BAY1082439
目录号 : KM7463 CAS No. : 1375469-38-7 纯度 : 98%

BAY1082439 是一种具有口服活性的,选择性 PI3Kα/β/δ 抑制剂。BAY1082439 也能抑制 PIK3CA 的突变形式,BAY1082439 对抑制 Pten 丢失的前列腺癌的生长有很强的作用。

规格 价格 是否有货 数量
5mg
In-stock
10mg
In-stock
25mg
In-stock
50mg
In-stock
100mg
In-stock
200mg 询价 In-stock
500mg 询价 In-stock

Other Forms of Rapamycin:

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生物活性

BAY1082439 is an orally bioavailable, selective PI3Kα/β/δ inhibitor. BAY1082439 also inhibits mutated forms of PIK3CA. BAY1082439 is highly effective in inhibiting Pten-null prostate cancer growth.

体外研究

BAY1082439 is a highly selective PI3Kα/α-balanced inhibitor. BAY1082439 has an IC50 ratio of 1:3 in biochemical assays of PI3Kα (4.9 nM) vs. PI3Kα (15.0 nM), and >1000-fold selectivity against mTOR kinase.
BAY1082439 (0.1-1 μM; 72 hours) is more effective than PI3Kα- and/or PI3Kβ-selective inhibitors in blocking PTEN-null prostate cancer cells.

Cell Viability Assay

Cell Line: PC3 and LNCaP cells (PTEN-null human prostate cancer cell lines)
Concentration: 0.1, 0.33, 1, 3.3, 10 μM
Incubation Time: 72 hours
Result: Efectively inhibited cell growth by blocking the G1/S cell cycle transition and by inducing apoptosis.
体内研究

BAY1082439 (75 mg/kg; p.o.; daily for 4 weeks) is effective in preventing Pten-null prostate cancer progression.

Animal Model: Pten conditional knockout mouse model (Pb-Cre;Pten, CP model)
Dosage: 75 mg/kg
Administration: P.o.; daily for 4 weeks
Result: Significantly decreased tumor size and P-AKT staining, nearly normal luminal architecture, and a significant reduction of Ki67-positive cells. Significantly inhibit the human prostate cancer growth.
分子式
C25H30N6O5
分子量
494.54
CAS号
1375469-38-7
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
In solvent -80°C 6 months
-20°C 1 month
溶解性数据
In Vitro: 

DMSO : 5 mg/mL (10.11 mM; ultrasonic and adjust pH to 5 with HCl)

配制储备液
浓度 溶剂体积 质量 1 mg 5 mg 10 mg
1 mM 2.0221 mL 10.1104 mL 20.2208 mL
5 mM 0.4044 mL 2.0221 mL 4.0442 mL
10 mM 0.2022 mL 1.0110 mL 2.0221 mL
*

请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液;一旦配成溶液,请分装保存,避免反复冻融造成的产品失效。
储备液的保存方式和期限:-80°C, 6 months; -20°C, 1 month。-80°C 储存时,请在 6 个月内使用,-20°C 储存时,请在 1 个月内使用。

临床试验
The molarity calculator equation
Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)
The dilution calculator equation
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
This equation is commonly abbreviated as: C1V1 = C2V2
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