Vevorisertib trihydrochloride,

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Vevorisertib trihydrochloride

CAS No. : 1416775-08-0

MCE 国际站：Vevorisertib trihydrochloride

产品活性：Vevorisertib (ARQ 751) trihydrochloride 是选择性、变构、pan-AKT 和 AKT1-E17K 突变抑制剂，可有效抑制 AKT 的磷酸化。Vevorisertib trihydrochloride 对 AKT1 和 AKT1-E17K 的 Kd 值分别为 1.2 nM 和 8.6 nM。Vevorisertib trihydrochloride 对 AKT1、AKT2 和 AKT3 的 IC₅₀ 值分别为 0.55、0.81 和 1.3 nM。 Vevorisertib trihydrochloride 可用于癌症的研究。

研究领域：PI3K/Akt/mTOR

作用靶点：Akt

In Vitro: Vevorisertib trihydrochloride (0, 12, 33, 111, 333, 1000 nM, 2 hours) inhibits phosphorylation of AKT1-E17K.
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.
Vevorisertib trihydrochloride (5 μM) exhibites 57% inhibition of full-length AKT1.
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.
Vevorisertib trihydrochloride has anti-proliferative effect on esophageal, breast, and head and neck cancer cells (GI₅₀ < 1 μM).
Vevorisertib trihydrochloride exhibits strong anti-proliferative activity in PIK3CA mutant cell lines.
Vevorisertib trihydrochloride (MK-4440)/imatinib mesylate (IM) combination shows cell cycle arrest, and increases cell death of gastrointestinal stromal tumor (GIST) cells.
Vevorisertib trihydrochloride exhibits strong anti-proliferative activity in PIK3CA mutant cell lines:

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	-	-	+

In Vivo: 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.
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.
Vevorisertib trihydrochloride reachs C_max plasma concentrations of ≥2 μM.
Vevorisertib trihydrochloride is generally well-tolerated at dose levels up to 120 mg/kg.
Vevorisertib trihydrochloride (MK-4440)/IM combination shows superior efficacy in an IM-sensitive preclinical model of GIST compared with either single agent.

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