An inhibitor of Mps1/TTK
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Mps1/TTK Inhibitor

Item No. 25554

Product Insert (PDF)Safety Data Sheet (SDS) (PDF)
Technical Information
Formal Name
N-(2,6-diethylphenyl)-4,5-dihydro-8-[[2-methoxy-4-(4-methyl-1-piperazinyl)phenyl]amino]-1-methyl-1H-pyrazolo[4,3-h]quinazoline-3-carboxamide
CAS Number
1202055-39-7
Molecular Formula
C33H40N8O2
Formula Weight
580.7
Purity
≥98%
Formulation (Request formulation change)
A solid
Solubility(Learn about Variance in Solubility)
Water: Slightly Soluble
SMILES
CN(N=C1C(NC2=C(CC)C=CC=C2CC)=O)C3=C1CCC4=C3N=C(NC5=C(OC)C=C(N6CCN(C)CC6)C=C5)N=C4
InChi Code
InChI=1S/C33H40N8O2/c1-6-21-9-8-10-22(7-2)28(21)36-32(42)30-25-13-11-23-20-34-33(37-29(23)31(25)40(4)38-30)35-26-14-12-24(19-27(26)43-5)41-17-15-39(3)16-18-41/h8-10,12,14,19-20H,6-7,11,13,15-18H2,1-5H3,(H,36,42)(H,34,35,37)
InChi Key
DHKBTAOKHPQHKT-UHFFFAOYSA-N
Shipping & Storage Information
Storage
-20°C
Shipping
Room temperature in continental US; may vary elsewhere
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    1 mg

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    10 mg

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    25 mg

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    Product Description

    Mps1/TTK inhibitor is an inhibitor of monopolar spindle 1 (Mps1/TTK; IC50 = 5.8 nM), a kinase involved in mitotic spindle checkpoint signaling that is overexpressed in certain cancerous tumors.1,2 It inhibits Mps1 phosphorylation of kinetochore scaffold 1 (KNL1) and increases the rate of mitosis and the number of cells entering anaphase within 15 minutes, indicating Mps1 checkpoint inhibition, when used at a concentration of 100 nM.1 Mps1/TTK inhibitor (50 and 100 nM) increases the number of missegregated chromosomes, with an increased number of errors at 100 nM compared with 50 nM. It also inhibits colony formation of DLD1, HCT116, and U2OS cells (IC50s = 24.6, 20.1, and 20.6 nM, respectively).

    WARNING This product is not for human or veterinary use.

    References & Product Citations
    Product Description References

    1. Koch, A., Maia, A., Janssen, A., et al. Molecular basis underlying resistance to Mps1/TTK inhibitors. Oncogene 35(19), 2518-2528 (2016).

    2. Alimova, I., Ng, J., Harris, P., et al. MPS1 kinase as a potential therapeutic target in medulloblastoma. Oncol. Rep. 36(5), 2633-2640 (2016).