Miransertib hydrochloride

SKU: orb1704860

Description

Miransertib hydrochloride is an orally bioavailable, allosteric pan-Akt inhibitor targeting AKT1/2/3. It is used in research for PI3K/Akt pathway-related cancers, leishmaniasis, and Proteus syndrome, with studies demonstrating its efficacy in both cellular and animal models.

Research Area

Infectious Disease & Virology, Signal Transduction

Key Properties

• CAS Number: 1313883-00-9
• MW: 468.98
• Purity: 99.81% (May vary between batches)
• Formula: C₂₇H₂₅ClN₆
• SMILES: Cl.Nc1ncccc1-c1nc2ccc(nc2n1-c1ccc(cc1)C1(N)CCC1)-c1ccccc1
• Target: Parasite,Akt
• Solubility: DMSO:40 mg/mL (85.29 mM);10% DMSO+90% Saline:2 mg/mL (4.26 mM)

Bioactivity

• Target IC50:
  Akt2:174 nM|Akt1:2.7 nM|Akt3:8.1 nM
• In Vivo:
  Miransertib (ARQ-092; Compound 21a) demonstrates effective oral bioavailability in rats (62%, 5 mg/kg) and monkeys (49%, 10 mg/kg), with half-lives of 17 hours and 7 hours, respectively. Peak plasma concentrations are 198 ng/mL in rats and 258 ng/mL in monkeys, with AUC values of 5496 h·ng/mL and 2960 h·ng/mL, respectively. Additionally, Miransertib effectively inhibits tumor growth in a human xenograft mouse model of endometrial adenocarcinoma .
• In Vitro:
  In a comprehensive study involving various tumor-derived cell lines, Miransertib (ARQ-092; Compound 21a) demonstrated significant anti-proliferative effects in cell lines harboring mutations in PIK3CA/PIK3R1 compared to those with the wild-type (wt) PIK3CA/PIK3R1 or PTEN deficiency. Additionally, Miransertib effectively inhibited p-Akt (S473) and p-Akt (T308) in AN3CA and A2780 cells and suppressed p-PRAS40 (T246) with an IC 50 of 0.31 μM. Notably, Miransertib was highly effective against intracellular amastigotes of L. donovani or L. amazonensis in infected macrophages and promoted mTOR-dependent autophagy in Leishmania-infected macrophages, highlighting its diverse therapeutic potential.

Storage & Handling

• Storage: store at low temperature | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

Miransertib (ARQ 092) HCl, ARQ-092 hydrochloride

Compound Identifiers

PubChem CID

67305743