1. Cell Cycle/DNA Damage Cytoskeleton
  2. Microtubule/Tubulin
  3. D-64131

D-64131 is an orally active tubulin inhibitor, with an IC50 of 0.53 μM for tubulin polymerization. D-64131 has antimitotic activity. D-64131 can be used for cancer research.

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

D-64131 Chemical Structure

D-64131 Chemical Structure

CAS No. : 74588-78-6

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 44 In-stock
Solution
10 mM * 1 mL in DMSO USD 44 In-stock
Solid
5 mg USD 40 In-stock
10 mg USD 65 In-stock
25 mg USD 135 In-stock
50 mg USD 220 In-stock
100 mg USD 350 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE D-64131

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

D-64131 is an orally active tubulin inhibitor, with an IC50 of 0.53 μM for tubulin polymerization. D-64131 has antimitotic activity. D-64131 can be used for cancer research[1][2].

IC50 & Target

IC50: 0.53 μM (tubulin polymerization)[2]

Cellular Effect
Cell Line Type Value Description References
HeLa IC50
0.068 μM
Compound: 1
In vitro inhibitory activity against HeLa/KB cells using XTT proliferation assay.
In vitro inhibitory activity against HeLa/KB cells using XTT proliferation assay.
[PMID: 11741473]
SK-OV-3 IC50
0.68 μM
Compound: 1
In vitro inhibitory activity against SK-OV-3 cells using XTT proliferation assay.
In vitro inhibitory activity against SK-OV-3 cells using XTT proliferation assay.
[PMID: 11741473]
In Vitro

D-64131 is antimitotic by binding to β-tubulin, thereby destabilizing microtubules and arresting mitotic cells in the M-phase[1].
D-64131 inhibits the proliferation of tumor cells from 12 of 14 different organs and tissues with mean IC50s of 62 nM[1].
D-64131 is cytotoxic toward MDR/MRP tumor cell lines[1].
D-64131 suppresses U373 proliferation and cell cycle with IC50s of 74 nM and 62.7nM, respectively[2].

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

Cell Cycle Analysis[1]

Cell Line: HeLa/KB cervical carcinoma cells
Concentration: 1 nM-1 μM
Incubation Time: 48 hours
Result: Induced dose-dependently arrested in G2-M before induction of apoptotic cell death.
In Vivo

D-64131 (200-400 mg/kg; p.o.; daily; days 1-5, 8-9, and 15-18) significantly inhibits tumor growth in the human amelanoic melanoma MEXF 989 tumor xenograft mice model[1].
D-64131 has oral bioavailability and is well tolerated at efficacious doses[1].

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

Animal Model: Outbred nude mice (6-8 weeks), human amelanoic melanoma MEXF 989 tumor xenograft model[1]
Dosage: 200 mg/kg, 400 mg/kg
Administration: Oral administration, daily, on days 1-5, 8-9, and 15-18 after xenograft
Result: Resulted in significant tumor growth inhibition during treatment.
Molecular Weight

251.28

Formula

C16H13NO2

CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

O=C(C(N1)=CC2=C1C=CC(OC)=C2)C3=CC=CC=C3

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 2 years
-20°C 1 year
Solvent & Solubility
In Vitro: 

DMSO : ≥ 100 mg/mL (397.96 mM; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

*"≥" means soluble, but saturation unknown.

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 3.9796 mL 19.8981 mL 39.7962 mL
5 mM 0.7959 mL 3.9796 mL 7.9592 mL
View the 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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

  • Molarity Calculator

  • Dilution Calculator

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

Mass
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Concentration
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Volume
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Molecular Weight *

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start)

C1

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Volume (start)

V1

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Concentration (final)

C2

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Volume (final)

V2

In Vivo:

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.

  • Protocol 1

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

    Solubility: ≥ 2.5 mg/mL (9.95 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.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

Dosage

mg/kg

Animal weight
(per animal)

g

Dosing volume
(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
%
DMSO +
+
%
Tween-80 +
%
Saline
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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).
Calculation results:
Working solution concentration: mg/mL
Method for preparing stock solution: mg drug dissolved in μL  DMSO (Stock solution concentration: mg/mL).
The concentration of the stock solution you require exceeds the measured solubility. The following solution is for reference only. If necessary, please contact MedChemExpress (MCE).
Method for preparing in vivo working solution for animal experiments: Take μL DMSO stock solution, add μL . μL , mix evenly, next add μL Tween 80, mix evenly, then add μL Saline.
 If the continuous dosing period exceeds half a month, please choose this protocol carefully.
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
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, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 3.9796 mL 19.8981 mL 39.7962 mL 99.4906 mL
5 mM 0.7959 mL 3.9796 mL 7.9592 mL 19.8981 mL
10 mM 0.3980 mL 1.9898 mL 3.9796 mL 9.9491 mL
15 mM 0.2653 mL 1.3265 mL 2.6531 mL 6.6327 mL
20 mM 0.1990 mL 0.9949 mL 1.9898 mL 4.9745 mL
25 mM 0.1592 mL 0.7959 mL 1.5918 mL 3.9796 mL
30 mM 0.1327 mL 0.6633 mL 1.3265 mL 3.3164 mL
40 mM 0.0995 mL 0.4975 mL 0.9949 mL 2.4873 mL
50 mM 0.0796 mL 0.3980 mL 0.7959 mL 1.9898 mL
60 mM 0.0663 mL 0.3316 mL 0.6633 mL 1.6582 mL
80 mM 0.0497 mL 0.2487 mL 0.4975 mL 1.2436 mL
100 mM 0.0398 mL 0.1990 mL 0.3980 mL 0.9949 mL
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Help & FAQs
  • Do most proteins show cross-species activity?

    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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D-64131
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