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)