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Chemical Structure : Miransertib free base
CAS No.: 1313881-70-7
Catalog No.: PC-73209Not For Human Use, Lab Use Only.
Miransertib free base (ARQ-092, MK-7075) is a potent, selective and allosteric pan-Akt inhibitor with IC50 of 2.7 nM, 14 nM and 8.1 nM for Akt1, Akt2, Akt3, respectively.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 10 mg | $148 | In stock | |
| 25 mg | $258 | In stock | |
| 50 mg | $458 | In stock | |
| 100 mg | $758 | In stock | |
| 1 g | Get quote |
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Miransertib free base (ARQ-092, MK-7075) is a potent, selective and allosteric pan-Akt inhibitor with IC50 of 2.7 nM, 14 nM and 8.1 nM for Akt1, Akt2, Akt3, respectively.
Miransertib (ARQ-092) also potently inhibits AKT1-E17K mutant inhibitor and phosphorylation of AKT.
Miransertib (ARQ-092) inhibited AKT activation not only by dephosphorylating the membrane-associated active form, but also by preventing the inactive form from localizing into plasma membrane.
Miransertib (ARQ-092) exhibited strong anti-tumor activity in endometrial PDX models harboring mutant AKT1-E17K and other tumor models.
ARQ 092 enhanced tumor inhibition of a common chemotherapeutic agent (paclitaxel).
Miransertib (ARQ-092) inhibited proliferation across multiple tumor types but is most potent in leukemia, breast, endometrial, and colorectal cancer cell lines.
Miransertib (ARQ-092) was more prevalent in cancer cell lines containing PIK3CA/PIK3R1 mutations compared to those with wt-PIK3CA/PIK3R1 or PTEN mutations.
| M.Wt | 432.531 | |
| Formula | C27H24N6 | |
| Appearance | Solid | |
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| Solubility |
10 mM in DMSO |
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1. Yu Y, et al. PLoS One. 2015 Oct 15;10(10):e0140479.
2. Lapierre JM, et al. J Med Chem. 2016 Jul 14;59(13):6455-69.
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