Vevorisertib (MK-4440, ARQ 751)

Chemical Structure : Vevorisertib

CAS No.: 1416775-46-6

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货号: PC-38375Not For Human Use, Lab Use Only.

Vevorisertib (MK-4440, ARQ 751) is a novel potent, selective, allosteric pan-AKT inhibitor with IC50 of 0.55 nM, 0.81 nM and 1.31 nM for AKT1, 2 and 3, respectively.

规格	价格	库存
5 mg	￥2280	In stock
10 mg	￥3680	In stock
50 mg	￥6580	In stock
100 mg		Get quote

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Vevorisertib (MK-4440, ARQ 751) is a novel potent, selective, allosteric pan-AKT inhibitor with IC50 of 0.55 nM, 0.81 nM and 1.31 nM for AKT1, 2 and 3, respectively.
Vevorisertib (MK-4440, ARQ 751) does not inhibit a panel of 245 kinases by greater than 50% at 5 μM, nor does it inhibit AKT lacking the PH domain.
ARQ 751 strongly binds to wild-type AKT1 and mutant AKT1-E17K with Kd of 1.2 nM and 8.6 nM, respectively, and suppresses pAKT(S473) in 293T cells transiently transfected with AKT1-E17K.
ARQ 751 showed antiproliferative effects (GI50 <1 uM) against a panel of cancer cell lines, including esophageal, breast and head and neck cancer cells.
Cancer cell lines with PIK3CA/PIK3R1 mutations are more sensitive to ARQ 751 (GI50<1μM) compared to wild-type.
ARQ 751 causes significant pathway inhibition in vitro (at the concentrations of 3 nM on pAKT[S473] and 70 nM on pPRAS40 [T246]) and in vivo (on both pAKT[S473] and pPRAS40[T246].
ARQ 751 (75 and 120 mg/kg) inhibits tumor growth in in AN3CA endometrial cancer xenograft model, as well as AKT1-E17K mutant endometrial PDX model.

物理化学性质&存储条件

分子量	586.744
分子式	C35H38N8O
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	N-(1-(3-(3-(4-(1-aminocyclobutyl)phenyl)-2-(2-aminopyridin-3-yl)-3H-imidazo[4,5-b]pyridin-5-yl)phenyl)piperidin-4-yl)-N-methylacetamide

参考文献

1. Kozinova M, et al. Cancers (Basel). 2021 Jul 23;13(15):3699.

2. Yi Yu, et al. Cancer Res (2016) 76 (14_Supplement): 374.