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PF-AKT400

(Synonyms: AKT protein kinase inhibitor)

目录号: PL01596 纯度: ≥98%

PF-AKT400 是一种有效的, ATP 竞争性的选择性 Akt 抑制剂，对 PKBα (IC50=0.5 nM) 的选择性比 PKA (IC50=450 nM) 高 900 倍。

CAS No. :1004990-28-6

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中文名称	PF-AKT400
中文别名	(S)-N-[[3-氨基-1-(5-乙基-7H-吡咯并[2,3-d]嘧啶-4-基)吡咯烷-3-基]甲基]-2,4-二氟苯甲酰胺
英文名称	PF-AKT400
英文别名	16-(3-Chlorophenoxy)-17,18,19,20-tetranorprostaglandin F2alpha;(S)-N-[[3-Amino-1-(5-ethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrrolidin-3-yl]methyl]-2,4-difluorobenzamide;(S)-N-[[3-Amino-1-(5-ethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)pyrrolidin-3-yl]methyl]-2,4-difluorobenza;AKT protein kinase inhibitor;N-{[(3S)-3-Amino-1-(5-ethyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-3-py rrolidinyl]methyl}-2,4-difluorobenzamide;AKT INHIBITOR;1L-6-HYDROXYMETHYL-CHIRO-INOSITOL 2-(R)-2-O-METHYL-3-O-OCTADECYLCARBONATE;PF-AKT400;N-[[(3S)-3-AMINO-1-(5-ETHYL-7H-PYRROLO[2,3-D]PYRIMIDIN-4-YL)-3-PYRROLIDINYL]METHYL]-2,4-DIFLUORO-BENZAMIDE;BenzaMide, N-[[(3S)-3-aMino-1-(5-ethyl-7H-pyrrolo[2,3-d]pyriMidin-4-yl)-3-pyrrolidinyl]Methyl]-2,4-difluoro-
Cas No.	1004990-28-6
分子式	C₂₀H₂₂N₆OF₂
分子量	400.43
包装储存	Powder -20°C 3 years；4°C 2 years
详情描述	PF-AKT400 是一种有效的, ATP 竞争性的选择性 Akt 抑制剂，对 PKBα (IC50=0.5 nM) 的选择性比 PKA (IC50=450 nM) 高 900 倍。

产品详情	PF-AKT400 是一种有效的, ATP 竞争性的选择性 Akt 抑制剂，对 PKBα (IC₅₀=0.5 nM) 的选择性比 PKA (IC₅₀=450 nM) 高 900 倍。
生物活性	PF-AKT400 is a broadly selective, potent, ATP-competitive Akt inhibitor, displays 900-fold greater selectivity for PKBα (IC 50 =0.5 nM) than PKA (IC 50 =450 nM).
性状	Solid
IC50 & Target[1][2]	PKBα 0.5 nM (IC50) PKA 450 nM (IC50
体外研究(In Vitro)	PF-AKT400 (Compound 42) provides significantly enhanced selectivity for Akt relative to earlier leads such as spiroindoline 2. Free IC50 and EC50 values are estimated for phospho-S6 reduction (110 nM) and Akt hyperphosphorylation (216 nM), respectively. These values corresponded well to the cellular IC50 for PF-AKT400 in U87 cells measuring p-GSK-3α (310 nM). has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)	PF-AKT400 is subsequently evaluated for modulation of Akt in tumors and in multiple in vivo mouse models of antitumor efficacy. It is active in a PC3 prostate carcinoma xenograft experiment, with 75% TGI observed at 100 mg/kg b.i.d. dosing for 10 days. In a colorectal carcinoma (Colo205) xenograft study, PF-AKT400 produces 60% TGI at 150 mg/kg b.i.d. after 10 days. Most intriguingly, in combination with Rapamycin (10 mg/kg, ip), 75 mg/kg b.i.d. (10 days) of PF-AKT400 results in 98% TGI in an additional PC3 prostate carcinoma xenograft study compared to 56% TGI and 66% TGI with PF-AKT400 and Rapamycin as single agents. To define the in vivo potency of PF-AKT400 (Compound 42) in the PC3 xenograft model, oral administration of 25, 75, and 100 mg/kg PF-AKT400 is performed with blood and tumor sampling over time. Immunoblot analysis of detergent-soluble extracts derived from PC3 tu
运输条件	Room temperature in continental US; may vary elsewhere.
储存方式	Powder -20°C 3 years；4°C 2 years
参考文献	[1]. Chen SF, et al. Binding selectivity studies of PKBα using molecular dynamics simulation and free energy calculations. J Mol Model. 2013 Nov;19(11):5097-5112. [2]. Freeman-Cook KD, et al. Design of selective, ATP-competitive inhibitors of Akt. J Med Chem. 2010 Jun 24;53(12):4615-4622.

溶解度数据	In Vitro: DMSO : ≥ 100 mg/mL (249.73 mM)配制储备液

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[1]. Chen SF, et al. Binding selectivity studies of PKBα using molecular dynamics simulation and free energy calculations. J Mol Model. 2013 Nov;19(11):5097-5112.
[2]. Freeman-Cook KD, et al. Design of selective, ATP-competitive inhibitors of Akt. J Med Chem. 2010 Jun 24;53(12):4615-4622.

1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。

2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。

PF-AKT400

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