Tubulozole
Tubulozole (R 46846) is an orally active inhibitor of tubulin polymerization with an ID50 of 0.34 μM. Tubulozole induces activation of the Chk1 kinase and phosphorylation of ERK1/2, which is required for microtubule formation. Tubulozole arrests Mitosis at the metaphase stage. Tubulozole causes cells to accumulate in the radiosensitive mitotic phase of the cell cycle. Tubulozole exerts anticancer activity against colon cancer. Tubulozole produces a radiosensitizing effect in mouse tumor models and enhances the tumor growth delay effect when combined with γ-ray irradiation. Tubulozole is used in studies related to colon cancer, fascioliasis, MO4 fibrosarcoma, and Lewis lung carcinoma.
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- CAS No.: 84697-22-3
- Formula: C23H23Cl2N3O4S
- Molecular Weight:508.42
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
Description
IC50 & Target
[1]|
Chk1 |
ERK1 |
ERK2 |
In Vitro
Tubulozole (10 μM; 6 h) selectively induces robust Chk1 kinase activation in colon adenocarcinoma COLO 205 cells, while producing minimal Chk1 activation in normal human colon epithelial CRL cells[1].
Tubulozole (10 μM; 3-6 h) induces rapid, early phosphorylation of Chk1 (Ser-345) and Bad (Ser-155) in colon adenocarcinoma COLO 205 cells, followed by enhanced 14-3-3β binding to both phosphorylated Cdc25C and phosphorylated Bad[1].
Tubulozole (10 μM) drives the translocation of phosphorylated Cdc25C (Ser-216) from the nucleus to the cytoplasm in colon adenocarcinoma COLO 205 cells[1].
Tubulozole inhibits purified tubulin polymerization in vitro with an ID50 of 0.34 μM[4].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Human colon adenocarcinoma COLO 205 cells
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Concentration:10 μM
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Incubation Time:3 h, 6 h
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Result:Induces phosphorylation of Chk1 at Ser-345 as early as 3 h post-exposure, with no change in total Chk1 protein expression.
Induces phosphorylation of Bad at Ser-155 as early as 3 h post-exposure.
Significantly increases the binding of phosphorylated Cdc25C (Ser-216) and phosphorylated Bad (Ser-155) to 14-3-3β protein at 6 h of treatment.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:CDF1 (DBA/2× C3H) hybrid mice (male, 18-22 g body weight)[4]
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Dosage:160 mg/kg
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Administration:oral gavage; single dose
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Result:Produce initial subcutaneous MO4 fibrosarcoma tumor regression equivalent to the initial tumor regression achieved with 80 mg/kg erbulozole administered at its optimal 2-hour pretreatment interval before 10 Gy gamma irradiation.
Confirm the 6-hour pretreatment window as the established optimal time point for Tubulozole (hydrochloride) to exert maximum tumor radiation enhancement effects in this model, a time interval that is non-optimal for erbulozole which shows negative excess growth delay at 4 and 6 hour pretreatment intervals.
Chemical Information
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CAS No. 84697-22-3
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Molecular Weight 508.42
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Formula C23H23Cl2N3O4S
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SMILES
O=C(NC1=CC=C(C=C1)SC[C@@H]2O[C@@](C3=CC=C(C=C3Cl)Cl)(OC2)CN4C=CN=C4)OCC
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Synonyms
R 46846
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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
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Tubulozole Related Classifications
HY-119169 Related Classifications
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Keywords
- Tubulozole
- 84697-22-3
- R 46846
- R46846
- R-46846
- Microtubule/Tubulin
- Checkpoint Kinase (Chk)
- ERK
- Mitosis
- colon cancer cells
- Lewis lung carcinoma
- ERK1/2 phosphorylation
- tubulin polymerization inhibitor
- COLO 205 cells
- Fasciola hepatica
- colon cancer
- CRL cells
- Chk1 kinase activation
- microtubule formation
- Inhibitor
- inhibitor
- inhibit