Tubulin polymerization-IN-84
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.
For research use only. We do not sell to patients.
- Purity: 99.59%
- CAS No.: 2982893-14-9
- Formula: C23H22N2O3
- Molecular Weight:374.43
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Storage:
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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Solvent & Solubility
- Purity & Documentation
- References
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Help & FAQs
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Bioactive Compound Library Max
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Biological Activity
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CHP-134 | GI50 |
0.152 μM
Compound: 4a
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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
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[PMID: 37736192] |
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.
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Cell Line:B16-F10
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Concentration:0.1 μM; 0.5 μM; 1 μM; 5 μM
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Incubation Time:24 h
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Result:Dose-dependently suppressed wound closure and decreased migration rate versus control.
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Cell Line:B16-F10
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Concentration:0.5 μM; 1 μM; 5 μM
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Incubation Time:24 h
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Result:Dose-dependently suppressed colony formation and reduced colony numbers versus control.
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Cell Line:B16-F10
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Concentration:0.5 μM; 1 μM; 5 μM
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Incubation Time:48 h
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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).
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Cell Line:B16-F10
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Concentration:0.1 μM; 0.5 μM; 1 μM; 5 μM
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Incubation Time:48 h
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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).
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Cell Line:B16-F10
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Concentration:0.1 μM; 0.5 μM; 1 μM; 5 μM
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Incubation Time:After treatment
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Result:Competitively inhibited EBI-induced β-tubulin adduct formation in a concentration-dependent manner, indicating binding to the colchicine-binding site of β-tubulin.
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Cell Line:B16-F10
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Concentration:0.5 μM; 1 μM; 5 μM
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Incubation Time:12 h
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Result:Induced disassembly of cytoplasmic microtubule networks compared with control.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 mice bearing established B16-F10 melanoma tumors[1]
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Dosage:10 + 10 mg/kg (5b + PD-L1 mAb)
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Administration:Intraperitoneal injection (i.p.); once daily (QD); for 14 days
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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
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CAS No. 2982893-14-9
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Appearance Solid
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Molecular Weight 374.43
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Formula C23H22N2O3
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Color White to off-white
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SMILES
COC1=CC(C2=CC=CN3C=C(N=C23)C4=CC=C(C=C4)C)=CC(OC)=C1OC
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
-20°C, stored under nitrogen
* In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
Solvent & Solubility
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)
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.
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.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- 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.
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.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%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
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (stored under nitrogen)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Purity & Documentation
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Data Sheet (282 KB)
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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)
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Handling Instructions (2659 KB)
References
Complete Stock Solution Preparation Table
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.
| 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 |
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