| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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Purity: ≥98%
Miransertib HCl (formerly known as ARQ-092; MK7075), the HCl salt of Miransertib, is a novel, orally bioactive and selective allosteric inhibitor of AKT anticancer activity. With IC50 values of 5.0 nM, 4.5 nM, and 16 nM for AKT1, 2, and 3, respectively, it inhibits AKT. In patients with advanced solid tumors, it shows a tolerable safety profile. The PI3K/AKT signaling pathway may be inhibited as a result of ARQ 092's non-ATP competitive binding to and inhibition of AKT activity. As a result, there may be a decrease in tumor cell proliferation and an increase in tumor cell apoptosis. In addition, ARQ 092 acted as a potent inhibitor of the AKT1-E17K mutant protein and reduced tumor development in a mouse model of human xenograft endometrial adenocarcinoma. Additionally, ARQ 092 may be a promising new treatment for patients with NSML (Noonan Syndrome with Multiple Lentigines) who have hypertrophy.
| Targets |
Leishmania; Akt1 E17K mutant; Akt1 (IC50 = 2.7 nM); Akt3 (IC50 = 8.1 nM); Akt2 (IC50 = 174 nM)
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| ln Vitro |
Miransertib (ARQ-092; Compound 21a) exhibits stronger anti-proliferative activity in cell lines with PIK3CA/PIK3R1 mutations than in cell lines with wild-type (wt) PIK3CA/PIK3R1 or PTEN loss in a large panel of cell lines derived from various tumor types. In both AN3CA and A2780 cells, miransertib exhibits excellent inhibition of p-Akt (S473) and p-Akt (T308). With Miransertib (IC50=0.31 M), the downstream protein p-PRAS40 (T246) is seen to be inhibited[1]. Miransertib is markedly effective against intracellular amastigotes of L. donovani or L. amazonensis-infected macrophages. Additionally, in Leishmania-infected macrophages, miransertib increases mTOR dependent autophagy. [2]
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| ln Vivo |
In rats (5 mg/kg) and monkeys (10 mg/kg), miransertib (ARQ-092; Compound 21a) exhibits good absolute oral bioavailability with F values of 62% and 49%, respectively. Rats' t1/2 values are 17 h compared to monkeys' 7 h, indicating that rats have a longer half-life than monkeys. Rats and monkeys, respectively, had Cmax values of 198 ng/mL and 258 ng/mL, and AUCinf values of 5496 hng/mL and 2960 hng/mL, respectively[1]. Miransertib (ARQ-092; Compound 21a) inhibits tumor growth in a human xenograft mouse model of endometrial adenocarcinoma[1].
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| Cell Assay |
Cells (MDA-MB-453: 1.5 106; NCI-H1650: 1 106; KU-19-19: 0.7 106) are seeded into 6 well plates, incubated for an overnight period, and then exposed to full media containing various concentrations of AKT inhibitors (ARQ 092, ARQ 751, MK-2206, GDC-0068) for 2 hours. Lysates are obtained after treating cells under predetermined conditions. Following SDS-PAGE, immunoblotting is used to separate the proteins from extracts.
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| Animal Protocol |
Male SCD mice
100 mg/10ml/kg oral administration |
| References |
| Molecular Formula |
C27H25CLN6
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|---|---|
| Molecular Weight |
468.99
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| Exact Mass |
468.1829
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| Elemental Analysis |
C, 69.15; H, 5.37; Cl, 7.56; N, 17.92
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| CAS # |
1313883-00-9
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| Related CAS # |
Miransertib;1313881-70-7
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| Appearance |
Solid powder
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| SMILES |
NC1=NC=CC=C1C2=NC3=CC=C(C4=CC=CC=C4)N=C3N2C5=CC=C(C6(N)CCC6)C=C5.[H]Cl
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| InChi Key |
DRHSWSSVIKDJME-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C27H24N6.ClH/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);1H
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| Synonyms |
ARQ092 hydrochloride; MK-7075; ARQ-092 hydrochloride; MK7075; ARQ 092
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (5.33 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 25.0 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.1322 mL | 10.6612 mL | 21.3224 mL | |
| 5 mM | 0.4264 mL | 2.1322 mL | 4.2645 mL | |
| 10 mM | 0.2132 mL | 1.0661 mL | 2.1322 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
| NCT Number | Status | Interventions | Conditions | Sponsor/Collaborators | Start Date | Phases |
| NCT04980872 | Active Recruiting |
Drug: Miransertib | PIK3CA-Related Overgrowth Spectrum (PROS) Proteus Syndrome (PS) |
Merck Sharp & Dohme LLC | November 2, 2021 | Phase 2 |
| NCT01473095 | Completed | Drug: ARQ 092 | Solid Tumor Malignant Lymphoma |
ArQule, Inc. | November 2011 | Phase 1 |
| NCT02594215 | Completed | Drug: MK-7075 (miransertib) | Proteus Syndrome | National Human Genome Research Institute | November 16, 2015 | Phase 1 |
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