1. Cell Cycle/DNA Damage Cytoskeleton Apoptosis
  2. Microtubule/Tubulin Apoptosis
  3. Indibulin

Indibulin  (Synonyms: ZIO 301; D 24851)

Cat. No.: HY-13649 Purity: 99.89%
SDS COA Handling Instructions

Indibulin (ZIO 301), an orally applicable inhibitor of tubulin assembly, shows potent anticancer activity with a minimal neurotoxicity. Indibulin reduces inter-kinetochoric tension, produces aberrant spindles, activates mitotic checkpoint proteins Mad2 and BubR1, and induces mitotic arrest and apoptosis.

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

Indibulin Chemical Structure

Indibulin Chemical Structure

CAS No. : 204205-90-3

Size Price Stock Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
USD 77 In-stock
Solution
10 mM * 1 mL in DMSO USD 77 In-stock
Solid
5 mg USD 70 In-stock
10 mg USD 112 In-stock
25 mg USD 235 In-stock
50 mg USD 380 In-stock
100 mg USD 610 In-stock
200 mg   Get quote  
500 mg   Get quote  

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This product is a controlled substance and not for sale in your territory.

Customer Review

Based on 1 publication(s) in Google Scholar

Top Publications Citing Use of Products

1 Publications Citing Use of MCE Indibulin

  • Biological Activity

  • Purity & Documentation

  • References

  • Customer Review

Description

Indibulin (ZIO 301), an orally applicable inhibitor of tubulin assembly, shows potent anticancer activity with a minimal neurotoxicity. Indibulin reduces inter-kinetochoric tension, produces aberrant spindles, activates mitotic checkpoint proteins Mad2 and BubR1, and induces mitotic arrest and apoptosis[1].

IC50 & Target

Tubulin[1]

Cellular Effect
Cell Line Type Value Description References
A2780 EC50
19 nM
Compound: Indibulin
Antiproliferative activity against human A2780 cells incubated for 72 hrs by ATPlite reagent based assay
Antiproliferative activity against human A2780 cells incubated for 72 hrs by ATPlite reagent based assay
[PMID: 31047749]
A2780 EC50
20 nM
Compound: Indibulin
Antiproliferative activity against D4-9-31 resistance human A2780 cells incubated for 72 hrs by ATPlite reagent based assay
Antiproliferative activity against D4-9-31 resistance human A2780 cells incubated for 72 hrs by ATPlite reagent based assay
[PMID: 31047749]
A549 IC50
2.1 μM
Compound: Indibulin
Growth inhibition of human A549 cells after 48 hrs by MTT assay
Growth inhibition of human A549 cells after 48 hrs by MTT assay
[PMID: 28131777]
DU-145 IC50
0.18 μM
Compound: Indibulin
Growth inhibition of human DU145 cells after 48 hrs by MTT assay
Growth inhibition of human DU145 cells after 48 hrs by MTT assay
[PMID: 28131777]
HCT-15 IC50
0.56 μM
Compound: Indibulin
Growth inhibition of human HCT15 cells after 48 hrs by MTT assay
Growth inhibition of human HCT15 cells after 48 hrs by MTT assay
[PMID: 28131777]
KB IC50
44 nM
Compound: D-24851
Cytotoxicity against human KB/HeLa cells after 48 hrs by XTT assay
Cytotoxicity against human KB/HeLa cells after 48 hrs by XTT assay
[PMID: 19682911]
L1210 IC50
44 nM
Compound: D-24851
Cytotoxicity against mouse L1210 cells after 48 hrs by XTT assay
Cytotoxicity against mouse L1210 cells after 48 hrs by XTT assay
[PMID: 19682911]
MCF7 IC50
1.1 μM
Compound: Indibulin
Cytotoxicity against human MCF7 cells assessed as reduction in cell survival after 48 hrs by MTT assay
Cytotoxicity against human MCF7 cells assessed as reduction in cell survival after 48 hrs by MTT assay
[PMID: 28494255]
MDA-MB-231 IC50
0.074 μM
Compound: Indibulin
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell survival after 48 hrs by MTT assay
Cytotoxicity against human MDA-MB-231 cells assessed as reduction in cell survival after 48 hrs by MTT assay
[PMID: 28494255]
PC-3 IC50
0.4 μM
Compound: Indibulin
Growth inhibition of human PC3 cells after 48 hrs by MTT assay
Growth inhibition of human PC3 cells after 48 hrs by MTT assay
[PMID: 28131777]
SK-BR-3 IC50
0.033 μM
Compound: Indibulin
Growth inhibition of human SKBR3 cells after 48 hrs by MTT assay
Growth inhibition of human SKBR3 cells after 48 hrs by MTT assay
[PMID: 22850214]
SK-OV-3 IC50
77 nM
Compound: D-24851
Cytotoxicity against human SKOV3 cells after 48 hrs by XTT assay
Cytotoxicity against human SKOV3 cells after 48 hrs by XTT assay
[PMID: 19682911]
In Vitro

Indibulin (300-2100 nM; 48?hours) inhibits the proliferation of MCF-7 cells with an IC50 of 150?nM[1].
Indibulin (300, 600 nM; 48?hours) blockes the cells in the G2/M phase indicating that indibulin blockes the progression of the cell cycle at mitosis[1].
Indibulin (150-600 nM; 24?hours) induces apoptosis in MCF-7 cells[1].
Indibulin (150-600 nM; 48?hours) with 300 and 600?nM generates cleaved fragments of PARP protein the treatment of MCF-7 cells[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 cells
Concentration: 300, 600, 900, 1200, 1500, 1800, 2100 nM
Incubation Time: 48 hours
Result: Inhibited the proliferation of MCF-7 cells with an IC50 of 150 nM.

Cell Cycle Analysis[1]

Cell Line: MCF-7 cells
Concentration: 300, 600 nM
Incubation Time: 48 hours
Result: Blocked the cells in the G2/M phase of the cell cycle.

Apoptosis Analysis[1]

Cell Line: MCF-7 cells
Concentration: 150, 300 and 600 nM
Incubation Time: 24 hours
Result: Induced apoptosis in MCF-7 cells.

Western Blot Analysis[1]

Cell Line: MCF-7 cells
Concentration: 150, 300 and 600 nM
Incubation Time: 48 hours
Result: Generated cleaved fragments of PARP protein in 300 and 600 nM.
Clinical Trial
Molecular Weight

389.83

Formula

C22H16ClN3O2

CAS No.
Appearance

Solid

Color

Off-white to yellow

SMILES

O=C(NC1=CC=NC=C1)C(C2=CN(CC3=CC=C(Cl)C=C3)C4=C2C=CC=C4)=O

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 : 50 mg/mL (128.26 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.5652 mL 12.8261 mL 25.6522 mL
5 mM 0.5130 mL 2.5652 mL 5.1304 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

×
Volume (start)

V1

=
Concentration (final)

C2

×
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    90% (20% SBE-β-CD in Saline)

    Solubility: 2.08 mg/mL (5.34 mM); Suspended solution; Need ultrasonic

    This protocol yields a suspended solution of 2.08 mg/mL. Suspended solution can be used for oral and intraperitoneal injection.

    Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

    Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
  • Protocol 2

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

    Solubility: ≥ 2.08 mg/mL (5.34 mM); Clear solution

    This protocol yields a clear solution of ≥ 2.08 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 (20.8 mg/mL) to 900 μL Corn oil, and mix evenly.

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

Purity: 99.89%

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 2.5652 mL 12.8261 mL 25.6522 mL 64.1305 mL
5 mM 0.5130 mL 2.5652 mL 5.1304 mL 12.8261 mL
10 mM 0.2565 mL 1.2826 mL 2.5652 mL 6.4131 mL
15 mM 0.1710 mL 0.8551 mL 1.7101 mL 4.2754 mL
20 mM 0.1283 mL 0.6413 mL 1.2826 mL 3.2065 mL
25 mM 0.1026 mL 0.5130 mL 1.0261 mL 2.5652 mL
30 mM 0.0855 mL 0.4275 mL 0.8551 mL 2.1377 mL
40 mM 0.0641 mL 0.3207 mL 0.6413 mL 1.6033 mL
50 mM 0.0513 mL 0.2565 mL 0.5130 mL 1.2826 mL
60 mM 0.0428 mL 0.2138 mL 0.4275 mL 1.0688 mL
80 mM 0.0321 mL 0.1603 mL 0.3207 mL 0.8016 mL
100 mM 0.0257 mL 0.1283 mL 0.2565 mL 0.6413 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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Indibulin
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