ChemicalBook >> CAS DataBase List >>Acetamide, N-[1-[3-[3-[4-(1-aminocyclobutyl)phenyl]-2-(2-amino-3-pyridinyl)-3H-imidazo[4,5-b]pyridin-5-yl]phenyl]-4-piperidinyl]-N-methyl-, hydrochloride (1:3)

Acetamide, N-[1-[3-[3-[4-(1-aminocyclobutyl)phenyl]-2-(2-amino-3-pyridinyl)-3H-imidazo[4,5-b]pyridin-5-yl]phenyl]-4-piperidinyl]-N-methyl-, hydrochloride (1:3)

Acetamide, N-[1-[3-[3-[4-(1-aminocyclobutyl)phenyl]-2-(2-amino-3-pyridinyl)-3H-imidazo[4,5-b]pyridin-5-yl]phenyl]-4-piperidinyl]-N-methyl-, hydrochloride (1:3) structure

CAS No.: 1416775-08-0

Chemical Name:: Acetamide, N-[1-[3-[3-[4-(1-aminocyclobutyl)phenyl]-2-(2-amino-3-pyridinyl)-3H-imidazo[4,5-b]pyridin-5-yl]phenyl]-4-piperidinyl]-N-methyl-, hydrochloride (1:3)

Synonyms: ARQ 751 trihydrochloride;Vevorisertib trihydrochloride;Acetamide, N-[1-[3-[3-[4-(1-aminocyclobutyl)phenyl]-2-(2-amino-3-pyridinyl)-3H-imidazo[4,5-b]pyridin-5-yl]phenyl]-4-piperidinyl]-N-methyl-, hydrochloride (1:3)

CBNumber:: CB311009994

Molecular Formula:: C35H39ClN8O

Molecular Weight:: 623.2

MDL Number:

MOL File:: 1416775-08-0.mol

Last updated:2024-07-02 08:55:04

Request For Quotation

Acetamide, N-[1-[3-[3-[4-(1-aminocyclobutyl)phenyl]-2-(2-amino-3-pyridinyl)-3H-imidazo[4,5-b]pyridin-5-yl]phenyl]-4-piperidinyl]-N-methyl-, hydrochloride (1:3) Properties

storage temp.	4°C, away from moisture
solubility	DMSO : 150 mg/mL (215.48 mM; Need ultrasonic)
form	Solid
color	White to yellow

Acetamide, N-[1-[3-[3-[4-(1-aminocyclobutyl)phenyl]-2-(2-amino-3-pyridinyl)-3H-imidazo[4,5-b]pyridin-5-yl]phenyl]-4-piperidinyl]-N-methyl-, hydrochloride (1:3) Chemical Properties,Uses,Production

Biological Activity

Vevorisertib (ARQ 751) trihydrochloride is a selective, allosteric, pan-AKT and AKT1-E17K mutant inhibitors. Vevorisertib trihydrochloride potently inhibit phosphorylation of AKT. Vevorisertib trihydrochloride has Kd values of 1.2 nM and 8.6 nM for AKT1 and AKT1-E17K, respectively. Vevorisertib trihydrochloride has IC50 values of 0.55, 0.81, and 1.3 nM for AKT1, AKT2, and AKT3, respectively. Vevorisertib trihydrochloride can be used for the research of cancer[1]. Vevorisertib trihydrochloride (0, 12, 33, 111, 333, 1000 nM, 2 hours) inhibits phosphorylation of AKT1-E17K[1].Vevorisertib trihydrochloride (1 μM for 2 hours; NIH 3T3 cells are transfected with either pcDNAAKT-WT-GFP or pcDNA-E17K-GFP) inhibits plasma membrane translocation of AKT-WT and AKT1-E17K irrespective of the presence of growth factors[1].Vevorisertib trihydrochloride (5 μM) exhibites 57% inhibition of full-length AKT1[1].Vevorisertib trihydrochloride (0, 0.012, 0.037, 0.11, 0.33, 1 μM; 2 hours) shows a dose-dependent effect on mTORC1 and AKT direct substrates including PRAS40, GSK3β, FOXO, BAD, and AS160 in cancer cell lines[1].Vevorisertib trihydrochloride has anti-proliferative effect on esophageal, breast, and head and neck cancer cells (GI50 < 1 μM)[1].Vevorisertib trihydrochloride exhibits strong anti-proliferative activity in PIK3CA mutant cell lines[1].Vevorisertib trihydrochloride (MK-4440)/imatinib mesylate (IM) combination shows cell cycle arrest, and increases cell death of gastrointestinal stromal tumor (GIST) cells[2].Vevorisertib trihydrochloride exhibits strong anti-proliferative activity in PIK3CA mutant cell lines[1]: Breast Cancer Cell Lines GI50 (nM) PIK3CA ER PR HER2 T47D 1.05 H1047R + + - EFM-19 1.54 H1047R + + - MCF-7 2.20 E545K + + - BT474 3.25 K111N + + + MDA-MB-453 6.05 H1047R - - + Vevorisertib trihydrochloride (25, 50 and 75 mg/kg; p.o.; 5 days dosing followed by a 4 day dosing holiday for 20 days) shows potent tumor growth inhibition of 68, 78 and 98%, respectively[1].Vevorisertib trihydrochloride (5, 10, 20, 40, 80, and 120 mg/kg; p.o. daily for ten days) shows tumor growth inhibition of 29, 33, 50, 73, 83, and 92%, respectively[1].Vevorisertib trihydrochloride reachs Cmax plasma concentrations of ≥2 μM[1].Vevorisertib trihydrochloride is generally well-tolerated at dose levels up to 120 mg/kg[1].Vevorisertib trihydrochloride (MK-4440)/IM combination shows superior efficacy in an IM-sensitive preclinical model of GIST compared with either single agent[2].

References

[1]. Yu Y, et al. Targeting AKT1-E17K and the PI3K/AKT Pathway with an Allosteric AKT Inhibitor, ARQ 092. PLoS One. 2015 Oct 15;10(10):e0140479. [2]. Kozinova M, et al. Combined Inhibition of AKT and KIT Restores Expression of Programmed Cell Death 4 (PDCD4) in Gastrointestinal Stromal Tumor. Cancers (Basel). 2021 Jul 23;13(15):3699.

Acetamide, N-[1-[3-[3-[4-(1-aminocyclobutyl)phenyl]-2-(2-amino-3-pyridinyl)-3H-imidazo[4,5-b]pyridin-5-yl]phenyl]-4-piperidinyl]-N-methyl-, hydrochloride (1:3) Preparation Products And Raw materials

Raw materials

Preparation Products

Acetamide, N-[1-[3-[3-[4-(1-aminocyclobutyl)phenyl]-2-(2-amino-3-pyridinyl)-3H-imidazo[4,5-b]pyridin-5-yl]phenyl]-4-piperidinyl]-N-methyl-, hydrochloride (1:3) Suppliers

Global( 6)Suppliers

Supplier	Tel	Email	Country	ProdList	Advantage
ShangHai ChuanQian Chemcial Technique Centre	15869524721	3525679403@qq.com	China	3721	58
Chengdu PEIP Pharmaceutical Technology Co., LTD.	028-61715638 18011352545	1242335275@qq.com	China	411	58
Shanghai Tachizaki Biomedical Research Center	18014399201	sales@chemlab-tachizaki.com	China	2539	58
Nantong QuanYi Biotechnology Co., Ltd	0513-66337626 18051384581	sales@chemhifuture.com	China	4551	58
Shanghai?Medlife?Pharm-Tech?Co.,?Ltd	021-59167510 18117107507	vip@med-life.cn	China	5012	58
TargetMol Chemicals Inc.	15002134094	marketing@targetmol.cn	China	28091	58

Supplier	Advantage
ShangHai ChuanQian Chemcial Technique Centre	58
Chengdu PEIP Pharmaceutical Technology Co., LTD.	58
Shanghai Tachizaki Biomedical Research Center	58
Nantong QuanYi Biotechnology Co., Ltd	58
Shanghai?Medlife?Pharm-Tech?Co.,?Ltd	58
TargetMol Chemicals Inc.	58

Acetamide, N-[1-[3-[3-[4-(1-aminocyclobutyl)phenyl]-2-(2-amino-3-pyridinyl)-3H-imidazo[4,5-b]pyridin-5-yl]phenyl]-4-piperidinyl]-N-methyl-, hydrochloride (1:3) Vevorisertib trihydrochloride ARQ 751 trihydrochloride 1416775-08-0