Cat. No.: HY-13649

Indibulin

(Synonyms: ZIO 301; D 24851)

1 Cited Publications

Customer Review

Based on 1 publication(s) in Google Scholar

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.

Purity: 99.89%
CAS No.: 204205-90-3
Formula: C₂₂H₁₆ClN₃O₂
Molecular Weight:389.83

Storage:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year

Indibulin Chemical Structure

CAS No.: 204205-90-3

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

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

Biological Activity
- Description
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- Clinical Trial
Chemical Information
Publications (1)
Solvent & Solubility
- In Vitro
- In Vivo
Purity & Documentation
References
Help & FAQs
Bioz

Biological Activity

Description

IC₅₀ & Target

BUBR1

All Checkpoint Kinase (Chk) Isoforms :

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]
A549	IC₅₀	0.398 μM Compound: D-24851	Cytotoxicity against human A549 cells assessed as cell growth inhibition Cytotoxicity against human A549 cells assessed as cell growth inhibition	[PMID: 33132173]
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]
DU-145	IC₅₀	0.05 μM Compound: D-24851	Cytotoxicity against human DU-145 cells assessed as cell growth inhibition Cytotoxicity against human DU-145 cells assessed as cell growth inhibition	[PMID: 33132173]
HCT-116	IC₅₀	0.05 μM Compound: D-24851	Cytotoxicity against human HCT-116 cells assessed as cell growth inhibition Cytotoxicity against human HCT-116 cells assessed as cell growth inhibition	[PMID: 33132173]
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]
HeLa	IC₅₀	0.115 μM Compound: 1; D-24851	Antiproliferative activity against human HeLa cells assessed as reduction in cell viability Antiproliferative activity against human HeLa cells assessed as reduction in cell viability	[PMID: 31753698]
HepG2	IC₅₀	>10000 nM Compound: D-24851	In vitro anticancer activity against human hepatocellular HepG2 cells In vitro anticancer activity against human hepatocellular HepG2 cells	[PMID: 12699388]
HT-29	IC₅₀	72 nM Compound: D-24851	Antiproliferative activity against human HT-29 cells Antiproliferative activity against human HT-29 cells	[PMID: 19743863]
HT-29	IC₅₀	72 nM Compound: fig 2 cmpd 2	Cytotoxicity against multidrug resistance human HT-29 cells assessed as cell growth inhibition Cytotoxicity against multidrug resistance human HT-29 cells assessed as cell growth inhibition	[PMID: 36970141]
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	5416 nM Compound: D-24851	In vitro anticancer activity against human breast MCF-7/ADR subline (adriamycin-resistant) In vitro anticancer activity against human breast MCF-7/ADR subline (adriamycin-resistant)	[PMID: 12699388]
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]
MCF7S	IC₅₀	1134 nM Compound: D-24851	In vitro anticancer activity against human breast MCF-7 cells In vitro anticancer activity against human breast MCF-7 cells	[PMID: 12699388]
MDA-MB-231	IC₅₀	74 nM Compound: D-24851	Antiproliferative activity against human MDA-MB-231 cells Antiproliferative activity against human MDA-MB-231 cells	[PMID: 19743863]
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]
MES-SA/Dx5	IC₅₀	3018 nM Compound: D-24851	In vitro anticancer activity against human uterus MES-SA/DX5 subline (doxorubicin-resistant) In vitro anticancer activity against human uterus MES-SA/DX5 subline (doxorubicin-resistant)	[PMID: 12699388]
MES-SA/Dx5	IC₅₀	7371 nM Compound: D-24851	In vitro anticancer activity against human uterus MES-SA cells In vitro anticancer activity against human uterus MES-SA cells	[PMID: 12699388]
NUGC-3	IC₅₀	524 nM Compound: D-24851	In vitro anticancer activity against human gastric NUGC3 cells In vitro anticancer activity against human gastric NUGC3 cells	[PMID: 12699388]
P388	IC₅₀	77 nM Compound: D-24851	In vitro anticancer activity against murine leukemic P388 cells In vitro anticancer activity against murine leukemic P388 cells	[PMID: 12699388]
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]
PC-3	IC₅₀	0.04 μM Compound: D-24851	Cytotoxicity against human PC-3 cells assessed as cell growth inhibition Cytotoxicity against human PC-3 cells assessed as cell growth inhibition	[PMID: 33132173]
PC-3	IC₅₀	64 nM Compound: fig 2 cmpd 2	Cytotoxicity against multidrug resistance human PC-3 cells assessed as cell growth inhibition Cytotoxicity against multidrug resistance human PC-3 cells assessed as cell growth inhibition	[PMID: 36970141]
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]
SK-OV-3	IC₅₀	0.2 μM Compound: D-24851	Cytotoxicity against human SK-OV-3 cells assessed as cell growth inhibition Cytotoxicity against human SK-OV-3 cells assessed as cell growth inhibition	[PMID: 33132173]
SK-OV-3	IC₅₀	36 nM Compound: fig 2 cmpd 2	Cytotoxicity against multidrug resistance human SK-OV-3 cells assessed as cell growth inhibition Cytotoxicity against multidrug resistance human SK-OV-3 cells assessed as cell growth inhibition	[PMID: 36970141]
T47D	IC₅₀	0.04 μM Compound: D-24851	Cytotoxicity against human T47D cells assessed as cell growth inhibition Cytotoxicity against human T47D cells assessed as cell growth inhibition	[PMID: 33132173]
U-87MG ATCC	IC₅₀	77 nM Compound: fig 2 cmpd 2	Cytotoxicity against multidrug resistance human U87 cells assessed as cell growth inhibition Cytotoxicity against multidrug resistance human U87 cells assessed as cell growth inhibition	[PMID: 36970141]

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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

CAS No. 204205-90-3
Appearance Solid
Molecular Weight 389.83
Formula C₂₂H₁₆ClN₃O₂
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
Synonyms

ZIO 301; D 24851
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

Publications (1)

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Journal Impact Factor

Toxicol Appl Pharmacol

In silico and in vitro assessment of drugs potentially causing adverse effects by inhibiting CYP17A1. [Abstract]

2024 May:486:116945. PMID: 38688424

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)

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

2.5652 mL

12.8261 mL

25.6522 mL

5 mM

0.5130 mL

2.5652 mL

5.1304 mL

10 mM

0.2565 mL

1.2826 mL

2.5652 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, 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

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

Mass Mass

Concentration Concentration

Volume Volume

Molecular Weight Molecular Weight

Dilution Calculator

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

Concentration _(start) Concentration _(start)

Volume _(start) Volume _(start)

Concentration _(final) Concentration _(final)

Volume _(final) Volume _(final)

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 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.

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 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

Purity & Documentation

Select Batch:

Purity: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (282 KB)
SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Portuguese - PT (393 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]. Kapoor S, et al. Indibulin dampens microtubule dynamics and produces synergistic antiproliferative effect with vinblastine in MCF-7 cells: Implications in cancer chemotherapy. Sci Rep. 2018 Aug 17;8(1):12363. [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

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

Keywords

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CAS No.:
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Indibulin

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Covalent Screening Library

Cytoskeleton Compound Library

Orally Active Compound Library

Anti-Lung Cancer Compound Library

Protein-protein Interaction Inhibitor Library

Human Metabolite Library

Heterocyclic Compound Library

Cell Death Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

High-Efficiency Gene Editing Compound Library

Publications Citing Use of MedChemExpress (MCE) Indibulin

All Checkpoint Kinase (Chk) Isoforms

Biological Activity

Chemical Information

Publications (1)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Indibulin

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Covalent Screening Library

Cytoskeleton Compound Library

Orally Active Compound Library

Anti-Lung Cancer Compound Library

Protein-protein Interaction Inhibitor Library

Human Metabolite Library

Heterocyclic Compound Library

Cell Death Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Covalent Screening Library Plus

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

Mass Spectrometry Human Metabolite Library

High-Efficiency Gene Editing Compound Library

Publications Citing Use of MedChemExpress (MCE) Indibulin

All Checkpoint Kinase (Chk) Isoforms

Biological Activity

Chemical Information

Publications (1)

Solvent & Solubility

Purity & Documentation

References

Help & FAQs

Complete Stock Solution Preparation Table

Indibulin Related Classifications

Cat. No.: HY-13649