83086-73-1
Chemical Structure
Tubulozole hydrochloride
Synonym(s): R 46846 hydrochloride
- CAS No.: 83086-73-1
- Formula:C23H24Cl3N3O4S
- Molecular Weight:544.88
InChIKey: HZQPPNNARUQMJA-IMIWJGOWSA-N
SMILES: CCOC(NC(C=C1)=CC=C1SC[C@@H](CO2)O[C@]2(C3=C(C=C(C=C3)Cl)Cl)CN4C=CN=C4)=O.Cl
Biological Activity: Tubulozole hydrochloride (R 46846 hydrochloride) is an orally active inhibitor of tubulin polymerization with an ID50 of 0.34 μM. Tubulozole hydrochloride induces activation of the Chk1 kinase and phosphorylation of ERK1/2, which is required for microtubule formation. Tubulozole hydrochloride arrests Mitosis at the metaphase stage. Tubulozole hydrochloride causes cells to accumulate in the radiosensitive mitotic phase of the cell cycle. Tubulozole hydrochloride exerts anticancer activity against colon cancer. Tubulozole hydrochloride produces a radiosensitizing effect in mouse tumor models and enhances the tumor growth delay effect when combined with γ-ray irradiation. Tubulozole hydrochloride is used in studies related to colon cancer, fascioliasis, MO4 fibrosarcoma, and Lewis lung carcinoma[1][2][3][4].
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Tubulozole hydrochloride | Tubulozole hydrochloride (R 46846 hydrochloride) is an orally active inhibitor of tubulin polymerization with an ID50 of 0.34 μM. Tubulozole hydrochloride induces activation of the Chk1 kinase and phosphorylation of ERK1/2, which is required for microtubule formation. Tubulozole hydrochloride arrests Mitosis at the metaphase stage. Tubulozole hydrochloride causes cells to accumulate in the radiosensitive mitotic phase of the cell cycle. Tubulozole hydrochloride exerts anticancer activity against colon cancer. Tubulozole hydrochloride produces a radiosensitizing effect in mouse tumor models and enhances the tumor growth delay effect when combined with γ-ray irradiation. Tubulozole hydrochloride 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]
