Art. -Nr.: HY-120786

MPT0B014

(Synonyms: 6-(3′,4′,5′-Trimethoxybenzoyl)quinoline)

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MPT0B014 is a tubulin polymerization inhibitor. MPT0B014 induces cancer cell apoptosis. MPT0B014 can be used for the research of cancer.

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Reinheit: 99.67%
CAS. Nr.: 1215208-59-5
Formel: C₁₉H₁₇NO₄
Molecular Weight:323.34

Speicherung:

Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month

MPT0B014 Chemical Structure

CAS. Nr.: 1215208-59-5

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

MPT0B014 is a tubulin polymerization inhibitor. MPT0B014 induces cancer cell apoptosis. MPT0B014 can be used for the research of cancer^[1].

IC₅₀ & Target

Tubulin polymerization^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HT-29	IC₅₀	24.6 nM Compound: 9	Antiproliferative activity against human HT-29 cells after 72 hrs by methylene blue dye assay Antiproliferative activity against human HT-29 cells after 72 hrs by methylene blue dye assay	[PMID: 20148562]
KB	IC₅₀	24 nM Compound: 9	Antiproliferative activity against human KB cells after 72 hrs by methylene blue dye assay Antiproliferative activity against human KB cells after 72 hrs by methylene blue dye assay	[PMID: 20148562]
MKN-45	IC₅₀	16.3 nM Compound: 9	Antiproliferative activity against human MKN45 cells after 72 hrs by methylene blue dye assay Antiproliferative activity against human MKN45 cells after 72 hrs by methylene blue dye assay	[PMID: 20148562]
NCI-H460	IC₅₀	36 nM Compound: 9	Antiproliferative activity against human H460 cells after 72 hrs by methylene blue dye assay Antiproliferative activity against human H460 cells after 72 hrs by methylene blue dye assay	[PMID: 20148562]

In Vitro

MPT0B014 (0-1 μM; 48 h) inhibits A549, H1299 and H226 cells growth in a dose-dependent manner^[1].
MPT0B014 (0.05-0.3 μM; 24 and 48 h) arrests cell cycle at G2/M and sub-G1 phases and induces apoptosis in A549 cells^[1].

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

Cell Viability Assay^[1]

Cell Line:

A549, H1299, H226 and HUVEC cells
Concentration:

0, 0.025, 0.05, 0.075 and 1 μM
Incubation Time:

48 h
Result:

Inhibited cell viability with IC₅₀s of 0.109±0.01, 0.055±0.004, 0.077±0.005 and 0.536±0.166 μM against A549, H1299, H226 and HUVEC cells, respectively.

Cell Cycle Analysis^[1]

Cell Line:

A549, H1299 and H226
Concentration:

0.05, 0.1 and 0.3 μM
Incubation Time:

24 and 48 h
Result:

Treatment for 24 h led to notable accumulation of cells in the G2/M phase. At 48 h, sub-G1 apoptotic cell populations were increased in a concentration-dependent manner. Cells in the G2/M phase began to rise at 12 h post-treatment and peaked at 24 h. Following this, there was an emergence of cells in the sub-G1 population phase until 48 h.

Western Blot Analysis^[1]

Cell Line:

A549, H1299 and H226
Concentration:

0.05, 0.1 and 0.3 μM
Incubation Time:

24 h
Result:

Resulted in a marked increase in expression of the mitosis marker MPM2 and the proteins cyclin B1, Cdc2, Thr161, Aurora A and Aurora B in a concentration-dependent manner. Decreased the expression of Cdc (Tyr15) and Cdc25C, whereas total protein levels of Cdc2 did not change.

Apoptosis Analysis^[1]

Cell Line:

A549
Concentration:

0.05, 0.075, 0.1 and 0.3 μM
Incubation Time:

48 h
Result:

Induced apoptosis in a concentration-dependent manner.

Western Blot Analysis^[1]

Cell Line:

A549
Concentration:

0.05, 0.1 and 0.3 μM
Incubation Time:

24, 36 and 48 h
Result:

Induced activation of caspases-3, -7, -8 and -9, and cleavage of PARP in a time- and concentration-dependent manner. Significantly induced Bcl-2 phosphorylation. Down-regulated Mcl-1 expression in a concentration-dependent manner.

In Vivo

The combination of MPT0B014 (100 mg/kg; i.v./i.p.; daily for 25 days) and 25 mg/kg Erlotinib (HY-50896) significantly improves A549 tumor inhibition in mice^[1].

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

Animal Model:

Nude athymic mice, A549 xenografts^[1]
Dosage:

100 mg/kg alone or in combination with 25 mg/kg Erlotinib (HY-50896)
Administration:

i.v./i.p., daily for 25 days
Result:

The combined treatment resulted in more significant tumor growth delay (28%) compared with treatment alone (7%). The combination produced significantly higher anti-tumor activity. The growth of A549 cancer cell xenografts was suppressed by 11, 21 and 49% (tumor growth inhibition) after treatment with MPT0B014, Erlotinib and MPT0B014 plus Erlotinib, respectively.

Chemical Information

CAS. Nr. 1215208-59-5
Appearance Solid
Molecular Weight 323.34
Formel C₁₉H₁₇NO₄
Color Off-white to light yellow
SMILES

O=C(C1=CC=C2N=CC=CC2=C1)C3=CC(OC)=C(OC)C(OC)=C3
Synonyms

6-(3′,4′,5′-Trimethoxybenzoyl)quinoline
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	6 months
	-20°C	1 month

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 50 mg/mL (154.64 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

3.0927 mL

15.4636 mL

30.9272 mL

5 mM

0.6185 mL

3.0927 mL

6.1854 mL

10 mM

0.3093 mL

1.5464 mL

3.0927 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, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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)}

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (278 KB)
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)
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]. Tsai AC, et al. In vitro and in vivo anti-tumour effects of MPT0B014, a novel derivative aroylquinoline, and in combination with erlotinib in human non-small-cell lung cancer cells. Br J Pharmacol. 2014 Jan;171(1):122-33. [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, 6 months; -20°C, 1 month. 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	3.0927 mL	15.4636 mL	30.9272 mL	77.3180 mL
	5 mM	0.6185 mL	3.0927 mL	6.1854 mL	15.4636 mL
	10 mM	0.3093 mL	1.5464 mL	3.0927 mL	7.7318 mL
	15 mM	0.2062 mL	1.0309 mL	2.0618 mL	5.1545 mL
	20 mM	0.1546 mL	0.7732 mL	1.5464 mL	3.8659 mL
	25 mM	0.1237 mL	0.6185 mL	1.2371 mL	3.0927 mL
	30 mM	0.1031 mL	0.5155 mL	1.0309 mL	2.5773 mL
	40 mM	0.0773 mL	0.3866 mL	0.7732 mL	1.9329 mL
	50 mM	0.0619 mL	0.3093 mL	0.6185 mL	1.5464 mL
	60 mM	0.0515 mL	0.2577 mL	0.5155 mL	1.2886 mL
	80 mM	0.0387 mL	0.1933 mL	0.3866 mL	0.9665 mL
	100 mM	0.0309 mL	0.1546 mL	0.3093 mL	0.7732 mL

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MPT0B014

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Cytoskeleton Compound Library

Anti-Lung Cancer Compound Library

Protein-protein Interaction Inhibitor Library

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

High-Efficiency Gene Editing Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

MPT0B014

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Cytoskeleton Compound Library

Anti-Lung Cancer Compound Library

Protein-protein Interaction Inhibitor Library

Cell Death Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

High-Throughput Bioactive Compound Library

High-Efficiency Gene Editing Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

MPT0B014 Related Classifications

HY-120786 Related Classifications