2. Cell Cycle/DNA Damage Cytoskeleton Metabolic Enzyme/Protease
  3. Microtubule/Tubulin Prolyl Endopeptidase (PREP)
  4. 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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Tasidotin

Tasidotin Chemical Structure

CAS No. : 192658-64-3

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Tasidotin Related Antibodies

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Description

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].

In Vitro

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.

Tasidotin Related Antibodies

Cell Proliferation Assay[1]

Cell Line: Burkitt lymphoma CA46 suspension cells
Concentration: Multiple unspecified concentrations
Incubation Time: 48 h
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.

Cell Proliferation Assay[1]

Cell Line: MCF-7 human breast carcinoma monolayer cells
Concentration: Multiple unspecified concentrations
Incubation Time: 48 h
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.
Parmacokinetics
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
In Vivo

Tasidotin (0.75 mg/kg; i.v.; single dose; 30 minutes infusion) achieves high cerebrospinal fluid penetration in healthy adult male rhesus monkeys, with a mean CSF:plasma AUC0-t ratio of 1.1, and reaches concentrations associated with antiproliferative activity in the CSF for several hours post-administration[2].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Macaca mulatta (adult male, 11.4-15.9 kg)[2]
Dosage: 0.75 mg/kg
Administration: i.v.; single dose; 30 minutes infusion
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.
Molecular Weight

606.85

Formula

C32H58N6O5
CAS No.
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
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Tasidotin Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Tasidotin192658-64-3ILX651ILX 651ILX-651Microtubule/TubulinProlyl Endopeptidase (PREP)prolyl oligopeptidasePOPBurkitt lymphoma CA46 cellsmicrotubule assemblybovine tubulinnonhuman primatesMCF-7 human breast carcinoma cellsCCRF-CEM human leukemia cellsMDA-MB-435 human breast carcinoma cellsHS 578-T human breast carcinoma cellsFlavobacterium meningosepticumInhibitorinhibitorinhibit

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