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Chemical Structure : Vevorisertib
CAS No.: 1416775-46-6
Catalog No.: 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 5 mg | $228 | In stock | |
| 10 mg | $368 | In stock | |
| 50 mg | $658 | 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.
| M.Wt | 586.744 | |
| Formula | C35H38N8O | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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 |
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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.
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