PI-273
目录号: PL09836 纯度: ≥98.0%
CAS No. :925069-34-7
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中文名称
PI-273
中文别名
2-(3-(4-氯苯甲酰基)硫脲基)-4-乙基-5-甲基噻吩-3-甲酰胺
英文名称
PI-273
英文别名
ARONIS023355;STK355951;BB0293001;2-({[(4-chlorobenzoyl)amino]carbonothioyl}amino)-4-ethyl-5-methylthiophene-3-carboxamide;2-({[(4-chlorophenyl)carbonyl]carbamothioyl}amino)-4-ethyl-5-methylthiophene-3-carboxamide;2-({[(4-chlorobenzoyl)amino]carbothioyl}amino)-4-ethyl-5-methyl-3-thiophenecarboxamide;2-({[(4-chlorobenzoyl)amino]carbonothioyl}amino)-4-ethyl-5-methyl-3-thiophenecarboxamide;PI-273;2-[[[(4-Chlorobenzoyl)amino]thioxomethyl]amino]-4-ethyl-5-methyl-3-thiophenecarboxamide (ACI);2-[(4-Chlorobenzoyl)carbamothioylamino]-4-ethyl-5-methylthiophene-3-carboxamide;2-[3-(4-Chloro-benzoyl)-thioureido]-4-ethyl-5-methyl-thiophene-3-carboxylic acid amide;PI 273
Cas No.
925069-34-7
分子式
C16H16ClN3O2S2
分子量
381.90
包装储存
Powder -20°C 3 years;4°C 2 years
产品详情
PI-273 是第一种可逆的和特异性磷脂酰肌醇 4-激酶 (PI4KIIα) 抑制剂,IC50 为 0.47 μM。PI-273 可以抑制乳腺癌细胞的增殖,阻断细胞周期并诱导细胞凋亡。
生物活性
PI-273 is a first reversibly and specific phosphatidylinositol 4-kinase (PI4KIIα) inhibitor with an IC 50 of 0.47 μM. PI-273 can inhibit breast cancer cell proliferation, block the cell cycle and induce cell apoptosis.
性状
Solid
IC50 & Target[1][2]
PI4KIIα 0.47 μM (IC50)
体外研究(In Vitro)
PI-273 (2 μM; 48 hours) blocks the cell cycle at the G2-M phase.
PI-273 (2 μM; 48 hours) induces cell apoptosis in all three Ras wild-type breast cancer cells: MCF-7, T-47D, and SK-BR-3.
PI-273 (0.5-2 μM; for 3 days) can suppress the AKT signaling pathway in a dose- and time-dependent manner.
PI-273 of 1 μM and 2 μM inhibits the cell proliferation of both MCF-7 and T-47D cells in a time-dependent manner.
has not independently confirmed the accuracy of these methods. They are for reference only.
体内研究(In Vivo)
PI-273 (intraperitoneal injection; 25 mg/kg/day; 15 days) profoundly suppresses the tumor volume and weight in the MCF-7 xenografts.
PI-273 (0.5 mg/kg (intravenously) or 1.5 mg/kg (intragastrically); 0.08-5 hours) has a half-life of 0.411 hours for intravenous administration and 1.321 hours for intragastrical administration, and the absolute bioavailability of PI-273 is 5.1%.
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]. Li J, et al. PI-273, a Substrate-Competitive, Specific Small-Molecule Inhibitor of PI4KIIα, Inhibits the Growth of Breast Cancer Cells. Cancer Res. 2017 Nov 15;77(22):6253-6266.
溶解度数据
In Vitro: DMSO : 6.02 mg/mL (15.76 mM; ultrasonic and warming and heat to 60°C)配制储备液
搜索质检报告(COA)

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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