124033
Akt Inhibitor XVI, AT7867
別名:
Akt Inhibitor XVI, AT7867, p70S6K Inhibitor III, 4-(4-Chlorophenyl)-4-(4-(1H-pyrazol-4-yl)-phenyl)-piperidine, PKA Inhibitor XIV, S6K1 Inhibitor III, Chlorophenyl-pyrazolyl-phenyl-piperidine
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この商品について
実験式（ヒル表記法）:
C20H20ClN3
分子量:
337.85
NACRES:
NA.77
UNSPSC Code:
12352200
Assay:
≥99% (HPLC)
Form:
powder
Storage condition:
OK to freeze, protect from light
assay
≥99% (HPLC)
Quality Segment
form
powder
manufacturer/tradename
Calbiochem®
storage condition
OK to freeze, protect from light
color
white
solubility
DMSO: 100 mg/mL
shipped in
wet ice
storage temp.
2-8°C
General description
A cell-permeable pyrazolo compound that acts as a potent inhibitor against Akt (IC50 = 32, 17, and 47 nM against Akt1, Akt2, and Akt3, respectively), PKA (IC50 = 20 nM), and p70S6K (IC50 = 85 nM) in an ATP-competitive manner (Ki = 18 nM using AKT2), with much reduced activity toward RSK1 (IC50 >100 nM) and a panel of 13 other cellular kinases (IC50 >1 µM), including PDK1, PI 3-Kβ, SGK, GSK-3β, and MEK1. Shown to effectively reduce the phosphorylation levels of GSK-3β, S6R, and FKHRL1 (IC50 range from 2.08 to 4.45 µM against GSK-3β pSer9 level), as well as inhibit the proliferation (IC50 range from 0.94 to 11.86 µM) of cancer cells exhibiting constitutive Akt pathway activation, including the PTEN-deficient MES-SA uterine sarcoma and U87MG glioblastoma cell lines. AT7867 treatments via i.p. or p.o. (20 mg/kg and 90 mg/kg, respectively, once every 3 days) are also reported to result in Akt pathway and tumor growth inhibition in mice bearing MES-SA (~40% of untreated control on day 10 by i.p. or p.o.) or U87MG (~50% of untreated control on day 10 by i.p.) xenograft in vivo.
Packaging
Packaged under inert gas
Preparation Note
Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.
Other Notes
Grimshaw, K.M., et al. 2010. Mol. Cancer Ther.9, 1100.
Saxty, G., et al. 2007. J. Med. Chem.50, 2293.
Saxty, G., et al. 2007. J. Med. Chem.50, 2293.
Legal Information
CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany
Disclaimer
Toxicity: Standard Handling (A)
保管分類
11 - Combustible Solids
wgk
WGK 3
flash_point_f
Not applicable
flash_point_c
Not applicable
適用法令
試験研究用途を考慮した関連法令を主に挙げております。化学物質以外については、一部の情報のみ提供しています。 製品を安全かつ合法的に使用することは、使用者の義務です。最新情報により修正される場合があります。WEBの反映には時間を要することがあるため、適宜SDSをご参照ください。
124033-VMG: + 124033-10MG:
jan
試験成績書（COA）
製品のロット番号・バッチ番号を入力して、試験成績書（COA） を検索できます。ロット番号・バッチ番号は、製品ラベルに「Lot」または「Batch」に続いて記載されています。