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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 192658-64-3
- 分子式: C32H58N6O5
- 分子量:606.85
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保管条件:
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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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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.
化学情報
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CAS 番号 192658-64-3
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分子量 606.85
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分子式 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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別名
ILX651 free base
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)
Tasidotin 関連分類
HY-106021 関連分類
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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