192658-64-3
Chemical Structure
Tasidotin
Synonym(s): ILX651 free base
- CAS No.: 192658-64-3
- Formula:C32H58N6O5
- Molecular Weight:606.85
IUPAC Name: (S)-N-(tert-butyl)-1-(N-dimethyl-L-valyl-L-valyl-N-methyl-L-valyl-L-prolyl)pyrrolidine-2-carboxamide
InChIKey: QMCOCIWNMHBIIA-LROMGURASA-N
SMILES: C([C@@H](N(C([C@@H](NC([C@H](C(C)C)N(C)C)=O)[C@@H](C)C)=O)C)C(C)C)(=O)N1[C@H](C(=O)N2[C@H](C(NC(C)(C)C)=O)CCC2)CCC1
Biological Activity: Tasidotin (ILX651 free base) is a tubulin inhibitor and competitive Prolyl Endopeptidase (PREP) inhibitor, with an IC50 of 10 μM against bovine tubulin. Tasidotin exhibits high cerebrospinal fluid penetration in non-human primates. Tasidotin antagonizes microtubule assembly and induces an extended assembly lag phase, thereby inhibiting mitosis and cell proliferation, and exerts cytotoxic and oncolytic effects on cancer cells. Tasidotin is metabolized into polypeptides and proline inside cells, and its in vivo metabolism is mediated by prolyl endopeptidase. Tasidotin can be applied in research related to Burkitt's lymphoma, breast cancer, leukemia, melanoma, central nervous system malignancies and various solid tumors[1][2][3].
| Cat. No. | Product Name | Purity | Description | Pricing | |||||||||||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
|
|
Tasidotin | Tasidotin (ILX651 free base) is a tubulin inhibitor and competitive Prolyl Endopeptidase (PREP) inhibitor, with an IC50 of 10 μM against bovine tubulin. Tasidotin exhibits high cerebrospinal fluid penetration in non-human primates. Tasidotin antagonizes microtubule assembly and induces an extended assembly lag phase, thereby inhibiting mitosis and cell proliferation, and exerts cytotoxic and oncolytic effects on cancer cells. Tasidotin is metabolized into polypeptides and proline inside cells, and its in vivo metabolism is mediated by prolyl endopeptidase. Tasidotin can be applied in research related to Burkitt's lymphoma, breast cancer, leukemia, melanoma, central nervous system malignancies and various solid tumors. | |||||||||||||||||||||
|
loading...
/
|
|||||||||||||||||||||||
- [1]. Bai R, et al. Intracellular activation and deactivation of tasidotin, an analog of dolastatin 15: correlation with cytotoxicity. Mol Pharmacol. 2009;75(1):218-226. [Content Brief]
- [2]. Kilburn LB, et al. Plasma and cerebrospinal fluid pharmacokinetics of tasidotin (ILX-651) and its metabolites in non-human primates. Cancer Chemother Pharmacol. 2009;64(2):335-340. [Content Brief]
- [3]. Deutch C E, et al. Conversion of the anti-tumor agent tasidotin (ILX651) to its active metabolite by prolyl oligopeptidase[J]. Enzyme and microbial technology, 2010, 46(3-4): 246-251.
Keywords
