological alteration of AC cells from fibroepithelioid to a glial cell type caused by the exposure to a certain concentration of dibutyryl cyclic adenosine 3/':5/'-monophosphate. In addition, Ansamitocin p-3 treatment at 16 nM causes the well-defined network of cytoplasmic microtubules of A31 cells rapidly dispersed. Short-term Ansamitocin p-3 treatment also inhibits the synthesis of DNA in A31 cells or KB cells. These results confirm that Ansamitocin p-3 acts by interfering with the microtubule assembly system, thus resulting in an inhibition of mitotic spindle fiber formation and, ultimately, cytokilling. Ansamitocin p-3 displays potent cytotoxicity against A-549, HT-29, and MCF-7 cells in a dose-dependent manner with ED50 of 4 ×10-7, 4 × 10-7, and 2 × 10-6 μg/mL, respectively. Ansamitocin p-3 also exhibits cytotoxicity against HCT-116 cells with a much low EC50 of 0.081 nM. Ansamitocin p-3 enhances the effect of radiation both in Drosophila cells and human cancer cells in a p53 dependent manner.In vivoAnsamitocin p-3 treatment (>1 μg) significantly suppresses the growth of leukemia SN36, and induces an increased arrest in metaphase of P388 leukemia cells. Ansamitocin p-3 treatment at 25 μg/kg/day significantly prolongs the survival time of mice bearing i.p. B16 melanoma by 130%. Ansamitocin p-3 treatment also significantly prolongs the survival time of mice bearing Ehrlich ascites carcinoma, Sarcoma 180, and P815 mastocytoma, while slightly prolongs the survival time of mice bearing ascites MOPC-104E myeloma,leukemia L1210, and leukemia C1498.Cell Research(from reference)Cell lines：A31 and KB Concentrations：Dissolved in DMSO, final concentrations ~10 μM Incubation Time：~24 hours. Specification: 0.98 Molecular Formula: C32H43ClN2O9 Molecular Weight: 635.14 PubChem CID: 5282049 Isomeric SMILES: C[C@@H]1[C@@H]2C[C@]([C@@H](/C=C/C=C(/CC3=CC(=C(C(=C3)OC)Cl)N(C(=O)C[C@@H]([C@]4([C@H]1O4)C)OC(=O)C(C)C)C)/C)OC)(NC(=O)O2)O Related Documents: https://ald-pub-files.oss-cn-shanghai.aliyuncs.com/aladdinsci/pdp/sds/1/A412781-SCI_f5e827b226648d8823c505b8249b9503.pdf