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AT13148

CAS No. : 1056901-62-2

MCE 站：AT13148

产品活性：AT13148 是一种可口服的，ATP 竞争性的 AGC kinase 的抑制剂，能够抑制 Akt1/Akt2/Akt3，p70S6K，PKA 和 ROCKI/ROCKII 的活性，IC₅₀ 值分别为 38 nM/402 nM/50 nM，8 nM，3 nM 和 6 nM/4 nM。

研究领域：PI3K/Akt/mTOR  |  Stem Cell/Wnt  |  Protein Tyrosine Kinase/RTK  |  TGF-beta/Smad  |  Cytoskeleton  |  Cell Cycle/DNA Damage  |  MAPK/ERK Pathway

作用靶点：Akt  |  PKA  |  ROCK  |  Ribosomal S6 Kinase (RSK)

In Vitro: AT13148 inhibits a panel of kinases at 10 μM, and the IC₅₀ values for p70S6K, PKA, ROCKI, and ROCKII are all less than 10 nM and those for AKT1, 2, and 3 are 38, 402, and 50 nM, respectively. For the related AGC kinases RSK1 and SGK3, the IC₅₀ values are 85 and 63 nM, respectively. In contrast, IC₅₀ values for the non-AGC kinases CHK2 and Aurora B are both greater than 800 nM. AT13148 potently inhibits proliferation with GI₅₀ values of 1.5 to 3.8 μM across a selected panel of cancer cell lines. AT13148 treatment in gastric cancer cells dramatically suppresses activation of multiple AGC kinases, including Akt (at p-Thr-308), p70S6 kinase (p70S6K), glycogen synthase kinase 3β (GSK-3β) and p90 ribosomal S6 kinase (RSK).

In Vivo: Oral drug administration of 5 mg/kg of AT13148 results in complete bioavailability. Clear inhibition of phosphorylation of the AKT substrates GSK3β, tuberin, and the p70S6K target S6RP are also observed in PTEN-deficient MES-SA human uterine tumor xenografts after treatment with 40 and 50 mg/kg p.o. of AT13148. Oral gavage of AT13148 at well-tolerated doses significantly inhibits HGC27 xenograft tumor growth in nude mice. AGC activity is also dramatically decreased in AT13148-administrated HGC27 tumors.

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