TC-Mps1-12

Name: TC-Mps1-12
Brand: MedChemExpress
SKU: HY-110115
Rating: 4.5 (1 reviews)

Cat. No.: HY-110115 Purity: 99.76%: Data Sheet
COA

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Handling Instructions
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TC-Mps1-12 is a potent and selective monopolar spindle 1 (Mps1) inhibitor, with an IC₅₀ of 6.4 nM.

For research use only. We do not sell to patients.

TC-Mps1-12 Chemical Structure

CAS No. : 1206170-62-8

Size	Stock	Quantity
Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO ready for reconstitution	In-stock	Estimated Time of Arrival: December 31
Solution
10 mM * 1 mL in DMSO	In-stock	Estimated Time of Arrival: December 31
Solid
1 mg	In-stock	Estimated Time of Arrival: December 31
5 mg	In-stock	Estimated Time of Arrival: December 31
10 mg	In-stock	Estimated Time of Arrival: December 31
50 mg	Get quote
100 mg	Get quote

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Based on 1 publication(s) in Google Scholar

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Description

TC-Mps1-12 is a potent and selective monopolar spindle 1 (Mps1) inhibitor, with an IC₅₀ of 6.4 nM^[1].

IC₅₀ & Target

IC50: 6.4 nM (Mps1)^[1]

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	0.84 μM Compound: 12	Antiproliferative activity against human A549 cells after 72 hrs by WST8 assay Antiproliferative activity against human A549 cells after 72 hrs by WST8 assay	[PMID: 24900510]
A549	IC₅₀	840 nM Compound: 14; TC Mps1 12	Antiproliferative activity against human A549 cells by MTT assay Antiproliferative activity against human A549 cells by MTT assay	[PMID: 31121430]
HCT-116	IC₅₀	0.56 μM Compound: 6	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]
HCT-116	GI₅₀	1.6 μM Compound: 6	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]
RERF-LC-AI	IC₅₀	131 nM Compound: 12	Inhibition of FLAG-tagged Mps1 autophosphorylation in human RERF-LC-AI cells expressing Tet-suppressible promotor after 3 hrs by immunoblotting Inhibition of FLAG-tagged Mps1 autophosphorylation in human RERF-LC-AI cells expressing Tet-suppressible promotor after 3 hrs by immunoblotting	[PMID: 24900510]
Sf9	IC₅₀	0.011 μM Compound: 6	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

TC-Mps1-12 inhibits the growth of pMps1 cell lines with IC50 values of 131 nM in autophosphorylation assay^[1].
TC-Mps1-12 (72 hours) inhibits the growth of cells in a dose-dependent manner and with an IC₅₀ values of 0.84 μM^[1].

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

Cell Viability Assay^[1]

Cell Line:	549 cells
Concentration:
Incubation Time:	72 hours
Result:	Inhibited the growth of cells in a dose-dependent manner and with an IC₅₀ values of 0.84 μM.

In Vivo

TC-Mps1-12 (25-100 mg/kg; p.o.; daily; for 19 days) inhibits the growth of A549 cells in a dose-dependent manner in vivo. At a dose of 100 mg/kg, TC-Mps1-12 exhibits 47% tumor growth inhibition without body weight loss^[1].
TC-Mps1-12 shows good PK properties with a Cmax of 3542 ng/mL and AUC of 6604 ng h/mL at an oral dose of 25 mg/kg^[1].

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

Animal Model:	A549 mouse xenograft model^[1]
Dosage:	25 mg/kg, 50 mg/kg, 100 mg/kg
Administration:	Oral administration; once daily; for 19 days
Result:	Inhibited the growth of A549 cells in a dose-dependent manner.

Animal Model:	A549 mouse xenograft model (pharmacokinetic )^[1]
Dosage:	25 mg/kg
Administration:	Oral administration
Result:	C_max = 3542 ng/mL, AUC = 6604 ng h/mL

Molecular Weight

324.38

Formula

C₁₇H₂₀N₆O

CAS No.

1206170-62-8

Appearance

Solid

Color

White to off-white

SMILES

N#CC1=C(N=C(NC2=CC=C(C(N)=O)C=C2)C=C1N)NC(C)(C)C

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Solvent & Solubility

In Vitro:

DMSO : 50 mg/mL (154.14 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	3.0828 mL	15.4140 mL	30.8280 mL
5 mM	0.6166 mL	3.0828 mL	6.1656 mL
10 mM	0.3083 mL	1.5414 mL	3.0828 mL

View the Complete Stock Solution Preparation Table

* 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.

Molarity Calculator
Dilution Calculator

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)

Volume _(start)

Concentration _(final)

Volume _(final)

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage

mg/kg

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(per animal)

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(per animal)

μL

Number of animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Calculation results:

Working solution concentration: mg/mL

Purity & Documentation

Purity: 99.76%

Select Batch:

Data Sheet (274 KB) SDS (251 KB)

COA (248 KB) RP-HPLC (254 KB)

Handling Instructions (2659 KB)

References

[1]. Kusakabe K, et al. Diaminopyridine-based potent and selective mps1 kinase inhibitors binding to an unusual flipped-Peptide conformation. ACS Med Chem Lett. 2012 Jun 6;3(7):560-4. [Content Brief]

Complete Stock Solution Preparation Table

Optional Solvent	Concentration Solvent Mass	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.0828 mL	15.4140 mL	30.8280 mL	77.0701 mL
	5 mM	0.6166 mL	3.0828 mL	6.1656 mL	15.4140 mL
	10 mM	0.3083 mL	1.5414 mL	3.0828 mL	7.7070 mL
	15 mM	0.2055 mL	1.0276 mL	2.0552 mL	5.1380 mL
	20 mM	0.1541 mL	0.7707 mL	1.5414 mL	3.8535 mL
	25 mM	0.1233 mL	0.6166 mL	1.2331 mL	3.0828 mL
	30 mM	0.1028 mL	0.5138 mL	1.0276 mL	2.5690 mL
	40 mM	0.0771 mL	0.3854 mL	0.7707 mL	1.9268 mL
	50 mM	0.0617 mL	0.3083 mL	0.6166 mL	1.5414 mL
	60 mM	0.0514 mL	0.2569 mL	0.5138 mL	1.2845 mL
	80 mM	0.0385 mL	0.1927 mL	0.3854 mL	0.9634 mL
	100 mM	0.0308 mL	0.1541 mL	0.3083 mL	0.7707 mL

TC-Mps1-12 Related Classifications

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:

TC-Mps1-121206170-62-8Mps1Monopolar spindle 1A549cellsInhibitorinhibitorinhibit

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TC-Mps1-12

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Complete Stock Solution Preparation Table

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