Fig. 1 · Structure

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Miransertib hydrochloride

Akt inhibitor

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.

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Biological Activity

Cellular Effect

Cell Line Activity Value Description Reference
A2780 IC50 0.73 μM Antiproliferative activity against human A2780 cells after 72 hrs by MTS/PMS assay [PMID: 27305487]
AN3-CA IC50 0.71 μM Antiproliferative activity against human AN3CA cells after 72 hrs by MTS/PMS assay [PMID: 27305487]
IGROV-1 IC50 0.21 μM Antiproliferative activity against human IGROV1 cells after 72 hrs by MTS/PMS assay [PMID: 27305487]
LNCaP IC50 0.9 μM Antiproliferative activity against human LNCAP cells after 72 hrs by MTS/PMS assay [PMID: 27305487]
Sf9 IC50 0.0027 μM Inhibition of full length unphosphorylated AKT1 (1 to 480 residues) (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotin-GRPRTSSFAEG as substrate preincubated for 20 mins followed by substrate addition measured after 30 mins by [PMID: 27305487]
Sf9 IC50 0.0045 μM Inhibition of full length active AKT2 (1 to 481 residues) (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotin-GRPRTSSFAEG as substrate preincubated for 20 mins followed by substrate/PDK1/MAPKAPK2/DOPS/DOPC/PtdIns(3,4,5)P3 addi [PMID: 27305487]
Sf9 IC50 0.005 μM Inhibition of full length active AKT1 (1 to 480 residues) (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotin-GRPRTSSFAEG as substrate preincubated for 20 mins followed by substrate/PDK1/MAPKAPK2/DOPS/DOPC/PtdIns(3,4,5)P3 addi [PMID: 27305487]
Sf9 IC50 0.0081 μM Inhibition of full length unphosphorylated AKT3 (1 to 479 residues) (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotin-GRPRTSSFAEG as substrate preincubated for 20 mins followed by substrate addition measured after 30 mins by [PMID: 27305487]
Sf9 IC50 0.014 μM Inhibition of full length unphosphorylated AKT2 (1 to 481 residues) (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotin-GRPRTSSFAEG as substrate preincubated for 20 mins followed by substrate addition measured after 30 mins by [PMID: 27305487]
Sf9 IC50 0.016 μM Inhibition of full length active AKT3 (1 to 479 residues) (unknown origin) expressed in baculovirus infected Sf9 insect cells using biotin-GRPRTSSFAEG as substrate preincubated for 20 mins followed by substrate/PDK1/MAPKAPK2/DOPS/DOPC/PtdIns(3,4,5)P3 addi [PMID: 27305487]

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Specifications

Manufacturer Adooq Bioscience
Actions Inhibitor
CAS Number 1313883-00-9
Applications Akt inhibitor
Formula C27H25ClN6
Molecular Weight 468.98
Synonyms ARQ-092 hydrochloride; ARQ092
SMILES
NC1=NC=CC=C1C2=NC3=CC=C(C4=CC=CC=C4)N=C3N2C5=CC=C(C6(N)CCC6)C=C5.[H]Cl

Storage & Solubility

In Vitro Solubility

Reported Solubility

No reported solubility data are available for this product.

Preparing Stock Solutions

Stock preparation is unavailable for this product molecular weight.

Calculated stock concentrations do not establish solvent solubility. Refer to the reported solubility data for experimental guidance.

Storage

Store powder at -20°C, keep desiccated.
In powder form, the chemical is stable for 36 months.
In solution, store at -20°C and use within 1 month to prevent loss of potency. Aliquot to avoid multiple freeze/thaw cycles.

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