Art. -Nr.: HY-16114

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BNC105

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BNC105 is a tubulin polymerization inhibitor with potent antiproliferative and tumor vascular disrupting properties.

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Reinheit: 98.27%
CAS. Nr.: 945771-74-4
Formel: C₂₀H₂₀O₇
Molecular Weight:372.37

Speicherung:

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

BNC105 Chemical Structure

CAS. Nr.: 945771-74-4

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Biologische Aktivität
- Beschreibung
- Cellular Effect
- In Vitro
- Clinical Trial
Chemical Information
Publications (1)
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

BNC105 is a tubulin polymerization inhibitor with potent antiproliferative and tumor vascular disrupting properties.

Cellular Effect

Cell Line	Type	Value	Description	References
786-0	IC₅₀	0.39 nM Compound: 8, BNC105P	Antiproliferative activity against MDR-1 overexpressing human 786-0 cells in presence of MDR1 inhibitor verapamil Antiproliferative activity against MDR-1 overexpressing human 786-0 cells in presence of MDR1 inhibitor verapamil	[PMID: 21774499]
786-0	IC₅₀	0.58 nM Compound: 8, BNC105P	Antiproliferative activity against MDR-1 overexpressing human 786-0 cells Antiproliferative activity against MDR-1 overexpressing human 786-0 cells	[PMID: 21774499]
A2780	IC₅₀	0.03 nM Compound: 8, BNC105P	Cytotoxicity against human A2780 cells Cytotoxicity against human A2780 cells	[PMID: 21774499]
A2780 ADR	IC₅₀	0.06 nM Compound: 8, BNC105P	Cytotoxicity against human A2780/ADR cells Cytotoxicity against human A2780/ADR cells	[PMID: 21774499]
A2780cisR	IC₅₀	0.01 nM Compound: 8, BNC105P	Cytotoxicity against human A2780cis cells Cytotoxicity against human A2780cis cells	[PMID: 21774499]
A-375	IC₅₀	1.5 nM Compound: 8, BNC105P	Antiproliferative activity against human A375 after 48 hrs by spectrophotometry Antiproliferative activity against human A375 after 48 hrs by spectrophotometry	[PMID: 21774499]
A-431	IC₅₀	18.6 nM Compound: 8, BNC105P	Antiproliferative activity against human A431 after 48 hrs by spectrophotometry Antiproliferative activity against human A431 after 48 hrs by spectrophotometry	[PMID: 21774499]
AU565	IC₅₀	5.8 nM Compound: 8, BNC105P	Antiproliferative activity against human AU565 after 48 hrs by spectrophotometry Antiproliferative activity against human AU565 after 48 hrs by spectrophotometry	[PMID: 21774499]
BT-549	IC₅₀	0.34 nM Compound: 8, BNC105P	Antiproliferative activity against human BT549 after 48 hrs by spectrophotometry Antiproliferative activity against human BT549 after 48 hrs by spectrophotometry	[PMID: 21774499]
Calu-6	IC₅₀	0.16 nM Compound: 8, BNC105P	Antiproliferative activity against human Calu6 after 48 hrs by spectrophotometry Antiproliferative activity against human Calu6 after 48 hrs by spectrophotometry	[PMID: 21774499]
DU-145	IC₅₀	0.36 nM Compound: 8, BNC105P	Antiproliferative activity against human DU145 after 48 hrs by spectrophotometry Antiproliferative activity against human DU145 after 48 hrs by spectrophotometry	[PMID: 21774499]
HUVEC	IC₅₀	0.31 nM Compound: 8, BNC105P	Antiproliferative activity against HUVEC grown in presence of growth factors after 48 hrs by spectrophotometry Antiproliferative activity against HUVEC grown in presence of growth factors after 48 hrs by spectrophotometry	[PMID: 21774499]
HUVEC	IC₅₀	25 nM Compound: 8, BNC105P	Antiproliferative activity against HUVEC grown in absence of growth factors after 48 hrs by spectrophotometry Antiproliferative activity against HUVEC grown in absence of growth factors after 48 hrs by spectrophotometry	[PMID: 21774499]
LoVo	IC₅₀	0.24 nM Compound: 8, BNC105P	Antiproliferative activity against human LoVo after 48 hrs by spectrophotometry Antiproliferative activity against human LoVo after 48 hrs by spectrophotometry	[PMID: 21774499]
MCF7	IC₅₀	2.4 nM Compound: 8, BNC105P	Antiproliferative activity against human MCF7 cells assessed after 48 hrs by spectrophotometry Antiproliferative activity against human MCF7 cells assessed after 48 hrs by spectrophotometry	[PMID: 21774499]
MDA-MB-231	IC₅₀	0.63 nM Compound: 8, BNC105P	Antiproliferative activity against human MDA-MB-231 after 48 hrs by spectrophotometry Antiproliferative activity against human MDA-MB-231 after 48 hrs by spectrophotometry	[PMID: 21774499]
SK-OV-3	IC₅₀	0.59 nM Compound: 8, BNC105P	Antiproliferative activity against human SKOV3 after 48 hrs by spectrophotometry Antiproliferative activity against human SKOV3 after 48 hrs by spectrophotometry	[PMID: 21774499]
U-87MG ATCC	IC₅₀	0.41 nM Compound: 8, BNC105P	Antiproliferative activity against human U87MG after 48 hrs by spectrophotometry Antiproliferative activity against human U87MG after 48 hrs by spectrophotometry	[PMID: 21774499]

In Vitro

BNC105 exhibits excellent potency against a panel of different cancer cell lines with IC₅₀ <1 nM for DU145, Calu-6, MDA-MB-231 etc.
The selectivity observed for BNC105 against activated over quiescent HUVECs is also observed in human aortic arterial endothelial cells (HAAECs).
BNC105 also exhibits good potency toward the cisplatin resistant cell line A2780cis.

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

Clinical Trial

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

Chemical Information

CAS. Nr. 945771-74-4
Appearance Solid
Molecular Weight 372.37
Formel C₂₀H₂₀O₇
Color Light yellow to yellow
SMILES

COC1=CC(C(C2=C(C)OC3=C(O)C(OC)=CC=C23)=O)=CC(OC)=C1OC
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Biochem Biophys Res Commun

Unraveling the molecular mechanism of BNC105, a phase II clinical trial vascular disrupting agent, provides insights into drug design. [Abstract]

2020 Feb 18;S0006-291X(20)30008-5. PMID: 32085900

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 25 mg/mL (67.14 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

2.6855 mL

13.4276 mL

26.8551 mL

5 mM

0.5371 mL

2.6855 mL

5.3710 mL

10 mM

0.2686 mL

1.3428 mL

2.6855 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.

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 (6.71 mM); Suspended solution; Need ultrasonic and warming

This protocol yields a suspended solution of 2.5 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 (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% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (6.71 mM); Suspended solution; Need ultrasonic and warming

This protocol yields a suspended solution of 2.5 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 (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

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

Solubility: ≥ 2.5 mg/mL (6.71 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 (280 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)
- Korean - KR (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)

Verweise

[1]. Flynn BL, et al. Discovery of 7-hydroxy-6-methoxy-2-methyl-3-(3,4,5-trimethoxybenzoyl)benzo[b]furan (BNC105), a tubulin polymerization inhibitor with potent antiproliferative and tumor vascular disrupting properties. J Med Chem. 2011 Sep 8;54(17):6014-27. [Content Brief]

[2]. Kremmidiotis G, et al. BNC105: a novel tubulin polymerization inhibitor that selectively disrupts tumor vasculature and displays single-agent antitumor efficacy. Mol Cancer Ther. 2010 Jun;9(6):1562-73. [Content Brief]

[3]. Inglis DJ, et al. The vascular disrupting agent BNC105 potentiates the efficacy of VEGF and mTOR inhibitors in renal and breast cancer. Cancer Biol Ther. 2014;15(11):1552-60. [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	2.6855 mL	13.4276 mL	26.8551 mL	67.1378 mL
	5 mM	0.5371 mL	2.6855 mL	5.3710 mL	13.4276 mL
	10 mM	0.2686 mL	1.3428 mL	2.6855 mL	6.7138 mL
	15 mM	0.1790 mL	0.8952 mL	1.7903 mL	4.4759 mL
	20 mM	0.1343 mL	0.6714 mL	1.3428 mL	3.3569 mL
	25 mM	0.1074 mL	0.5371 mL	1.0742 mL	2.6855 mL
	30 mM	0.0895 mL	0.4476 mL	0.8952 mL	2.2379 mL
	40 mM	0.0671 mL	0.3357 mL	0.6714 mL	1.6784 mL
	50 mM	0.0537 mL	0.2686 mL	0.5371 mL	1.3428 mL
	60 mM	0.0448 mL	0.2238 mL	0.4476 mL	1.1190 mL

Keywords

BNC105

1 Cited Publications

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BNC105

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Publications Citing Use of MedChemExpress (MCE) BNC105

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

BNC105

Anti-COVID-19 Compound Library

Cytoskeleton Compound Library

Anti-Lung Cancer Compound Library

Protein-protein Interaction Inhibitor Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Drug Repurposing Compound Library Plus

Clinical Compound Library Plus

Bioactive Compound Library

High-Throughput Bioactive Compound Library

High-Efficiency Gene Editing Compound Library

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Clinical Compound Library

Anti-Aging Compound Library

Drug Repurposing Compound Library

Publications Citing Use of MedChemExpress (MCE) BNC105

Biologische Aktivität

Chemical Information

Publications (1)

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

BNC105 Related Classifications

HY-16114 Related Classifications