2. Cell Cycle/DNA Damage Cytoskeleton Apoptosis
  3. Mps1 Apoptosis
  4. 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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Mps1-IN-5 Chemical Structure

Mps1-IN-5 Chemical Structure

CAS No. : 2890819-31-3

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Mps1-IN-5 Related Antibodies

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Description

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[1].

IC50 & Target

IC50: 29 nM (Mps1)[1]
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.

Mps1-IN-5 Related Antibodies

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.
Molecular Weight

439.52

Formula

C24H25N9
CAS No.
SMILES

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

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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Mps1-IN-5 Related Classifications

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The dilution calculator equation

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

This equation is commonly abbreviated as: C1V1 = C2V2

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
× = ×
C1   V1   C2   V2
Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Mps1-IN-52890819-31-3Mps1ApoptosisMonopolar spindle 1antiproliferativeanti-tumorMCF-74T1 cellsp-Mps1DNA damageapoptosisG2/M phasebreast cancerInhibitorinhibitorinhibit

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