BGT226 NVP-BGT226|cas:915020-55-2|西域试剂

BGT226 NVP-BGT226,99.51%

产品编号：Bellancom-13334A| CAS NO：915020-55-2| 分子式：C₂₈H₂₅F₃N₆O₂| 分子量：534.53

BGT226 (NVP-BGT226) 是一种 PI3K (针对 PI3Kα，PI3Kβ，PI3Kγ 的 IC50分别是4 nM，63 nM，38 nM ) /mTOR 双抑制剂，对人头颈癌细胞具有较强的生长抑制活性。

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货号	价格	库存与货期
Bellancom-13334A	￥1430.00	杭州北京（现货）
Bellancom-13334A	￥2530.00	杭州北京（现货）
Bellancom-13334A	￥9900.00	杭州北京（现货）
Bellancom-13334A	￥13730.00	杭州北京（现货）

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BGT226 NVP-BGT226

产品介绍

BGT226 (NVP-BGT226) 是一种 PI3K (针对 PI3Kα，PI3Kβ，PI3Kγ 的 IC₅₀分别是4 nM，63 nM，38 nM ) /mTOR 双抑制剂，对人头颈癌细胞具有较强的生长抑制活性。

生物活性

BGT226 (NVP-BGT226) is a PI3K (with IC₅₀s of 4 nM, 63 nM and 38 nM for PI3Kα, PI3Kβ and PI3Kγ)/mTOR dual inhibitor which displays potent growth-inhibitory activity against human head and neck cancer cells.

体外研究

BGT226 shows significant growth inhibition or signal blockage profiles compared with LY294002 and Rapamycin. BGT226 (10-10000 nM) inhibits FaDu and OECM1 cells growth with IC₅₀s of 23.1±7.4 and 12.5±5.1 nM, respectively.
The expression levels of p-mTOR Ser2481 are decreased in BGT226-treated cell lines (200 nM; 24 hours) and both p-AKT Ser473 and p-mTOR Ser2448 are also decreased in BGT226-treated cell lines.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Cell Viability Assay

Cell Line:	FaDu cells; OECM1 cells
Concentration:	10, 100, 1000, 10000 nM
Incubation Time:
Result:	Inhibited FaDu and OECM1 cells growth with IC₅₀s of 23.1±7.4 and 12.5±5.1 nM, respectively.

Western Blot Analysis

Cell Line:	FaDu cells; OECM1 cells
Concentration:	200 nM
Incubation Time:	24 hours
Result:	p-mTOR Ser2481 expression levels decreased, and both p-AKT Ser473 and p-mTOR Ser2448 expression levels also decreased.

体内研究
(In Vivo)

BGT226 (2.5 and 5 mg/kg; oral administration for 21 days in male athymic mice) causes 34.7% and 76.1% reduction of the tumor growth on day 21 compared with control.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male athymic mice (strain BALB/cAnN.Cg-Foxn1nu/CrlNarl) with FaDu cell xenografted mouse model
Dosage:	2.5 and 5 mg/kg
Administration:	Oral administration; 21 days
Result:	Caused 34.7% and 76.1% reduction of the tumor growth.

体内研究

BGT226 (2.5 and 5 mg/kg; oral administration for 21 days in male athymic mice) causes 34.7% and 76.1% reduction of the tumor growth on day 21 compared with control.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male athymic mice (strain BALB/cAnN.Cg-Foxn1nu/CrlNarl) with FaDu cell xenografted mouse model
Dosage:	2.5 and 5 mg/kg
Administration:	Oral administration; 21 days
Result:	Caused 34.7% and 76.1% reduction of the tumor growth.

体内研究

BGT226 (2.5 and 5 mg/kg; oral administration for 21 days in male athymic mice) causes 34.7% and 76.1% reduction of the tumor growth on day 21 compared with control.

西域 has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Male athymic mice (strain BALB/cAnN.Cg-Foxn1nu/CrlNarl) with FaDu cell xenografted mouse model
Dosage:	2.5 and 5 mg/kg
Administration:	Oral administration; 21 days
Result:	Caused 34.7% and 76.1% reduction of the tumor growth.

性状

Solid

溶解性数据

In Vitro:

DMSO : 10 mg/mL (18.71 mM; ultrasonic and warming and heat to 60°C)

配制储备液

浓度溶剂体积质量	1 mg	5 mg	10 mg

1 mM	1.8708 mL	9.3540 mL	18.7080 mL
5 mM	0.3742 mL	1.8708 mL	3.7416 mL
10 mM	0.1871 mL	0.9354 mL	1.8708 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。

In Vivo:

请根据您的实验动物和给药方式选择适当的溶解方案。以下溶解方案都请先按照 In Vitro 方式配制澄清的储备液，再依次添加助溶剂：

——为保证实验结果的可靠性，澄清的储备液可以根据储存条件，适当保存；体内实验的工作液，建议您现用现配，当天使用；以下溶剂前显示的百
分比是指该溶剂在您配制终溶液中的体积占比；如在配制过程中出现沉淀、析出现象，可以通过加热和/或超声的方式助溶

1.

请依序添加每种溶剂： 10% DMSO 40% PEG300 5% Tween-80 45% saline
Solubility: ≥ 1 mg/mL (1.87 mM); Clear solution

此方案可获得 ≥ 1 mg/mL (1.87 mM，饱和度未知) 的澄清溶液。
以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 400 μL PEG300 中，混合均匀；向上述体系中加入50 μL Tween-80，混合均匀；然后继续加入 450 μL生理盐水定容至 1 mL。
将 0.9 g 氯化钠，完全溶解于 100 mL ddH₂O 中，得到澄清透明的生理盐水溶液
2.

请依序添加每种溶剂： 10% DMSO 90% corn oil
Solubility: ≥ 1 mg/mL (1.87 mM); Clear solution

此方案可获得 ≥ 1 mg/mL (1.87 mM，饱和度未知) 的澄清溶液，此方案不适用于实验周期在半个月以上的实验。
以 1 mL 工作液为例，取 100 μL 10.0 mg/mL 的澄清 DMSO 储备液加到 900 μL玉米油中，混合均匀。

*以上所有助溶剂都可在西域网站选购。

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

参考文献

. Markman B, et al. Phase I safety, pharmacokinetic, and pharmacodynamic study of the oral phosphatidylinositol-3-kinase and mTOR inhibitor BGT226 in patients with advanced solid tumors. Ann Oncol. 2012 Sep;23(9):2399-408. [Content Brief]

. Chang KY, et al. Novel phosphoinositide 3-kinase/mTOR dual inhibitor, NVP-BGT226, displays potent growth-inhibitory activity against human head and neck cancer cells in vitro and in vivo. Clin Cancer Res. 2011 Nov 15;17(22):7116-26. [Content Brief]

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BGT226 NVP-BGT226,99.51%

BGT226 NVP-BGT226

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