Art. -Nr.: HY-179372

Tubulin polymerization-IN-84

Kundenbewertung

Based on 1 Customer Validation

Tubulin polymerization-IN-84 inhibits tubulin polymerization by targeting the colchicine-binding pocket, with anIC₅₀ = 10.9 μM. Tubulin polymerization-IN-84 shows antiproliferative activity against Jurkat, B16-F10, HCT116, and MDA-MB-231 cells (IC₅₀ = 60 nM, 380 nM, 138 nM, and 1.054 μM). Tubulin polymerization-IN-84 induces G2/M-phase arrest and apoptosis in B16-F10 cells. Tubulin polymerization-IN-84 suppresses tumor growth in a B16-F10 melanoma model and potentiates anti-tumor immunity in combination with a PD-L1 mAb for the research of T-cell acute lymphoblastic leukemia, melanoma, colon cancer, and breast cancer.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Reinheit: 99.59%
CAS. Nr.: 2982893-14-9
Formel: C₂₃H₂₂N₂O₃
Molecular Weight:374.43

Speicherung:

-20°C, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Tubulin polymerization-IN-84 Chemical Structure

CAS. Nr.: 2982893-14-9

Größe

Preis

Verfügbarkeit

Menge

Amount: USD 0.00

* Bitte wählen Sie Menge, bevor Sie Artikel hinzufügen.

Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

Cellular Effect

Cell Line	Type	Value	Description	References
CHP-134	GI₅₀	0.152 μM Compound: 4a	Growth inhibition of MYCN-amplified human CHP-134 cells assessed as reduction in cell viability measured after 3 days by Celltiter-glo assay Growth inhibition of MYCN-amplified human CHP-134 cells assessed as reduction in cell viability measured after 3 days by Celltiter-glo assay	[PMID: 37736192]

In Vitro

Tubulin polymerization-IN-84 (compound 5b) (48 h) inhibits proliferation of Jurkat, B16-F10, HCT116, and MDA-MB-231 cells (IC₅₀ = 60 nM, 380 nM, 138 nM, and 1.054 μM)^[1].
Tubulin polymerization-IN-84 (0.1-5 μM; 24 h) dose-dependently suppresses wound closure/migration and colony formation of B16-F10 cells^[1].
Tubulin polymerization-IN-84 (0.5-5 μM; 48 h) induces both G2/M-phase arrest and apoptosis in B16-F10 cells (G2/M: 9.75% in control vs 81.1% at 5 μM)^[1].
Tubulin polymerization-IN-84 directly binds to β-tubulin (KD = 31.84 μM)^[1].
Tubulin polymerization-IN-84 (0.1-5 μM) competes with EBI for binding to the colchicine-binding site of β-tubulin in B16-F10 cells in a concentration-dependent manner^[1].
Tubulin polymerization-IN-84 (0.5-5 μM; 12 h) induces disassembly of cytoplasmic microtubule networks in B16-F10 cells^[1].
Tubulin polymerization-IN-84 (0.5-5 μM; 6 h) dose-dependently disrupts HUVEC capillary-like network formation on Matrigel and reduces junctions/nodes^[1].

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

Cell Migration Assay ^[1]

Cell Line:

B16-F10
Concentration:

0.1 μM; 0.5 μM; 1 μM; 5 μM
Incubation Time:

24 h
Result:

Dose-dependently suppressed wound closure and decreased migration rate versus control.

Cell Proliferation Assay^[1]

Cell Line:

B16-F10
Concentration:

0.5 μM; 1 μM; 5 μM
Incubation Time:

24 h
Result:

Dose-dependently suppressed colony formation and reduced colony numbers versus control.

Cell Cycle Analysis^[1]

Cell Line:

B16-F10
Concentration:

0.5 μM; 1 μM; 5 μM
Incubation Time:

48 h
Result:

Increased the proportion of cells arrested at G2/M phase in a dose-dependent manner (9.75% in control vs 81.1% at 5 μM).

Apoptosis Analysis^[1]

Cell Line:

B16-F10
Concentration:

0.1 μM; 0.5 μM; 1 μM; 5 μM
Incubation Time:

48 h
Result:

Increased total apoptotic cells in a dose-dependent manner (14.79% in control vs 21.22%/23.65%/35.66% at 0.5/1/5 μM).

Western Blot Analysis^[1]

Cell Line:

B16-F10
Concentration:

0.1 μM; 0.5 μM; 1 μM; 5 μM
Incubation Time:

After treatment
Result:

Competitively inhibited EBI-induced β-tubulin adduct formation in a concentration-dependent manner, indicating binding to the colchicine-binding site of β-tubulin.

Immunofluorescence^[1]

Cell Line:

B16-F10
Concentration:

0.5 μM; 1 μM; 5 μM
Incubation Time:

12 h
Result:

Induced disassembly of cytoplasmic microtubule networks compared with control.

In Vivo

Tubulin polymerization-IN-84 (compound 5b) (10 mg/kg; i.p.; QD; 14 days) inhibits tumor growth in C57BL/6 mice bearing established B16-F10 melanoma tumors (TGI = 27.5%), and shows enhanced efficacy in combination with a PD-L1 mAb (10 + 10 mg/kg; TGI = 36.2%) without significant body-weight loss^[1].

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

Animal Model:

C57BL/6 mice bearing established B16-F10 melanoma tumors^[1]
Dosage:

10 + 10 mg/kg (5b + PD-L1 mAb)
Administration:

Intraperitoneal injection (i.p.); once daily (QD); for 14 days
Result:

Inhibited tumor growth as monotherapy (TGI = 27.5%) and showed higher tumor growth inhibition in combination with PD-L1 mAb (TGI = 36.2%), without significant body-weight loss.
Increased the proportion of activated CD3+CD8+ cytotoxic T cells in tumors (48.9% in combination group vs 31.8% in control).
Reduced Ki-67 expression and increased γ-H2AX signals in tumor tissues.
Showed no apparent histopathological abnormalities in major organs and no significant changes in serum biochemistry markers versus control.

Chemical Information

CAS. Nr. 2982893-14-9
Appearance Solid
Molecular Weight 374.43
Formel C₂₃H₂₂N₂O₃
Color White to off-white
SMILES

COC1=CC(C2=CC=CN3C=C(N=C23)C4=CC=C(C=C4)C)=CC(OC)=C1OC
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

-20°C, stored under nitrogen

* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (267.07 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

2.6707 mL

13.3536 mL

26.7073 mL

5 mM

0.5341 mL

2.6707 mL

5.3415 mL

10 mM

0.2671 mL

1.3354 mL

2.6707 mL

Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.

Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline

Solubility: ≥ 2.5 mg/mL (6.68 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.

Protocol 2

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (6.68 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
Saline +

The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).

Working solution concentration: 0.22 mg/mL

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 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)

Verweise

[1]. Cheng B, et al. Novel imidazo[1,2-a]pyridine-based tubulin polymerization inhibitors: Structure-activity relationships and anti-tumor immune potentiation. Eur J Med Chem. 2026;302(Pt 2):118356. doi:10.1016/j.ejmech.2025.118356 [Content Brief]

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.

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg
DMSO	1 mM	2.6707 mL	13.3536 mL	26.7073 mL	66.7682 mL
	5 mM	0.5341 mL	2.6707 mL	5.3415 mL	13.3536 mL
	10 mM	0.2671 mL	1.3354 mL	2.6707 mL	6.6768 mL
	15 mM	0.1780 mL	0.8902 mL	1.7805 mL	4.4512 mL
	20 mM	0.1335 mL	0.6677 mL	1.3354 mL	3.3384 mL
	25 mM	0.1068 mL	0.5341 mL	1.0683 mL	2.6707 mL
	30 mM	0.0890 mL	0.4451 mL	0.8902 mL	2.2256 mL
	40 mM	0.0668 mL	0.3338 mL	0.6677 mL	1.6692 mL
	50 mM	0.0534 mL	0.2671 mL	0.5341 mL	1.3354 mL
	60 mM	0.0445 mL	0.2226 mL	0.4451 mL	1.1128 mL
	80 mM	0.0334 mL	0.1669 mL	0.3338 mL	0.8346 mL
	100 mM	0.0267 mL	0.1335 mL	0.2671 mL	0.6677 mL

Keywords

Tubulin polymerization-IN-84

100 mg Angebot einholen

Subscribe to the

MedChemExpress

Newsletter

Produktname:
Art. -Nr.:
Menge:
MCE Japan Authorized Agent:

Produktname:
CAS. Nr.:
Species:
Reinheit:
Menge:

Tubulin polymerization-IN-84

Bioactive Compound Library Max

Bioactive Compound Library

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Cytoskeleton Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Protein-protein Interaction Inhibitor Library

Cell Death Library

Anti-Hematopathy Compound Library

MCE Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

High-Efficiency Gene Editing Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Tubulin polymerization-IN-84

Bioactive Compound Library Max

Bioactive Compound Library

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Cytoskeleton Compound Library

Anti-Breast Cancer Compound Library

Anti-Lung Cancer Compound Library

Anti-Blood Cancer Compound Library

Anti-Colorectal Cancer Compound Library

Protein-protein Interaction Inhibitor Library

Cell Death Library

Anti-Hematopathy Compound Library

MCE Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

High-Efficiency Gene Editing Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Tubulin polymerization-IN-84 Related Classifications

HY-179372 Related Classifications