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.
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- CAS No.: 192658-64-3
- 화학식: C32H58N6O5
- 분자량:606.85
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보관:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
Tasidotin inhibits the growth of Burkitt's lymphoma CA46 cells, with an IC50 of 100 nM[1].
Tasidotin inhibits the growth of MCF-7 human breast cancer cells with an IC50 of 150 nM[1].
Tasidotin (2-300 nM; 70 nM) potently inhibits the proliferation of various tumor cell lines in vitro, with IC50 values ranging from 2 to 300 nM; at a concentration of approximately 70 nM, it suppresses mitosis and cell proliferation by affecting microtubule dynamics[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Burkitt lymphoma CA46 suspension cells
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Concentration:Multiple unspecified concentrations
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Incubation Time:48 h
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Result:Inhibited the growth of CA46 cells with an IC50 of 100 nM.
Was substantially less cytotoxic than dolastatin 15 and dolastatin 10, but more cytotoxic than its metabolite P5.
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Cell Line:MCF-7 human breast carcinoma monolayer cells
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Concentration:Multiple unspecified concentrations
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Incubation Time:48 h
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Result:Inhibited the growth of MCF-7 cells with an IC50 of 150 nM.
Was substantially less cytotoxic than dolastatin 15, cemadotin, and dolastatin 10, but more cytotoxic than its metabolite P5.
| Species | Dose | Route | AUC0-∞ (Plasma) | T1/2 (Plasma) | CLplasma |
|---|---|---|---|---|---|
| Rhesus monkey[2] | 0.75 mg/kg | i.v. | 30 μM·min | 27 min | 44 mL/min/kg |
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Macaca mulatta (adult male, 11.4-15.9 kg)[2]
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Dosage:0.75 mg/kg
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Administration:i.v.; single dose; 30 minutes infusion
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Result:Achieved a mean CSF:plasma AUC ratio of 1.1.
Had a mean plasma AUC of 30 μM min, mean plasma half-life of 27 min, and mean plasma clearance of 44 mL/min/kg.
Had a mean CSF AUC of 28 μM min, with a mean CSF half-life of 96 min.
Reached peak CSF concentrations ranging from 53 to 272 nM, exceeding 70 nM for 2.5-3.5 hours in three of four animals.
Was well tolerated with no significant clinical or laboratory toxicity.
Chemical Information
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CAS No. 192658-64-3
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분자량 606.85
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화학식 C32H58N6O5
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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
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Synonyms
ILX651 free base
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
[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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Tasidotin Related Classifications
HY-106021 Related Classifications
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- Tasidotin
- 192658-64-3
- ILX651
- ILX 651
- ILX-651
- Microtubule/Tubulin
- Prolyl Endopeptidase (PREP)
- Burkitt lymphoma CA46 cells
- microtubule assembly
- prolyl oligopeptidase
- bovine tubulin
- nonhuman primates
- MCF-7 human breast carcinoma cells
- CCRF-CEM human leukemia cells
- MDA-MB-435 human breast carcinoma cells
- HS 578-T human breast carcinoma cells
- Flavobacterium meningosepticum
- Inhibitor
- inhibitor
- inhibit