AZ3146|cas 1124329-14-1|DC Chemicals

Cas No.:	1124329-14-1
Chemical Name:	9-Cyclopentyl-2-(2-methoxy-4-(1-methylpiperidin-4-yloxy)phenylamino)-7-methyl-7H-purin-8(9H)-one
Synonyms:	8H-Purin-8-one, 9-cyclopentyl-7,9-dihydro-2-[[2-methoxy-4-[(1-methyl-4-piperidinyl)oxy]phenyl]amino]-7-methyl-;AZ 3146;AZ-3146;8H-Purin-8-one, 9-cyclopentyl-7,9-dihydro-2-[[2-methoxy-4-[(1-methyl-4-piperidinyl)oxy]phenyl]...;AZ 3146 (AZ-3146);hesperadine;9-cyclopentyl-2-({2-methoxy-4-[(1-methylpiperidin-4-yl)oxy]-phenyl}amino)-7-methyl-7,9-dihydro-8H-purin-8-one;9-cyclopentyl-2-(2-methoxy-4-(1-methylpiperidin-4-yloxy)phenylamino)-7-methyl-7H-purin-8(9H)-one;CS-0883;9-Cyclopentyl-7,9-dihydro-2-[[2-methoxy-4-[(1-methyl-4-piperidinyl)oxy]phenyl]amino]-7-methyl-8H-purin-8-one;AZ3146;9-Cyclopentyl-2-[[2-methoxy-4-[(1-methylpiperidin-4-yl)oxy]-phenyl]amino]-7-methyl-7,9-dihydro-8H-purin-8-one;AK174927;9-cyclopentyl-2-[2-methoxy-4-(1-methylpiperidin-4-yl)oxyanilino]-7-methylpurin-8-one;9-cyclopentyl-2-({2-methoxy-4-[(1-methyl
SMILES:	O(C1C([H])=C([H])C(=C(C=1[H])OC([H])([H])[H])N([H])C1=NC([H])=C2C(=N1)N(C(N2C([H])([H])[H])=O)C1([H])C([H])([H])C([H])([H])C([H])([H])C1([H])[H])C1([H])C([H])([H])C([H])([H])N(C([H])([H])[H])C([H])([H])C1([H])[H]
Formula:	C₂₄H₃₂N₆O₃
M.Wt:	452.5493
Sotrage:	2 years -20°C Powder, 2 weeks 4°C in DMSO, 6 months -80°C in DMSO

Description:

AZ3146 is a reasonably potent and selective Mps1 inhibitor with IC50 of 35 nM for Mps1Cat.

In Vitro:

In in vitro kinase assays, AZ3146 inhibits human Mps1Cat with IC50 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. IC50s 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 GI50) 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 GI50 of approximately 3 μM (4-fold resistance), while the remaining clones have a GI50 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].

MSDS

COA

LOT NO.	DOWNLOAD

2018-0101
2018-0101

Cat. No.	Product name	Field of application
DC7866	NMS-P715	NMS-P715 is the first selective, ATP-competitive and orally bioavailable MPS1 small-molecule inhibitor(IC50=8 nM); selectively reduces cancer cell proliferation, leaving normal cells almost unaffected.
DC8119	Mps1-IN-2	Mps1-IN-2 is a potent Mps1 kianse inhibitor with IC50 value of 145 nM.
DC7470	MPI-0479605	MPI-0479605 is an ATP competitive and selective inhibitor of mitotic kinase Mps1 with IC50 of 1.8 nM, >40-fold selectivity over other kinases.
DC9679	BAY1217389	BAY1217389 is an orally bioavailable, selective inhibitor of the serine/threonine kinase monopolar spindle 1 (Mps1, TTK), with potential antineoplastic activity.
DC7072	AZ3146	AZ3146 is a potent and selective monopolar spindle 1 (Mps1) kinase inhibitor (IC50 = 35 nM); less potent to FAK, JNK1, JNK2, and Kit.