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Cat. No.: HY-149856

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Tubulin inhibitor 33

Tubulin inhibitor 33, a tubulin polymerization inhibitor, inhibits tubulin polymerization in a dose-dependent manner with an IC₅₀ of 9.05 μM. Tubulin inhibitor 33 has antitumor effects and induces cell apoptosis that can be used for antitumor research.

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

CAS No.: 2944462-67-1
Formula: C₂₄H₂₂N₄O₃
Molecular Weight:414.46

Storage:

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

Data Sheet (277 KB)

Tubulin inhibitor 33 Chemical Structure

CAS No.: 2944462-67-1

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Use of MCE Products

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target

IC50: 9.05 μM (tubulin)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A2780/Taxol	IC₅₀	5.1 nM Compound: 3a	Antiproliferative activity against paclitaxel resistant human A2780/Taxol cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay Antiproliferative activity against paclitaxel resistant human A2780/Taxol cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay	[PMID: 37145846]
A2780S	IC₅₀	1.6 nM Compound: 3a	Antiproliferative activity against parental human A2780S cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay Antiproliferative activity against parental human A2780S cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay	[PMID: 37145846]
B16-F10	IC₅₀	0.002 μM Compound: 3a	Antiproliferative activity against mouse B16-F10 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay Antiproliferative activity against mouse B16-F10 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay	[PMID: 37145846]
HeLa	IC₅₀	0.009 μM Compound: 3a	Antiproliferative activity against human HeLa cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay Antiproliferative activity against human HeLa cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay	[PMID: 37145846]
HepG2	IC₅₀	0.001 μM Compound: 3a	Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay Antiproliferative activity against human HepG2 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay	[PMID: 37145846]
HUVEC	IC₅₀	62.1 nM Compound: 3a	Cytotoxicity against HUVEC cells assessed as inhibition of cell proliferation incubated for 24 hrs by MTT assay Cytotoxicity against HUVEC cells assessed as inhibition of cell proliferation incubated for 24 hrs by MTT assay	[PMID: 37145846]
MCF7	IC₅₀	0.006 μM Compound: 3a	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell proliferation incubated for 48 hrs by MTT assay	[PMID: 37145846]

In Vitro

Tubulin inhibitor 33 (Compound 3a) (0-5 nM; 24-48 hours) inhibits the proliferation, antimigratory and colony formation and induces G2/M arrest and apoptosis in HepG-2 cells^[1].
Tubulin inhibitor 33 (0-5 nM; 12 hours) effectively inhibits tubulin polymerization in HepG-2 cells and disrupts microtubule dynamics
^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

MCF-7, HeLa, B16-F10, HepG-2 cells
Concentration:

0-5 nM
Incubation Time:

24-48 hours
Result:

Exhibited the antiproliferative activity against the growth of cancer cells with an average IC₅₀ value of 4.5 nM.
Suppressed the formation of HepG-2 colonies in a dose-dependent manner, with the colony-forming ability of HepG-2 cells being significantly suppressed.
Exhibited the antimigratory effects against HepG-2 cells.
Induced G2/M arrest and apoptosis in HepG-2 cells.

Immunofluorescence^[1]

Cell Line:

HepG-2 cells
Concentration:

0-5 nM
Incubation Time:

12 hours
Result:

Effectively inhibited tubulin polymerization in vitro and disrupted microtubule dynamics.

In Vivo

Tubulin inhibitor 33 (Compound 3a) (5 mg/kg; i.p. everyday for 14 days) significantly inhibits melanoma tumor growth with tumor growth inhibition (TGI) of 62.96%^[1].

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

Animal Model:

B16-F10 melanoma model in C57 mice^[1]
Dosage:

5 mg/kg
Administration:

Intraperitoneal injection (i.p.)
Result:

Significantly inhibited melanoma tumor growth with a TGI of 62.96%.

Chemical Information

CAS No. 2944462-67-1
Molecular Weight 414.46
Formula C₂₄H₂₂N₄O₃
SMILES

COC1=C(OC)C(OC)=CC(C2=NC=CC3=C2N=C(C4=CC=CC5=C4C=CN5C)N3)=C1
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 (277 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]. Ren Y, et.al. X-ray Crystal Structure-Guided Discovery of Novel Indole Analogues as Colchicine-Binding Site Tubulin Inhibitors with Immune-Potentiating and Antitumor Effects against Melanoma. J Med Chem. 2023 May 25;66(10):6697-6714. [Content Brief]

Calculators

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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.

Bioz

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100 mg

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