ChemicalBook > CAS DataBase List > ARQ 092

ARQ 092

Product Name: ARQ 092
CAS No.: 1313883-00-9
Chemical Name: ARQ 092
Synonyms: MK-7075);ARQ092 HCl;Miransertib HCl;ARQ092 Hydrochloride;Miransertib HCl (ARQ 092);Miransertib (ARQ 092) HCl;Miransertib hydrochloride;Miransertib (ARQ 092) HCl ，S8339;3-(3-(4-(1-Aminocyclobutyl)phenyl)-5-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine hydrochloride
CBNumber: CB83373055
Molecular Formula: C27H25ClN6
Formula Weight: 468.99
MOL File: 1313883-00-9.mol

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ARQ 092 Property

storage temp.: Store at -20°C
solubility: DMSO: 75 mg/mL (159.92 mM);Ethanol: 4 mg/mL (8.53 mM)
form: Solid
color: Light yellow to brown
Water Solubility: Water: Insoluble

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Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Warning

Hazard statements

H302Harmful if swallowed

H315Causes skin irritation

H319Causes serious eye irritation

H335May cause respiratory irritation

Precautionary statements

P261Avoid breathing dust/fume/gas/mist/vapours/spray.

P305+P351+P338IF IN EYES: Rinse cautiously with water for several minutes. Remove contact lenses, if present and easy to do. Continuerinsing.

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N-Bromosuccinimide Price

Ambeed

Product number: A803512
Product name: ARQ092
Purity: 98+%
Packaging: 1mg
Price: $39
Updated: 2021/12/16

Ambeed

Product number: A803512
Product name: ARQ092
Purity: 98+%
Packaging: 5mg
Price: $77
Updated: 2021/12/16

Ambeed

Product number: A803512
Product name: ARQ092
Purity: 98+%
Packaging: 10mg
Price: $131
Updated: 2021/12/16

Ambeed

Product number: A803512
Product name: ARQ092
Purity: 98+%
Packaging: 25mg
Price: $208
Updated: 2021/12/16

Ambeed

Product number: A803512
Product name: ARQ092
Purity: 98+%
Packaging: 50mg
Price: $270
Updated: 2021/12/16

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ARQ 092 Chemical Properties,Usage,Production

Uses

Miransertib hydrochloride (ARQ-092 hydrochloride) is a potent, orally active, selective and allosteric Akt inhibitor with IC50s of 2.7 nM, 14 nM and 8.1 nM for Akt1, Akt2, Akt3, respectively. Miransertib hydrochloride is also a potent the AKT1-E17K mutant protein inhibitor and has the potential for PI3K/AKT-driven tumors and Proteus syndrome research[1]. Miransertib hydrochloride is effective against Leishmania[2].

Synthesis

1313881-69-4

1313883-00-9

Step 4: Tert-butyl (1 -(4-(2-(2-(2-aminopyridin-3-yl)-5-phenyl-3H-imidazo[4,5-b]pyridin-3-yl)phenyl)cyclobutyl)carbamate (4.1 g) was dissolved in dichloromethane (100 mL), and a dioxane solution (20 mL) of 4.0 M HCl was slowly added. The reaction mixture was stirred at room temperature for 2.5 hours. After completion of the reaction, ether (50 mL) was added to the suspension and the solid was collected by filtration to afford 3-(3-(4-(1-aminocyclobutyl)phenyl)-5-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine hydrochloride (4.032 g, white solid). The product was characterized by 1H NMR (DMSO-d6, 400 MHz) and LCMS: 1H NMR δ 8.94 (s, 3H), 8.47 (bs, 1H), 8.38 (d, J = 8.8 Hz, 1H), 8.19-8.15 (m, 1H), 8.10-8.03 (m, 3H), 7.93-7.88 (m, 1H), 7.76 (d, J = 8.4 Hz, 1H), 7.69 (d, J = 8.4 Hz, 2H), 7.52-7.40 (m, 3H), 6.92 (t, J = 7.6 Hz, 1H), 2.70-2.57 (m, 4H), 2.29-2.20 (m, 1H), 1.90-1.80 (m, 1H); LCMS: m/z 433 [M + H]+. Calculated elemental analysis (C29H27ON7-3.06HCl-0.01C4H8O2-0.03C4H10O): C 59.61, H 5.28, N 15.36; measured values: C 59.62, H 5.05, N 15.36.

in vivo

Miransertib (ARQ-092; Compound 21a) shows good absolute oral bioavailability in rats (5 mg/kg) and monkeys (10 mg/kg) with F values of 62% and 49%, respectively. The half-life is longer in rats compared to monkeys with t_1/2 values of 17 h in rats versus 7 h in monkeys. The C_max is 198 ng/mL and 258 ng/mL and the AUC_inf was 5496 h?ng/mL and 2960 h?ng/mL in rats and monkeys, respectively^[1].
Miransertib (ARQ-092; Compound 21a) inhibits tumor growth in a human xenograft mouse model of endometrial adenocarcinoma^[1].

IC 50

Akt1: 2.7 nM (IC₅₀); Leishmania; Akt3: 8.1 nM (IC₅₀); Akt2: 174 nM (IC₅₀); Akt1 E17K mutant

References

[1] Lapierre JM, et al. Discovery of 3-(3-(4-(1-Aminocyclobutyl)phenyl)-5-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine (ARQ 092): An Orally Bioavailable, Selective, and Potent Allosteric AKT Inhibitor. J Med Chem. 2016 Jul 14;59(13):6455-69. DOI:10.1021/acs.jmedchem.6b00619
[2] Devki Nandan, et al. Miransertib (ARQ 092), an orally-available, selective Akt inhibitor is effective against Leishmania. PLoS One. 2018 Nov 6;13(11):e0206920. DOI:10.1371/journal.pone.0206920

ARQ 092 Preparation Products And Raw materials

Raw materials

Preparation Products

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1313883-00-9, ARQ 092Related Search:

Pyridine hydrochloride Trimethylamine hydrochloride Betaine hydrochloride Methylamine hydrochloride

ARQ092 HCl

Miransertib (ARQ 092) HCl

ARQ092 Hydrochloride

Miransertib HCl

Miransertib HCl (ARQ 092)

3-(3-(4-(1-Aminocyclobutyl)phenyl)-5-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine hydrochloride

MK-7075)

Miransertib hydrochloride

Miransertib (ARQ 092) HCl ，S8339

1313883-00-9