Art. -Nr.: HY-101287

MPT0B392

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MPT0B392, an orally active quinoline derivative, induces c-Jun N-terminal kinase (JNK) activation, leading to apoptosis. MPT0B392 inhibits tubulin polymerization and triggers induction of the mitotic arrest, followed by mitochondrial membrane potential loss and caspases cleavage by activation of JNK and ultimately leads to apoptosis. MPT0B392 is demonstrated to be a novel microtubule-depolymerizing agent and enhances the cytotoxicity of sirolimus in sirolimus-resistant acute leukemic cells and the multidrug resistant cell line.

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Reinheit: 99.63%
CAS. Nr.: 1346169-92-3
Formel: C₁₉H₂₀N₂O₆S
Molecular Weight:404.44

Speicherung:

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

MPT0B392 Chemical Structure

CAS. Nr.: 1346169-92-3

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Preis

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Use of MCE Products

Fluorescent Dye

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

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

JNK

Caspase

Alle JNK Isoform-spezifische Produkte anzeigen :

Alle Caspase Isoform-spezifische Produkte anzeigen :

Cellular Effect

Cell Line	Type	Value	Description	References
HT-29	IC₅₀	16 nM Compound: 15	Growth inhibition of human HT-29 cells after 72 hrs by methylene blue assay Growth inhibition of human HT-29 cells after 72 hrs by methylene blue assay	[PMID: 22060033]
KB	IC₅₀	18 nM Compound: 15	Growth inhibition of human KB cells after 72 hrs by methylene blue assay Growth inhibition of human KB cells after 72 hrs by methylene blue assay	[PMID: 22060033]
MKN-45	IC₅₀	4 nM Compound: 15	Growth inhibition of human MKN45 cells after 72 hrs by methylene blue assay Growth inhibition of human MKN45 cells after 72 hrs by methylene blue assay	[PMID: 22060033]

In Vitro

MPT0B392 (B392) (0.001-0.1 μM; 24 and 48 hours) inhibits the cell viability of HL60, MOLT-4, and CCRF-CEM cells with IC₅₀s of 0.02 μM, 0.03 μM and 0.02 μM, respectively^[1].
MPT0B392 (0.1 μM; 48 hours) induces apoptosis in HL60 cancer cells^[1].
MPT0B392 (0.1 μM for 6-48 hours; 0.01-0.1 μM for 24 and 48 hours) triggers cells arrest in the G2/M phase, followed by accumulation in subG1 phase in a concentration and time-dependent manner^[1].
MPT0B392 (0.1 μM; 48 hours) increases the phosphorylation of Bcl-2, Mcl-1S and decreases in Mcl-1L^[1].

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

Cell Viability Assay^[1]

Cell Line:

HL60 (acute promyelocytic leukemia), MOLT-4 (acute lymphoblastic leukemia), CCRF-CEM (acute lymphoblastic leukemia) cells
Concentration:

0.001, 0.003, 0.01, 0.03, 0.1 μM
Incubation Time:

24 and 48 hours
Result:

Inhibited the cell viability.

Apoptosis Analysis^[1]

Cell Line:

HL60 cells
Concentration:

0.1 μM
Incubation Time:

48 hours
Result:

Induced apoptosis in cancer cells.

Cell Cycle Analysis^[1]

Cell Line:

HL60 cells
Concentration:

0.1 μM or 0.01, 0.03, 0.1 μM
Incubation Time:

0.1 μM for 6-48 hours; 0.01-0.1 μM for 24 and 48 hours
Result:

Triggered cells arrest in the G2/M phase, followed by accumulation in subG1 phase in a concentration and time-dependent manner.

Western Blot Analysis^[1]

Cell Line:

HL60 cells
Concentration:

0.1 μM
Incubation Time:

48 hours
Result:

Increased the phosphorylation of Bcl-2, Mcl-1S and decreased in Mcl-1L.

In Vivo

The effects of MPT0B392 (oral gavage; 50 mg/kg or 100 mg/kg for 12 or 14 days) shows relative potent anti-leukemia activity in a vivo xenograft model^[1].

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

Animal Model:

Severe combined immunodeficient (SCID) mice ^[1]
Dosage:

50 mg/kg or 100 mg/kg
Administration:

Oral gavage; 12 or 14 days
Result:

Resulted in significant tumor growth delay (83.3%) and tumor volume inhibition without loss of body weight.

Chemical Information

CAS. Nr. 1346169-92-3
Appearance Solid
Molecular Weight 404.44
Formel C₁₉H₂₀N₂O₆S
Color Light yellow to yellow
SMILES

NC1=C2C(N=C(S(=O)(C3=CC(OC)=C(OC)C(OC)=C3)=O)C=C2)=CC=C1OC
Versand

Room temperature in continental US; may vary elsewhere.

Speicherung

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

Lösungsmittel & Löslichkeit

In Vitro:

DMSO : 100 mg/mL (247.26 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

2.4726 mL

12.3628 mL

24.7255 mL

5 mM

0.4945 mL

2.4726 mL

4.9451 mL

10 mM

0.2473 mL

1.2363 mL

2.4726 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)}

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 (6.18 mM); Suspended solution; Need ultrasonic

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.

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 (278 KB)
SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 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]. Chao MW, et al. An oral quinoline derivative, MPT0B392, causes leukemic cells mitotic arrest and overcomes drug resistant cancer cells. Oncotarget. 2017 Apr,8(17):27772-27785. [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	2.4726 mL	12.3628 mL	24.7255 mL	61.8139 mL
	5 mM	0.4945 mL	2.4726 mL	4.9451 mL	12.3628 mL
	10 mM	0.2473 mL	1.2363 mL	2.4726 mL	6.1814 mL
	15 mM	0.1648 mL	0.8242 mL	1.6484 mL	4.1209 mL
	20 mM	0.1236 mL	0.6181 mL	1.2363 mL	3.0907 mL
	25 mM	0.0989 mL	0.4945 mL	0.9890 mL	2.4726 mL
	30 mM	0.0824 mL	0.4121 mL	0.8242 mL	2.0605 mL
	40 mM	0.0618 mL	0.3091 mL	0.6181 mL	1.5453 mL
	50 mM	0.0495 mL	0.2473 mL	0.4945 mL	1.2363 mL
	60 mM	0.0412 mL	0.2060 mL	0.4121 mL	1.0302 mL
	80 mM	0.0309 mL	0.1545 mL	0.3091 mL	0.7727 mL
	100 mM	0.0247 mL	0.1236 mL	0.2473 mL	0.6181 mL

Keywords

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MPT0B392

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Immunology/Inflammation Compound Library

MAPK Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Oxygen Sensing Compound Library

Cytoskeleton Compound Library

Anti-Lung Cancer Compound Library

Anti-Blood Cancer Compound Library

Transcription Factor-Targeted Library

Protein-protein Interaction Inhibitor Library

Osteogenesis Compound Library

Heterocyclic Compound Library

Pain-Related Compound Library

Cell Death Library

Anti-Drug-Resistant Compound Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

High-Efficiency Gene Editing Compound Library

Alle JNK Isoform-spezifische Produkte anzeigen

Alle Caspase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

MPT0B392

Apoptosis Compound Library

Cell Cycle/DNA Damage Compound Library

Immunology/Inflammation Compound Library

MAPK Compound Library

Anti-Cancer Compound Library

Anti-Aging Compound Library

Oxygen Sensing Compound Library

Cytoskeleton Compound Library

Anti-Lung Cancer Compound Library

Anti-Blood Cancer Compound Library

Transcription Factor-Targeted Library

Protein-protein Interaction Inhibitor Library

Osteogenesis Compound Library

Heterocyclic Compound Library

Pain-Related Compound Library

Cell Death Library

Anti-Drug-Resistant Compound Library

Anti-Hematopathy Compound Library

Multi-Target Compound Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

Protein Kinase Compound Library

Non-Alcoholic Fatty Liver Disease (NAFLD) Compound Library

Cell Proliferation Compound Library

High-Throughput Bioactive Compound Library

High-Efficiency Gene Editing Compound Library

Alle JNK Isoform-spezifische Produkte anzeigen

Alle Caspase Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

MPT0B392 Related Classifications

HY-101287 Related Classifications