Tasidotin hydrochloride
Tasidotin hydrochloride is a peptide analog of the antimitotic depsipeptide dolastatin 15, as an inhibitor of microtubule assembly and microtubule dynamics.
For research use only. We do not sell to patients.
- CAS No.: 623174-20-9
- Formula: C32H59ClN6O5
- Molecular Weight:643.30
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
IC50 & Target
Microtubule[1]
In Vitro
Compared with other breast carcinoma lines, relatively low amounts of Tasidotin enters NCI/ADR-RES cells, consistent with Tasidotin's also being a P-glycoprotein substrate. Of the remaining lines, the greatest difference in sensitivity to Tasidotin is between the more sensitive MDA-MB-435 line and the less sensitive HS 578-T line. The IC50 values in the two lines are 4 and 200 nM, respectively[1]. The IC50 in Ewing's sarcoma, rhabdomyosarcoma, osteosarcoma, and synovial sarcoma lines ranges from 2 to 320 nM. In the SK-ES1 and RH30 cell lines, Tasidotin induces a G2-M arrest that persists for 48 h after Tasidotin is washed from the cells. In vitro, more than half the cells are in the early or late phase of apoptosis 48 h after treatment with Tasidotin. Following treatment for 24 h with 160 nM Tasidotin, the RH30 line and SK-ES1 line each shows an accumulation of cells in the G2-M phase. At hour 24, nearly all the RH30 cells are in the G2-M phase[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 623174-20-9
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Molecular Weight 643.30
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Formula C32H59ClN6O5
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SMILES
[H]Cl.O=C(N1CCC[C@H]1C(NC(C)(C)C)=O)[C@H]2N(C([C@H](C(C)C)N(C([C@H](C(C)C)NC([C@H](C(C)C)N(C)C)=O)=O)C)=O)CCC2
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Synonyms
ILX651
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
[1]. Bai R, et al. Intracellular activation and deactivation of Tasidotin, an analog of dolastatin 15: correlation with cytotoxicity. Mol Pharmacol. 2009 Jan;75(1):218-26. [Content Brief]
[2]. Garg V, et al. Preclinical analysis of Tasidotin HCl in Ewing's sarcoma, rhabdomyosarcoma, synovial sarcoma, and osteosarcoma. Clin Cancer Res. 2007 Sep 15;13(18 Pt 1):5446-54. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)