84697-22-3
Chemical Structure
Tubulozole
Synonym(s): R 46846
- CAS No.: 84697-22-3
- Formula:C23H23Cl2N3O4S
- Molecular Weight:508.42
IUPAC Name: ethyl (4-((((2R,4R)-2-((1H-imidazol-1-yl)methyl)-2-(2,4-dichlorophenyl)-1,3-dioxolan-4-yl)methyl)thio)phenyl)carbamate
InChIKey: OGPIBXIQNMQSPY-JPYJTQIMSA-N
SMILES: O=C(NC1=CC=C(C=C1)SC[C@@H]2O[C@@](C3=CC=C(C=C3Cl)Cl)(OC2)CN4C=CN=C4)OCC
Biological Activity: 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[1][2][3][4].
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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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References
- [1]. Chou YH, et al. Tubulozole-induced G2/M cell cycle arrest in human colon cancer cells through formation of microtubule polymerization mediated by ERK1/2 and Chk1 kinase activation. Food and chemical toxicology : an international journal published for the British Industrial Biological Research Association. 2007 Aug;45(8):1356-67.
- [2]. Stitt A W, et al. Spermatogenesis in Fasciola hepatica: an ultrastructural comparison of the effects of the anthelmintic, thiabendazole (“Fasinex”) and the microtubule inhibitor, tubulozole[J]. Invertebrate Reproduction & Development, 1992, 22(1-3): 139-150.
- [3]. Distelmans W, et al. Interaction between the microtubule inhibitor tubulozole and gamma-irradiation in murine tumors in vivo. International journal of radiation oncology, biology, physics. 1989 Jan;16(1):177-82.
- [4]. Distelmans W, et al. Influence of the synthetic microtubule inhibitor erbulozole (P.I.N.N.) (R 55 104), a new tubulozole congener, and gamma irradiation on murine tumors in vivo. European journal of cancer & clinical oncology. 1989 Oct;25(10):1499-504. [Content Brief]
