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Art. -Nr.: HY-149959

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Mps1-IN-6

Mps1-IN-6 is a potent Mps1 inhibitor with an IC₅₀ value of 2.596 nM. Mps1-IN-6 shows antiproliferative activity. Mps1-IN-6 shows antitumor activity.

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CAS. Nr.: 3043761-59-4
Formel: C₃₅H₃₉N₉O₃
Molecular Weight:633.74

Speicherung:

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

Data Sheet (275 KB)

Mps1-IN-6 Chemical Structure

CAS. Nr.: 3043761-59-4

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Fluorescent Dye

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

Mps1-IN-6 is a potent Mps1 inhibitor with an IC₅₀ value of 2.596 nM. Mps1-IN-6 shows antiproliferative activity. Mps1-IN-6 shows antitumor activity^[1].

IC₅₀ & Target

IC₅₀: 2.596 nM (Mps1)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HT-29	IC₅₀	>10 μM Compound: 31	Antiproliferative activity against human HT-29 cells assessed inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human HT-29 cells assessed inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 37037136]
MCF7	IC₅₀	>10 μM Compound: 31	Antiproliferative activity against human MCF7 cells assessed inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MCF7 cells assessed inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 37037136]
MDA-MB-468	IC₅₀	0.221 μM Compound: 31	Antiproliferative activity against human MDA-MB-468 cells assessed inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MDA-MB-468 cells assessed inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 37037136]
MV4-11	IC₅₀	0.823 μM Compound: 31	Antiproliferative activity against human MV4-11 cells assessed inhibition of cell growth incubated for 72 hrs by CCK-8 assay Antiproliferative activity against human MV4-11 cells assessed inhibition of cell growth incubated for 72 hrs by CCK-8 assay	[PMID: 37037136]

In Vitro

Mps1-IN-6 (compound 31) (0-10 µM; 72 h) shows antiproliferative activity with IC₅₀s of 0.221, >10, >10, 0.823, >10 µM for MDA-MB-468, MCF-7, REB, MV4-11, HT-29 cells, respectively^[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-468, MCF-7, REB, MV4-11, HT-29 cells
Concentration:

0-10 µM
Incubation Time:

72 h
Result:

Showed antiproliferative activity with IC₅₀s of 0.221, >10, >10, 0.823, >10 µM for MDA-MB-468, MCF-7, REB, MV4-11, HT-29 cells, respectively.

In Vivo

Mps1-IN-6 (30, 60 mg/kg; i.v.; once daily for 21 days) shows antitumor activity in mice^[1].
Pharmacokinetic Parameters of Mps1-IN-6 in Male Sprague-Dawley rats^[1].

parameters (unit)	iv (2 mg/kg)	po (10 mg/kg)
C₀ (ng/mL)	5237	-
C_max (ng/mL)	2920	160
T_1/2 (h)	0.825	1.05
T_max (h)	0.083	0.333
AUC_(0-t) (h*ng/mL)	1050	204
AUC_(0-∞) (h*ng/mL)	1052	208
MRT_(0-t) (h)	0.34	1.11
MRT_(0-∞) (h)	0.354	1.23
CL (mL/kg/min)	32	-
V_{ss (L/kg)}	0.672	-
F %	-	3.95

Male Sprague-Dawley rats, 2 mg/kg iv; 10 mg/kg po.

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

Animal Model:

Six to eight week-old female BALB/c nude mice (MDA-MB-468 mouse xenograft model)^[1]
Dosage:

30, 60 mg/kg
Administration:

I.v.; once daily for 21 days
Result:

Inhibited the tumor growth with TGI values of 21%, 34% for 30, 60 mg/kg, respectively.

Chemical Information

CAS. Nr. 3043761-59-4
Molecular Weight 633.74
Formel C₃₅H₃₉N₉O₃
SMILES

CCC1=CC=CC(CC)=C1N2CCN3C=C(C=C3C2=O)C4=C5C=NNC5=NC(NC6=C(C=C(C=C6)N7CCN(CC7)C(C)=O)OC)=N4
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 (275 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]. Shihe Hu, et al. Discovery of pyrazolo[3,4-b]pyridine derivatives as novel and potent Mps1 inhibitors for the treatment of cancer. European Journal of Medicinal Chemistry. 2023, 253: 115334.

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.

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MOQ

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100 mg

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