AZ3146
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MedKoo CAT#: 406239

CAS#: 1124329-14-1

Description: 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

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AZ3146
CAS# 1124329-14-1

Theoretical Analysis

MedKoo Cat#: 406239
Name: AZ3146
CAS#: 1124329-14-1
Chemical Formula: C24H32N6O3
Exact Mass: 452.25359
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
25.0mg USD 150.0 Same Day
50.0mg USD 250.0 Same Day
100.0mg USD 450.0 Same Day
200.0mg USD 750.0 Same Day
500.0mg USD 1250.0 Same Day
1.0g USD 1950.0 Same Day
2.0g USD 2950.0 Same Day
5.0g USD 4650.0 Same Day
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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

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

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 34.9 77.12
DMF 5.0 11.05
DMF:PBS (pH 7.2) (1:1) 0.5 1.1
Ethanol 42.31 93.49

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

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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.

AZ3146

25.0mg / USD 150.0


Additional Information