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Art. -Nr.: HY-151980

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Mps1-IN-5

Mps1-IN-5 is a potent and orally active Mps1 inhibitor with an IC₅₀ value of 29 nM. Mps1-IN-5 induces Apoptosis and cell cycle arrests at G2/M phase. Mps1-IN-5 shows antiproliferative activity and anti-tumor activity. Mps1-IN-5 inhibits phosphorylation of Mps1 and induces DNA damage.

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CAS. Nr.: 2890819-31-3
Formel: C₂₄H₂₅N₉
Molecular Weight:439.52

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (276 KB)

Mps1-IN-5 Chemical Structure

CAS. Nr.: 2890819-31-3

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Use of MCE Products

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

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

Biologische Aktivität

Beschreibung

IC₅₀ & Target

IC₅₀: 29 nM (Mps1)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
4T1	IC₅₀	0.4 μM Compound: 12	Antiproliferative activity against 4T1 cells assessed as inhibition of cell viability by MTT assay Antiproliferative activity against 4T1 cells assessed as inhibition of cell viability by MTT assay	[PMID: 36370549]
A549	IC₅₀	2.03 μM Compound: 12	Antiproliferative activity against human A549 cells assessed as inhibition of cell viability by MTT assay Antiproliferative activity against human A549 cells assessed as inhibition of cell viability by MTT assay	[PMID: 36370549]
AGS	IC₅₀	>3 μM Compound: 12	Antiproliferative activity against human AGS cells assessed as inhibition of cell viability by MTT assay Antiproliferative activity against human AGS cells assessed as inhibition of cell viability by MTT assay	[PMID: 36370549]
ES-2	IC₅₀	>3 μM Compound: 12	Antiproliferative activity against human ES2 cells assessed as inhibition of cell viability by MTT assay Antiproliferative activity against human ES2 cells assessed as inhibition of cell viability by MTT assay	[PMID: 36370549]
HCT-116	IC₅₀	1.06 μM Compound: 12	Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell viability by MTT assay Antiproliferative activity against human HCT-116 cells assessed as inhibition of cell viability by MTT assay	[PMID: 36370549]
HEY	IC₅₀	>3 μM Compound: 12	Antiproliferative activity against human HEY cells assessed as inhibition of cell viability by MTT assay Antiproliferative activity against human HEY cells assessed as inhibition of cell viability by MTT assay	[PMID: 36370549]
MCF7	IC₅₀	0.37 μM Compound: 12	Antiproliferative activity against human MCF7 cells assessed as inhibition of cell viability by MTT assay Antiproliferative activity against human MCF7 cells assessed as inhibition of cell viability by MTT assay	[PMID: 36370549]
MDA-MB-231	IC₅₀	2.68 μM Compound: 12	Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell viability by MTT assay Antiproliferative activity against human MDA-MB-231 cells assessed as inhibition of cell viability by MTT assay	[PMID: 36370549]
OVCAR-3	IC₅₀	>3 μM Compound: 12	Antiproliferative activity against human OVCAR-3 cells assessed as inhibition of cell viability by MTT assay Antiproliferative activity against human OVCAR-3 cells assessed as inhibition of cell viability by MTT assay	[PMID: 36370549]

In Vitro

Mps1-IN-5 (compound 12) (0-10 µM,24, 48, 72 h) inhibits the proliferation of MCF-7 and 4T1 cells in a time-dependent manner^[1].
Mps1-IN-5 (0, 0.5, 1.0, 5.0 µM; 24, 48 h) induces apoptosis and cell cycle arrests at G2/M phase in a dose-dependent manner in MCF-7 and 4T1 cells^[1].
Mps1-IN-5 (0, 0.03, 0.1, 1, 3 µM; 2 h) inhibits phosphorylation of Mps1 and induces DNA damage^[1].

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

Cell Proliferation Assay^[1]

Cell Line:

MDA-MB-231, MCF-7, 4T1, HEY, OVCAR-3, ES-2, HCT-116, A549, AGS cells
Concentration:

0-3 µM
Incubation Time:

72 h
Result:

Inhibited the cell growth with IC₅₀s of 2.68, 0.37, 0.40, >3, >3, >3, 1.06, 2.03, >3 µM for MDA-MB-231, MCF-7, 4T1, HEY, OVCAR-3, ES-2, HCT-116, A549, AGS cells, respectively.

Cell Cycle Analysis^[1]

Cell Line:

MCF-7, 4T1 cells
Concentration:

0, 0.5, 1.0, 5.0 µM
Incubation Time:

24 h
Result:

Induced cell cycle arrest of MCF-7 and 4T1 cells at the G2/M phase in a dose-dependent manner, decreased the protein expression levels of Cyclin B1 and CDK1.

Apoptosis Analysis^[1]

Cell Line:

MCF-7, 4T1 cells
Concentration:

0, 0.5, 1.0, 5.0 µM
Incubation Time:

48 h
Result:

Induced apoptosis and significantly increased the expression level of an apoptosis-related protein, cleaved poly ADP-ribose polymerase (PARP).

Western Blot Analysis^[1]

Cell Line:

MCF-7, 4T1 cells
Concentration:

0, 0.03, 0.1, 1, 3 µM
Incubation Time:

2 h
Result:

Increased the expression of level of γ-H2AX protein and decreased the protein expression of p-Mps1 in a dose-dependent manner.

In Vivo

Mps1-IN-5 (30, 60 mg/kg; p.o.; daily for 15 days) inhibits tumor growth without obvious toxicity in breast cancer models^[1].

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

Animal Model:

6-8 weeks, female BALB/C mice (4T1-luc mouse xenograft model)^[1]
Dosage:

30, 60 mg/kg
Administration:

P.o.; daily for 15 days
Result:

Significantly suppressed tumor growth and caused negligible damage to organs such as heart, liver, spleen, lung and kidneys.

Related Protocols :

Chemical Information

CAS. Nr. 2890819-31-3
Molecular Weight 439.52
Formel C₂₄H₂₅N₉
SMILES

CN1CCN(CC1)C2=CC=C(C=C2)NC3=NC4=C(C(N5N=C(C6=CC=CC=C65)N)=N3)C=CN4
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (276 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]. Li X, et al. Design, synthesis and biological evaluation of a new class of 7H-pyrrolo[2,3-d]pyrimidine derivatives as Mps1 inhibitors for the treatment of breast cancer. Eur J Med Chem. 2023 Jan 5;245(Pt 1):114887.

Calculators

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)}

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.

Bioz

Keywords

MOQ

Minimum order quantity

100 mg

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