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Akt &GSK-3

Miransertib (ARQ 092) (1313881-70-7)

Miransertib, also known as ARQ 092, is an oral activie, potent and selective AKT inhibitor with IC50 values: 5.0 nM (AKT1); 4.5 nM (AKT2); 16 nM (AKT3). ARQ 092 binds to and inhibits the activity of AKT in a non-ATP competitive manner,

Not Intended for Therapeutic Use. For research use only.

CAS: 1313881-70-7 Category

Miransertib (ARQ 092) (1313881-70-7) Description:

Miransertib, also known as ARQ 092, is an oral activie, potent and selective AKT inhibitor with IC50 values: 5.0 nM (AKT1); 4.5 nM (AKT2); 16 nM (AKT3). ARQ 092 binds to and inhibits the activity of AKT in a non-ATP competitive manner, which may result in the inhibition of the PI3K/AKT signaling pathway. This may lead to the reduction in tumor cell proliferation and the induction of tumor cell apoptosis. ARQ-092 demonstrated high enzymatic potency against AKT1, AKT2, and AKT3, as well as potent cellular inhibition of AKT activation and the phosphorylation of the downstream target PRAS40. ARQ-092 also served as a potent inhibitor of the AKT1-E17K mutant protein and inhibited tumor growth in a human xenograft mouse model of endometrial adenocarcinoma.

Miransertib (ARQ 092) (1313881-70-7) Specifications:

Product Name Miransertib(ARQ 092)
Synonym ARQ092; ARQ-092; ARQ 092; Miransertib
Chemical Name 3-(3-(4-(1-aminocyclobutyl)phenyl)-5-phenyl-3H-imidazo[4,5-b]pyridin-2-yl)pyridin-2-amine
Drug Class Antineoplastics
Purity ≥98% (HPLC)
CAS Number 1313881-70-7
Molecular Formula C27H24N6
Molecular Weight 432.531
Monoisotopic Mass 432.2062 g/mol
MDL number N/A
InChIKey HNFMVVHMKGFCMB-UHFFFAOYSA-N
InChi Code InChI=1S/C27H24N6/c28-24-21(8-4-17-30-24)25-32-23-14-13-22(18-6-2-1-3-7-18)31-26(23)33(25)20-11-9-19(10-12-20)27(29)15-5-16-27/h1-4,6-14,17H,5,15-16,29H2,(H2,28,30)
SMILES NC1=NC=CC=C1C2=NC3=CC=C(C4=CC=CC=C4)N=C3N2C5=CC=C(C6(N)CCC6)C=C5
Form Powder
Color White
Solubility  Soluble in DMSO, not soluble in water
Storage Temp.  0 – 4 C for short term (days to weeks), or -20 C for long term (months)
Shelf life >2 years if stored properly
Handling Protect from air and moisture
Application Miransertib is an oral activie, potent and selective AKT inhibitor

 


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RIDADR NONH for all modes of transport

References:

[1]. Lindhurst MJ, Yourick MR, Yu Y, Savage RE, Ferrari D, Biesecker LG. Repression of AKT signaling by ARQ 092 in cells and tissues from patients with Proteus syndrome. Sci Rep. 2015 Dec 11;5:17162. doi: 10.1038/srep17162. PubMed PMID: 26657992; PubMed Central PMCID: PMC4675973.

[2]. Yu Y, Savage RE, Eathiraj S, Meade J, Wick MJ, Hall T, Abbadessa G, Schwartz Targeting AKT1-E17K and the PI3K/AKT Pathway with an Allosteric AKT Inhibitor, ARQ 092. PLoS One. 2015 Oct 15;10(10):e0140479. doi: 10.1371/journal.pone.0140479. eCollection 2015. PubMed PMID: 26469692; PubMed Central PMCID: PMC4607407.

[3]. Miransertib (ARQ 092), an orally-available, selective Akt inhibitor is effective against Leishmania. Nandan D, Zhang N, Yu Y, Schwartz B, Chen S, Kima PE, Reiner NE. PLoS One. 2018 Nov 6;13(11):e0206920. doi: 10.1371/journal.pone.0206920. eCollection 2018. PMID: 30399177

[4]. Combination of AKT inhibitor ARQ 092 and sorafenib potentiates inhibition of tumor progression in cirrhotic rat model of hepatocellular carcinoma. Jilkova ZM, Kuyucu AZ, Kurma K, Ahmad Pour ST, Roth GS, Abbadessa G, Yu Y, Schwartz B, Sturm N, Marche PN, Hainaut P, Decaens T. Oncotarget. 2018 Jan 23;9(13):11145-11158. doi: 10.18632/oncotarget.24298. eCollection 2018 Feb 16. PMID: 29541403

[5]. Miransertib (ARQ 092), an orally-available, selective Akt inhibitor is effective against Leishmania. Nandan D, Zhang N, Yu Y, Schwartz B, Chen S, Kima PE, Reiner NE. PLoS One. 2018 Nov 6;13(11):e0206920. doi: 10.1371/journal.pone.0206920. eCollection 2018. PMID: 30399177

1 review for Miransertib (ARQ 092) (1313881-70-7)

  1. Cofttek

    Never had such good experience before,The Miransertib (ARQ 092) (1313881-70-7) is high purity,also customer service is pretty nice !gotta try!!

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