Vevorisertib trihydrochloride Biochemical

Vevorisertib trihydrochloride

Cat. Num. AAA227664

• Purity: 98%
• Synonyms: Vevorisertib trihydrochloride; N/A; Vevorisertib trihydrochloride biochemical

• Purity/Purification: 98%

• CAS: 1416775-08-0
• Targets&IC50: Akt3:1.31 nM (IC50), Akt1 E17K:8.6 nM (Kd), Akt2:0.81 nM (IC50), Akt1:0.55 nM (IC50), Akt1:1.2 nM (Kd)
• Solubility: <1mg/ml refers to the product slightly soluble or insoluble
• In vitro: 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 C max plasma concentrations of >=2 uM[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]. Animal Model: Endometrial PDX mouse xenograft models (AKT1-E17K mutation tumor fragments subcutaneously implanted in athymic nude mice; tumor volume of approximately 200 mm 3)[1]. Dosage: 25, 50 and 75 mg/kg. Administration: p.o.; 5 days dosing followed by a 4 day dosing holiday for 20 days. Result: Showed potent tumor growth inhibition of 68, 78 and 98%, respectively. Animal Model: AN3CA mouse xenograft models (female NCr nu/nu mice with 250 mm 3 tumors size)[1]. Dosage: 5, 10, 20, 40, 80, and 120 mg/kg. Administration: p.o.; daily for ten days. Result: Showed tumor growth inhibition of 29, 33, 50, 73, 83, and 92%, respectively.
• Preparation and Storage: Powder: -20 degree C for 3 years; In solvent: -80 degree C for 2 years

Structure

(Ezurpimtrostat, CAS 1914148-72-3)

Structure

(Ezurpimtrostat, CAS 1914148-72-3)

Related Product Information for Vevorisertib trihydrochloride biochemical

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 IC 50 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.

References

1. HALFON PHILIPPE, et al. SUBSTITUTED 2,4 DIAMINO-QUINOLINE AS NEW MEDICAMENT FOR FIBROSIS, AUTOPHAGY AND CATHEPSINS B (CTSB), L (CTSL) AND D (CTSD) RELATED DISEASES. WO2020048694 A1.