MedKoo Cat#: 406239 | Name: AZ3146
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Description:

WARNING: This product is for research use only, not for human or veterinary use.

AZ3146 is a novel and potent Mps1 inhibitor, which was used to probe the role of Mps1's catalytic activity during mitosis. AZ3146 also inhibits FAK, JNK1, JNK2, KSP and Kit. In in vitro kinase assays, AZ3146 inhibited human Mps1Cat with an IC50 (50% inhibitory concentration) of ~35 nM. AZ3146 also efficiently inhibited autophosphorylation of full-length Mps1 immunoprecipitated from human cells.

Chemical Structure

AZ3146
AZ3146
CAS#1124329-14-1

Theoretical Analysis

MedKoo Cat#: 406239

Name: AZ3146

CAS#: 1124329-14-1

Chemical Formula: C24H32N6O3

Exact Mass: 452.2536

Molecular Weight: 452.55

Elemental Analysis: C, 63.70; H, 7.13; N, 18.57; O, 10.61

Price and Availability

Size Price Availability Quantity
10mg USD 90.00 Ready to ship
25mg USD 150.00 Ready to ship
50mg USD 300.00 Ready to ship
100mg USD 500.00 Ready to ship
200mg USD 850.00 Ready to ship
500mg USD 1,350.00 Ready to ship
1g USD 2,150.00 Ready to ship
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Related CAS #
No Data
Synonym
AZ3146; AZ 3146; AZ-3146
IUPAC/Chemical Name
9-cyclopentyl-2-(2-methoxy-4-(1-methylpiperidin-4-yloxy)phenylamino)-7-methyl-7H-purin-8(9H)-one
InChi Key
YUKWVHPTFRQHMF-UHFFFAOYSA-N
InChi Code
InChI=1S/C24H32N6O3/c1-28-12-10-17(11-13-28)33-18-8-9-19(21(14-18)32-3)26-23-25-15-20-22(27-23)30(24(31)29(20)2)16-6-4-5-7-16/h8-9,14-17H,4-7,10-13H2,1-3H3,(H,25,26,27)
SMILES Code
O=C1N(C)C2=CN=C(NC3=CC=C(OC4CCN(C)CC4)C=C3OC)N=C2N1C5CCCC5
Appearance
white to off-white solid powder
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO, not in water
Shelf Life
>2 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.9001
More Info
        
Biological target:
AZ3146 is a Mps1 inhibitor with IC50 of 35 nM for Mps1Cat.
In vitro activity:
To confirm the inhibition effect of AZ3146, PCR assay was used to detect the TTK level treated with AZ3146 for 24h. As shown in Fig. 1 F-G, the expression of TTK were decreased when added with TTK inhibitor compared to control group. These results indicate that AZ3146 effectively inhibited the TTK expression at both the RNA and protein levels in liver cancer. Reference: Biochem Biophys Res Commun. 2021 Apr 23;550:84-91. https://pubmed.ncbi.nlm.nih.gov/33689884/
In vivo activity:
N/A
Solvent mg/mL mM
Solubility
DMSO 34.9 77.12
DMF 5.0 11.05
DMF:PBS (pH 7.2) (1:1) 0.5 1.10
Ethanol 42.3 93.49
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.

Preparing Stock Solutions

The following data is based on the product molecular weight 452.55 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.

Recalculate based on batch purity %
Concentration / Solvent Volume / Mass 1 mg 5 mg 10 mg
1 mM 1.15 mL 5.76 mL 11.51 mL
5 mM 0.23 mL 1.15 mL 2.3 mL
10 mM 0.12 mL 0.58 mL 1.15 mL
50 mM 0.02 mL 0.12 mL 0.23 mL
Formulation protocol:
1. Zhang H, Yao W, Zhang M, Lu Y, Tang J, Jiang M, Mou X, You G, Liang X. TTK inhibitor promotes radiosensitivity of liver cancer cells through p21. Biochem Biophys Res Commun. 2021 Apr 23;550:84-91. doi: 10.1016/j.bbrc.2021.01.089. Epub 2021 Mar 6. Erratum in: Biochem Biophys Res Commun. 2021 May 28;555:214. PMID: 33689884. 2. Liu X, Liao W, Yuan Q, Ou Y, Huang J. TTK activates Akt and promotes proliferation and migration of hepatocellular carcinoma cells. Oncotarget. 2015 Oct 27;6(33):34309-20. doi: 10.18632/oncotarget.5295. PMID: 26418879; PMCID: PMC4741454.
In vitro protocol:
1. Zhang H, Yao W, Zhang M, Lu Y, Tang J, Jiang M, Mou X, You G, Liang X. TTK inhibitor promotes radiosensitivity of liver cancer cells through p21. Biochem Biophys Res Commun. 2021 Apr 23;550:84-91. doi: 10.1016/j.bbrc.2021.01.089. Epub 2021 Mar 6. Erratum in: Biochem Biophys Res Commun. 2021 May 28;555:214. PMID: 33689884. 2. Liu X, Liao W, Yuan Q, Ou Y, Huang J. TTK activates Akt and promotes proliferation and migration of hepatocellular carcinoma cells. Oncotarget. 2015 Oct 27;6(33):34309-20. doi: 10.18632/oncotarget.5295. PMID: 26418879; PMCID: PMC4741454.
In vivo protocol:
N/A
1: Hewitt L, Tighe A, Santaguida S, White AM, Jones CD, Musacchio A, Green S, Taylor SS. 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. doi: 10.1083/jcb.201002133. PubMed PMID: 20624899; PubMed Central PMCID: PMC2911659.