BGT226

立即咨询

BGT226

本产品不向个人销售，仅用作科学研究，不用于任何人体实验及非科研性质的动物实验。

CAS NO:

915020-55-2

包装与价格：

包装	价格(元)
100mg	电议
250mg	电议
500mg	电议

产品名称

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 aPI3K(withIC₅₀s of 4 nM, 63 nM and 38 nM forPI3Kα,PI3KβandPI3Kγ)/mTORdual inhibitor which displays potent growth-inhibitory activity against human head and neckcancercells^[1]^[2].

IC₅₀& Target^[1]

PI3Kα

4 nM (IC₅₀)

PI3Kβ

63 nM (IC₅₀)

PI3Kγ

38 nM (IC₅₀)

mTOR

Autophagy

体外研究
(In Vitro)

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^[2].
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^[2].

Cell Viability Assay^[2]

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^[2]

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^[2].

Animal Model:	Male athymic mice (strain BALB/cAnN.Cg-Foxn1nu/CrlNarl) with FaDu cell xenografted mouse model^[2]
Dosage:	2.5 and 5 mg/kg
Administration:	Oral administration; 21 days
Result:	Caused 34.7% and 76.1% reduction of the tumor growth.

Clinical Trial

分子量

534.53

Formula

C₂₈H₂₅F₃N₆O₂

CAS 号

915020-55-2

运输条件

Room temperature in continental US; may vary elsewhere.

储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.