ALM301
目录号: PL04360 纯度: ≥99%
CAS No. :1313439-71-2
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中文名称
ALM301
英文名称
ALM301
英文别名
1H-Pyrido[2,3-b][1,4]oxazin-2(3H)-one, 6-[4-(cis-1-amino-3-hydroxycyclobutyl)phenyl]-1-ethyl-7-phenyl-;VAD044;ALM301
Cas No.
1313439-71-2
分子式
C25H25N3O3
分子量
415.48
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
ALM301 是一种具有口服活性的高特异性 AKT 抑制剂,对 AKT1、AKT2 和 AKT3 的 IC50 分别 0.13 μM、0.09 μM 和 2.75 μM。ALM301 抑制 AKT 磷酸化,能在体外其调节下游信号 。ALM301可抑制癌细胞增殖和肿瘤生长。
生物活性
ALM301 is an orally active highly specific AKT inhibitor with IC 50 values of 0.13 μM, 0.09 μM and 2.75 μM for AKT1, AKT2 and AKT3, respectively. ALM301 inhibits AKT phosphorylation and modulates downstream signalling in vitro. ALM301 can inhibit cancer cell proliferation and tumor growth.
性状
Solid
IC50 & Target[1][2]
AKT1 0.13 μM (IC50) Akt2 0.09 μM (IC5
体外研究(In Vitro)
ALM301 (0.001-10 μM; 72 h) inhibits the proliferation of cancer cells, and PI3KCA-mutant MCF-7 cells is the most sensitive; increases sub-G0 population in a dose-dependent manner.
ALM301 (1 μM; 1 h) inhibits AKT phosphorylation in MCF-7 and sustains up to 48 h, with an EC50 value of 0.47 μM. has not independently confirmed the accuracy of these methods. They are for reference only.Cell Proliferation Assay
体内研究(In Vivo)
ALM301 (10, 30 and 100 mg/kg; p.o.; single dosage) inhibits pAKT in tumors and suppresses tumor growth.
ALM301 (3 or 10 mg/kg; p.o.; q.d. for 49 days) shows better tumor inhibition ability when combined with Tamoxifen (HY-13757A). has not independently confirmed the accuracy of these methods. They are for reference only.
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]. Page N, et al. Identification and development of a subtype-selective allosteric AKT inhibitor suitable for clinical development. Sci Rep. 2022 Sep 20;12(1):15715.
溶解度数据
In Vitro: DMSO : 50 mg/mL (120.34 mM; Need ultrasonic)配制储备液
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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。

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