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PI3Kα-IN-9

产品编号 T61654 CAS 2715287-67-3

PI3Kα-IN-9 (compound 27) is a highly specific, orally active, and long-lasting inhibitor of PI3Kα, demonstrating potent inhibitory effects with IC50 values of 4.4, 128, 146, and 153 nM against PI3Kα, PI3Kγ, PI3Kδ, and PI3Kβ, respectively. Additionally, PI3Kα-IN-9 exhibits antiproliferative properties and effectively induces apoptosis. Given its characteristics, PI3Kα-IN-9 holds great potential for cancer research [1].

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PI3Kα-IN-9, CAS 2715287-67-3

规格	价格/CNY		货期	数量
2 mg	￥ 720		5日内发货
5 mg	￥ 1,230		5日内发货

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生物活性

化学信息

存储 & 溶解度

产品描述	PI3Kα-IN-9 (compound 27) is a highly specific, orally active, and long-lasting inhibitor of PI3Kα, demonstrating potent inhibitory effects with IC50 values of 4.4, 128, 146, and 153 nM against PI3Kα, PI3Kγ, PI3Kδ, and PI3Kβ, respectively. Additionally, PI3Kα-IN-9 exhibits antiproliferative properties and effectively induces apoptosis. Given its characteristics, PI3Kα-IN-9 holds great potential for cancer research [1].
体外活性	PI3Kα-IN-9 (compound 27) (0-8 μM; 72 hours; cancer cell lines) has antiproliferative activity and induces apoptosis [1]. PI3Kα-IN-9 (compound 27) (0-8 μM; MGC-803 cells) down-regulates the expression of PI3Kα protein, the proteins of PI3K downstream, p-AKT and p-P70S6 K [1]. Cell Viability Assay [1] Cell Line: MGC-803 (gastric cancer), SKOV-3 (ovarian cancer), PC-3(prostate cancer), MCF-7 (breast cancer), MDA-MB-231 (triple-negative breast cancer), HepG2 (liver cancer), RPMI8226 (multiple myeloma), K562 (chronic myeloid leukemia), U251 (glioma) and MOLT-4 (acute lymphoblastic leukemia) cell lines Concentration: 0-2 μM Incubation Time: 72 hours Result: Inhibited the growth of a variety of cancer cells with IC 50 values ranging from 0.43 to 1.33 μM. Apoptosis Analysis [1] Cell Line: MGC-803 cells Concentration: 0, 2, 4 and 8 μM Incubation Time: 36 hours Result: Increased the percentage of apoptotic cells from 12.07 to 61.69% in a dose-dependent manner.
体内活性	PI3Kα-IN-9 (compound 27) (1-10 mg/kg; p.o. and i.v.; for 24 hours; male Sprague-Dawley rat) has favorable stability (T 1/2 >10 h) and high bioavailability (130%) [1]. PI3Kα-IN-9 (compound 27) (30 mg/kg; p.o.; daily, for 3 weeks; male BALB/c nude mice) has antitumor activity and low cytotoxicity [1]. Animal Model: Male Sprague-Dawley rat [1] Dosage: 1 and 10 mg/kg Administration: Oral administration and intravenous injection; for 24 hours (Pharmacokinetic Analysis) Result: 1.19 parameters IV PO dose (mg/kg) 1 10 T 1/2 (h) 6.29 ﹥10 T max (h) 0.003 9.33 C max (ng/mL) 454.7 2256.7 AUC 0-t (ng·h/mL) 2237 36697 AUC 0-∞ (ng·h/mL) 2922.4 38114.3 CL (mL/h/kg) 343 F % 130.4 Animal Model: Male BALB/c nude mice [1] Dosage: 30 mg/kg Administration: Oral administration; daily, for 3 weeks Result: Inhibited tumor growth with a tumor growth inhibition (TGI) rate of 41.5%.

分子量	383.4
分子式	C18H21N7O3
CAS No.	2715287-67-3

存储

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

计算器

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稀释计算器

配液计算器

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剂量换算

对于不同动物的给药剂量换算，您也可以参考 更多...

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算，可以得到母液配置方法和体内配方的制备方法：比如您的给药剂量是10 mg/kg，每只动物体重20 g，给药体积100 μL，一共给药动物10 只，您使用的配方为5% DMSO+30% PEG300+5% Tween 80+60% ddH2O。那么您的工作液浓度为2 mg/mL。

母液配置方法：2 mg 药物溶于 50 μL DMSO (母液浓度为 40 mg/mL)，如您需要配置的浓度超过该产品的溶解度，请先与我们联系。

体内配方的制备方法：取 50 μL DMSO 主液，加入 300 μL PEG300，混匀澄清，再加 50 μL Tween 80，混匀澄清，再加 600 μL ddH2O, 混匀澄清。

第一步：请输入动物实验的基本信息

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第二步：请输入动物体内配方组成，不同的产品配方组成不同，如有配方需求，可先联系我们提供正确的体内配方。

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