Art. -Nr.: HY-12603

CCT251455

Name: CCT251455
Brand: MedChemExpress
SKU: HY-12603
Price: 500.00 USD
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CCT251455 is a potent and selective mitotic kinase monopolar spindle 1 (MPS1) inhibitor with an IC₅₀ of 3 nM.

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Reinheit: 99.10%
CAS. Nr.: 1400284-80-1
Formel: C₂₆H₂₆ClN₇O₂
Molecular Weight:503.98

Speicherung:

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

CCT251455 Chemical Structure

CAS. Nr.: 1400284-80-1

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

Biologische Aktivität

Beschreibung

CCT251455 is a potent and selective mitotic kinase monopolar spindle 1 (MPS1) inhibitor with an IC₅₀ of 3 nM.

IC₅₀ & Target

IC50: 3 nM (MPS1)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
HCT-116	GI₅₀	0.16 μM Compound: 65, CCT251455	Growth inhibition in human HCT116 cells after 72 hrs by MTT assay Growth inhibition in human HCT116 cells after 72 hrs by MTT assay	[PMID: 24256217]
HCT-116	GI₅₀	0.16 μM Compound: 53j; CCT251455	Growth inhibition of human HCT-116 cells Growth inhibition of human HCT-116 cells	[PMID: 38795520]
HCT-116	IC₅₀	0.043 μM Compound: 1; CCT251455	Inhibition of wild type Myc-ectopic MPS1 (unknown origin) expressed in human HCT116 cells assessed as autophosphorylation at Thr33/Ser37 after 2 hrs by electrochemiluminescence assay in presence of MG132 Inhibition of wild type Myc-ectopic MPS1 (unknown origin) expressed in human HCT116 cells assessed as autophosphorylation at Thr33/Ser37 after 2 hrs by electrochemiluminescence assay in presence of MG132	[PMID: 27055065]
HCT-116	IC₅₀	0.043 μM Compound: 65, CCT251455	Inhibition of Myc-tagged wild type MPS1 autophosphorylation in human HCT116 cells after 2 hrs in presence of proteosome inhibitor MG132 Inhibition of Myc-tagged wild type MPS1 autophosphorylation in human HCT116 cells after 2 hrs in presence of proteosome inhibitor MG132	[PMID: 24256217]
Sf9	IC₅₀	0.003 μM Compound: 1; CCT251455	Inhibition of human full length MPS1 expressed in recombinant baculovirus infected Sf9 insect cells using 5FAM-DHTGFLTEYVATRCONH2 as substrate after 60 to 90 mins Inhibition of human full length MPS1 expressed in recombinant baculovirus infected Sf9 insect cells using 5FAM-DHTGFLTEYVATRCONH2 as substrate after 60 to 90 mins	[PMID: 27055065]
Sf9	IC₅₀	0.003 μM Compound: 65, CCT251455	Inhibition of N-terminal 6XHis-tagged/GST-tagged full length human MPS1 expressed in recombinant baculovirus infected sf9 insect cells using 5FAM-DHTGFLTEYVATRCONH2 as substrate after 60 to 90 mins by fluorescence assay Inhibition of N-terminal 6XHis-tagged/GST-tagged full length human MPS1 expressed in recombinant baculovirus infected sf9 insect cells using 5FAM-DHTGFLTEYVATRCONH2 as substrate after 60 to 90 mins by fluorescence assay	[PMID: 24256217]

In Vitro

CCT251455 is a highly potent inhibitor of MPS1 that demonstrates high selectivity versus kinases tested in a broad kinome profiling panel. CCT251455 inhibits P-MPS1 with an IC₅₀ of 0.04 μM in cell-based assay and has a GI₅₀ of 0.16 μM^[1].

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

In Vivo

CCT251455 demonstrates a good oral pharmacokinetic profile in mouse and rat as well as inhibition of MPS1 activity in vivo following oral administration^[1].

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

Chemical Information

CAS. Nr. 1400284-80-1
Appearance Solid
Molecular Weight 503.98
Formel C₂₆H₂₆ClN₇O₂
Color Light yellow to brown
SMILES

O=C(N1C(C2=CN(C)N=C2)=CC3=C1C=C(NC4=CC=C(C5=CN=CN5C)C=C4Cl)N=C3)OC(C)(C)C
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 : 100 mg/mL (198.42 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

1.9842 mL

9.9210 mL

19.8421 mL

5 mM

0.3968 mL

1.9842 mL

3.9684 mL

10 mM

0.1984 mL

0.9921 mL

1.9842 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 (4.96 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).

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.

Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)

Solubility: 2.5 mg/mL (4.96 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 900 μL 20% SBE-β-CD in Saline, and mix evenly.

Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: ≥ 2.5 mg/mL (4.96 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

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

Protokoll

Cell Assay^[1]

HCT116 cells are treated with 0-20 μM CCT251455 for 72 h. Cell viability is measured using the MTT assay^[1].

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

Animal Administration^[1]

Mice^[1]

^[1]Human HCT116 colon carcinoma cells are sc injected bilaterally in the flanks of female CrTac:NCr-Fox1(nu) athymic mice. Once tumors reach a mean diameter of 8 mm (day 15), mice are dosed twice at a 12 h intervals with 50, 75, or 100 mg/kg of CCT251455 in 10% (v/v) DMSO and 5% (v/v) Tween 20 in saline. Mice are culled (n=3 per group) at 2, 10, and 72 h after the second dose. Tumors are snap-frozen and stored at -80 °C until analysis^[1].

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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (274 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]. Naud S, et al. Structure-based design of orally bioavailable 1H-pyrrolo[3,2-c]pyridine inhibitors of mitotic kinase monopolar spindle 1 (MPS1). J Med Chem. 2013 Dec 27;56(24):10045-65. [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	1.9842 mL	9.9210 mL	19.8421 mL	49.6051 mL
	5 mM	0.3968 mL	1.9842 mL	3.9684 mL	9.9210 mL
	10 mM	0.1984 mL	0.9921 mL	1.9842 mL	4.9605 mL
	15 mM	0.1323 mL	0.6614 mL	1.3228 mL	3.3070 mL
	20 mM	0.0992 mL	0.4961 mL	0.9921 mL	2.4803 mL
	25 mM	0.0794 mL	0.3968 mL	0.7937 mL	1.9842 mL
	30 mM	0.0661 mL	0.3307 mL	0.6614 mL	1.6535 mL
	40 mM	0.0496 mL	0.2480 mL	0.4961 mL	1.2401 mL
	50 mM	0.0397 mL	0.1984 mL	0.3968 mL	0.9921 mL
	60 mM	0.0331 mL	0.1654 mL	0.3307 mL	0.8268 mL
	80 mM	0.0248 mL	0.1240 mL	0.2480 mL	0.6201 mL
	100 mM	0.0198 mL	0.0992 mL	0.1984 mL	0.4961 mL

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Keywords

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CCT251455

NMS-P715

BAY1217389

AZ3146

Luvixasertib

Empesertib

BOS-172722

Mps1-IN-3

Mps1-IN-1

TC-Mps1-12

Luvixasertib hydrochloride

Mps1-IN-1 dihydrochloride

Luvixasertib hydrochloride (Standard)

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

Bioz

CCT251455

NMS-P715

BAY1217389

AZ3146

Luvixasertib

Empesertib

BOS-172722

Mps1-IN-3

Mps1-IN-1

TC-Mps1-12

Luvixasertib hydrochloride

Mps1-IN-1 dihydrochloride

Luvixasertib hydrochloride (Standard)

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Protokoll

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

CCT251455 Related Classifications

HY-12603 Related Classifications

Bioz