AZ 3146

Catalog No.S2731

AZ 3146 Chemical Structure

Molecular Weight(MW): 452.55

AZ3146 is a selective Mps1 inhibitor with IC50 of ~35 nM, contributes to recruitment of CENP-E (kinesin-related motor protein), less potent to FAK, JNK1, JNK2, and Kit.

Size Price Stock Quantity  
In DMSO USD 200 In stock
USD 150 In stock
USD 470 In stock
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2 Customer Reviews

  • Following single thymidine arrest (STA) for 24 h (the numbers above the arrows indicate the time in hours), cells were released into nocodazole (Noc) for 12 h and then treated with DMSO or Noc plus MG132 (to prevent mitotic exit). After 2 h, cells were processed for immunoprecipitation (IP). cells were synchronized using AZ3146 or other small molecule inhibitors. Cell lysates were then analyzed for BUBR1. Noc, nocodazole.

    J Biol Chem 2013 288(49), 35149-58. AZ 3146 purchased from Selleck.

    Dose response curves for the treatment of breast cancer cell lines in the absence or presence of escalating doses of the TTK inhibitor (TTKi) AZ3146. The survival of cells was measured using the CellTitre MTS/MTA assay carried out 6 days after treatment. Percentage survival (n ¼ 3 per dose) was calculated as the percentage of the signal from treated cells to that from control cells.

    Oncogenesis 2014 21, 3:e100. AZ 3146 purchased from Selleck.

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Biological Activity

Description AZ3146 is a selective Mps1 inhibitor with IC50 of ~35 nM, contributes to recruitment of CENP-E (kinesin-related motor protein), less potent to FAK, JNK1, JNK2, and Kit.
Targets
Mps1 [1]
(Cell-free assay)
~35 nM
In vitro

AZ3146 also inhibits FAK, JNK1, JNK2 and Kit. AZ3146 significantly inhibits phosphorylation of Mps1 in cells. Mitotic-specific phospho forms of aurora B and BubR1 are not affected by AZ3146. AZ3146 does not inhibit Cdk1 or aurora B in mitotic cells. HeLa cells treated with nocodazole and 2 μM AZ3146 only delay mitosis briefly and then rereplicate their genomes, indicating that AZ3146 overrides the SAC. AZ3146 also inhibits an already established SAC signal, as after release from a nocodazole block, AZ3146 dramatically accelerates mitotic exit.During an otherwise unperturbed mitosis, AZ3146 reduces the time to complete mitosis from 90 minutes in controls to 32 minutes. Strikingly, ~90% of AZ3146-treated HeLa cells undergo abnormal mitoses, although ~50% enter anaphase without aligning all of their chromosomes, and ~30% exit mitosis without undergoing obvious chromosome segregation. AZ3146 has a dramatic effect on kinetochore localization of Mad2, reducing its levels to ~15%, but its effect on Mad1 is less pronounced, with levels remaining at ~60%. When Mps1 is inhibited by AZ3146 before mitotic entry, subsequent recruitment of Mad1 and Mad2 to kinetochores is abolished. However, if Mps1 is inhibited by AZ3146 after mitotic entry, the Mad1–C-Mad2 core complex remains kinetochore bound, but O-Mad2 is not recruited to the core. [1]

Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
sf9 insect cells MUDGeY5kfGmxbjDhd5NigQ>? NIDrR3pKdmirYnn0bY9vKG:oIF6teIVzdWmwYXygOnhJcXNvdHHn[4VlN0eVVD30ZYdo\WRiZoXscEBt\W6pdHigbJVu[W5iTWDTNUBmgHC{ZYPz[YQhcW5icnXjc41jcW6jboSgZoFkfWyxdnnyeZMhcW6oZXP0[YQhe2Z7IHnud4VkfCClZXzsd{B2e2mwZzC1SmFONUSKVFfGUHRGYV[DVGLDU25JOiCjczDzeYJ{fHKjdHWgZYZ1\XJiNkCgeI8hQTBibXnud{BjgSCobIXvdoV{[2WwY3WgZZN{[XluIFnDOVA:PyCwTR?= NWn5[JBqOjR{NU[yNVc>
human HCT116 cells MkDFSpVv[3Srb36gZZN{[Xl? M1LjOWlvcGmkaYTpc44hd2ZiTYnjMZRi\2enZDD3bYxlKHS7cHWgUXBUOSCjdYTvdIhwe3Cqb4L5cIF1cW:wIHnuJIh2dWGwIFjDWFEyPiClZXzsd{Bi\nSncjCyJIhzeyCrbjDwdoV{\W6lZTDv[kBxem:2ZX;zc41mKGmwaHnibZRweiCPR{GzNkwhUUN3ME2wMlczKM7:TR?= NFPwU|IzPDJ3NkKxOy=>
human HCT116 cells NHfxbFVIem:5dHigbY5pcWKrdHnvckBie3OjeR?= M{TqelczKGh? MmrjS5Jwf3SqIHnubIljcXSrb36gbY4hcHWvYX6gTGNVOTF4IHPlcIx{KGGodHXyJFczKGi{czDifUBOXFRiYYPzZZktKEeLNUC9NU4zKM7:TR?= MWeyOFI2PjJzNx?=

... Click to View More Cell Line Experimental Data

Protocol

Solubility (25°C)

In vitro Ethanol 91 mg/mL (201.08 mM)
DMSO 28 mg/mL (61.87 mM)
Water Insoluble

* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.

Chemical Information

Molecular Weight 452.55
Formula

C24H32N6O3

CAS No. 1124329-14-1
Storage powder
Synonyms N/A

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Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID