1. Cell Cycle/DNA Damage Cytoskeleton
  2. Microtubule/Tubulin
  3. Tubulin-IN-52

Tubulin-IN-52 is a tubulin inhibitor. Tubulin-IN-52 demonstrates significant cytotoxicity toward a variety of cancer cell types including prostate, lung, and ovarian cancers with strong activity toward highly aggressive cancer lines (IC50 = 0.9-3.8 mM). Tubulin-IN-52 significantly inhibits the growth of established tumors without noticeable toxicity. Tubulin-IN-52 can be used for the study of cancer.

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

Tubulin-IN-52 Chemical Structure

Tubulin-IN-52 Chemical Structure

CAS No. : 2099064-75-0

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Description

Tubulin-IN-52 is a tubulin inhibitor. Tubulin-IN-52 demonstrates significant cytotoxicity toward a variety of cancer cell types including prostate, lung, and ovarian cancers with strong activity toward highly aggressive cancer lines (IC50 = 0.9-3.8 mM). Tubulin-IN-52 significantly inhibits the growth of established tumors without noticeable toxicity. Tubulin-IN-52 can be used for the study of cancer[1].

In Vitro

Tubulin-IN-52 (Compound 18) (1-10 μM, 72 h) induces significant cytotoxicity in the cell line A549, and the prostate cancer cell lines PC3 and PC3MLN4[1].
Tubulin-IN-52 (0.0032-50 μM) shows highly cytotoxic in cancer cells with EC50s of 2.4 μM (H157), 1.6 μM (Calu1), 1.4 μM (A549), 1.6 μM (PC3), 0.9 μM (PC3MLN4) and 1.0 μM (SKOV3)[1].
Tubulin-IN-52 (1 μM, 24 h) induces G2M cell cycle arrest in PC3MLN4 cells[1].
Tubulin-IN-52 (1 μM, 48 h) disrupts microtubule dynamics in PC3MLN4 cells[1].

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

Cell Viability Assay[1]

Cell Line: PC3MLN4, PC3 and A549 cells
Concentration: 1, 10 μM
Incubation Time: 72 h
Result: Induced significant cytotoxicity at 1 and 10 μM.

Cell Cycle Analysis[1]

Cell Line: PC3MLN4 cells
Concentration: 1 μM
Incubation Time: 24 h
Result: Induced G2M cell cycle arrest in PC3MLN4 cells.

Western Blot Analysis[1]

Cell Line: PC3MLN4, PC3 and A549 cells
Concentration: 1 μM
Incubation Time: 48 h
Result: Increased the level of cyclin B1.
In Vivo

Tubulin-IN-52 (Compound 18) (30 mg/kg, i.p., 3 times a week, two weeks ) shows significant inhibition of tumor growth in the PC3MLN4 xenograft mouse model[1].

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

Animal Model: PC3MLN4 cells (106)-derived subcutaneous xenograft athymic male mice (eight weeks)[1]
Dosage: 30 mg/kg
Administration: i.p. 3 times a week for two weeks
Result: Showed tumor volume (day 15) of 43.2 mm3 while that of the control group (C) is 118.8 mm3.
Showed treatment-to-control (T/C) ratio at the last time point of 0.36 (t-test p value ¼ .0481), below the T/C 0.45 threshold that defines active antitumor activity.
Showed no noticeable toxicity.
Molecular Weight

380.40

Formula

C20H20N4O4

CAS No.
SMILES

O=C(NC1=NC2=C(N1)C=C(C(C3=CC=C(N(C4COC4)C)C=C3)=O)C=C2)OC

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Room temperature in continental US; may vary elsewhere.

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

Purity & Documentation
References
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    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.

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Product Name:
Tubulin-IN-52
Cat. No.:
HY-177138
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