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Cat. No.: HY-177138

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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.

CAS No.: 2099064-75-0
Formula: C₂₀H₂₀N₄O₄
Molecular Weight:380.40

Storage:

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

Data Sheet (270 KB)

Tubulin-IN-52 Chemical Structure

CAS No.: 2099064-75-0

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
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Biological Activity

Description

Cellular Effect

Cell Line	Type	Value	Description	References
A549	EC₅₀	1.4 μM Compound: 18	Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human A549 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 29288939]
A549/TR	EC₅₀	3.8 μM Compound: 18	Cytotoxicity against human A549/TR cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human A549/TR cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 29288939]
Calu-1	EC₅₀	1.6 μM Compound: 18	Cytotoxicity against human Calu1 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human Calu1 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 29288939]
NCI-H157	EC₅₀	2.4 μM Compound: 18	Cytotoxicity against human NCI-H157 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human NCI-H157 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 29288939]
PC-3	EC₅₀	1.6 μM Compound: 18	Cytotoxicity against human PC3 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human PC3 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 29288939]
SK-OV-3	EC₅₀	1 μM Compound: 18	Cytotoxicity against human SKOV3 cells assessed as reduction in cell viability after 72 hrs by MTT assay Cytotoxicity against human SKOV3 cells assessed as reduction in cell viability after 72 hrs by MTT assay	[PMID: 29288939]

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, below the T/C 0.45 threshold that defines active antitumor activity.
Showed no noticeable toxicity.

Chemical Information

CAS No. 2099064-75-0
Molecular Weight 380.40
Formula C₂₀H₂₀N₄O₄
SMILES

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

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (270 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

References

[1]. Cheong JE, et al. Synthesis and anticancer activity of novel water soluble benzimidazole carbamates. Eur J Med Chem. 2018 Jan 20;144:372-385. [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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100 mg

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