[CAS NO. 1124329-14-1] AZ3146
PRODUCTS SPECIFICATIONS [1124329-14-1]
DESCRIPTION [1124329-14-1]
Overview
| MDL | MFCD18384959 |
|---|---|
| Molecular Weight | 452.55 |
| Molecular Formula | C24H32N6O3 |
| SMILES | CN(CC1)CCC1OC2=CC=C(NC3=NC(N(C4CCCC4)C(N5C)=O)=C5C=N3)C(OC)=C2 |
3 Publications Citing Use of MCE
IC50 & Target
|
Mps1 Cat 35 nM (IC 50 ) |
In Vitro
In in vitro kinase assays, AZ3146 inhibits human Mps1 Cat with IC 50 of ~35 nM. AZ3146 also efficiently inhibits autophosphorylation of full-length Mps1 immunoprecipitated from human cells [1] . TTK specific kinase inhibitor AZ3146 can decrease HCC cell growth. In vitro cell cytotoxicity assays are performed on SMMC-7721 and BEL-7404 cells. IC 50 s are calculated as being 7.13 μM (BEL-7404) and 28.62 μM (SMMC-7721). Both cells are further treated under the concentration of IC50 for 4 days. Significant inhibitions of cell proliferation are observed [2] . HCT116 cells are cultured for 10 days in 0.8 μM (the GI 50 ) of AZ3146 , then 2 μM AZ3146 for 3 weeks. Sixteen clones are isolated and cell lines generated, named AzR1-16, all of which are resistant to AZ3146-induced cell death in cell viability assays; AzR3 and 4 have a GI 50 of approximately 3 μM (4-fold resistance), while the remaining clones have a GI 50 of approximately 9 μM (11-fold resistance). When analyzing mitosis by time-lapse microscopy, while 2 μM AZ3146 causes the parental cell line to rapidly exited mitosis in 10 minutes [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Appearance
Solid
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
DMSO : 100 mg/mL ( 220.97 mM ; Need ultrasonic)
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 2.2097 mL | 11.0485 mL | 22.0970 mL |
| 5 mM | 0.4419 mL | 2.2097 mL | 4.4194 mL |
| 10 mM | 0.2210 mL | 1.1049 mL | 2.2097 mL |
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Add each solvent one by one: 10% DMSO >> 90% (20% SBE-β-CD in saline)
Solubility: ≥ 2.5 mg/mL (5.52 mM); Clear solution
References
- [1] Hewitt L, et al. Sustained Mps1 activity is required in mitosis to recruit O-Mad2 to the Mad1-C-Mad2 core complex. J Cell Biol. 2010 Jul 12;190(1):25-34.
- [2] Liu X, et al. TTK activates Akt and promotes proliferation and migration of hepatocellular carcinoma cells. Oncotarget. 2015 Oct 27;6(33):34309-20.
- [3] Gurden MD, et al. Naturally Occurring Mutations in the MPS1 Gene Predispose Cells to Kinase Inhibitor Drug Resistance. Cancer Res. 2015 Aug 15;75(16):3340-54.