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Cat. No.: HY-119169A

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Tubulozole hydrochloride

Name: Tubulozole hydrochloride
Brand: MedChemExpress
SKU: HY-119169A
Availability: PreOrder

(Synonyms: R 46846 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.

For research use only. We do not sell to patients.

CAS No.: 83086-73-1
Formula: C₂₃H₂₄Cl₃N₃O₄S
Molecular Weight:544.88

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

Tubulozole hydrochloride Chemical Structure

CAS No.: 83086-73-1

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
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Biological Activity

Description

IC₅₀ & Target

^[1]

Chk1

ERK1

ERK2

All Checkpoint Kinase (Chk) Isoforms :

All ERK Isoforms :

In Vitro

Tubulozole (10 μM; 6 h) hydrochloride 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) hydrochloride 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) hydrochloride drives the translocation of phosphorylated Cdc25C (Ser-216) from the nucleus to the cytoplasm in colon adenocarcinoma COLO 205 cells^[1].
Tubulozole hydrochloride 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.

Western Blot Analysis^[1]

Cell Line:

Human colon adenocarcinoma COLO 205 cells
Concentration:

10 μM
Incubation Time:

3 h, 6 h
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

Tubulozole (160 mg/kg; oral gavage; single dose) hydrochloride administered 6 hours prior to 10 Gy gamma irradiation at its documented optimal pretreatment schedule produces MO₄ fibrosarcoma tumor regression in male CDF₁ mice equivalent to that of 80 mg/kg Erbulozole (HY-105273) given 2 hours before radiation^[4].

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

Animal Model:

CDF₁ (DBA/2× C3H) hybrid mice (male, 18-22 g body weight)^[4]
Dosage:

160 mg/kg
Administration:

oral gavage; single dose
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

CAS No. 83086-73-1
Molecular Weight 544.88
Formula C₂₃H₂₄Cl₃N₃O₄S
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
Synonyms

R 46846 hydrochloride
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

Handling Instructions (2659 KB)

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]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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Tubulozole hydrochloride

All Checkpoint Kinase (Chk) Isoforms

All ERK Isoforms