化合物 BGT226,BGT226 maleate

化合物 BGT226|T6072|TargetMol

价格 询价
包装 1removed
最小起订量 1removed
发货地 上海
更新日期 2026-04-02
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产品详情

中文名称:化合物 BGT226英文名称:BGT226 maleate
CAS:1245537-68-1品牌: TargetMol
产地: 美国保存条件: Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
纯度规格: 98.77%产品类别: 抑制剂
货号: T6072
2026-04-02 化合物 BGT226 BGT226 maleate 1removed/RMB TargetMol 美国 Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. 98.77% 抑制剂

Product Introduction

Bioactivity

名称BGT226 maleate
描述BGT226 maleate (NVP-BGT226) is a class I PI3K/mTOR inhibitor for PI3Kα/β/γ (IC50: 4/63/38 nM) .
细胞实验NCI-H929, U266, RPMI-8226 and OPM2 MM cells are seeded in 96-well plates at a concentration of 1.5 × 104 cells/well in RPMI medium supplemented with 10% fetal bovine serum with or without NVP-BGT226 that is to be tested. After 36 hours, BrdU-labelling solution is added (final concentration: 10 μM), and cells are cultured for another 12 hours in a humidified atmosphere (37 °C/5% CO2). Then, the plates are centrifuged (10 min, 300 g), and the supernatants are discarded. The plates are dried at 60 °C for 2 hours. After fixation with ethanol/HCl for 30 min at -20 °C, the DNA is partially digested by nuclease treatment for 30 min at 37 °C. The cells are washed three times with medium and incubated with anti-BrdU-POD labelling solution for 30 min at 37 °C. The anti-POD solution is removed and the cells are washed three times with washing buffer. The ABTS substrate solution is added, and absorbance is measured in a microplate reader at 405 nm with a reference wave length of 490 nm.(Only for Reference)
体外活性The anti-proliferative and pro-apoptotic effects of NVP-BGT226 are independent of bcr-abl status. The activation of the AKT/mTOR signal cascade is suppressed by NVP-BGT226 in a concentration- and time-dependent manner. Flow cytometric analysis exhibits an accumulation of cells in the G(0)-G(1) phase with concomitant loss in the S-phase. NVP-BGT226 displays potent growth-inhibitory activity against all tested cell lines including SCC4, TU183 and KB cell lines with the IC50 ranging from 7.4 to 30.1 nM. Notably, both Detroit 562 and HONE-1 cells, which express PIK3CA mutation H1047R, are still sensitive to the growth-inhibitory effect of NVP-BGT226 treatment. In addition, the sensitivity to NVP-BGT226 between HONE-1 cells and its cisplatin-resistant variant is almost identical. Results of the terminal deoxynucleotidyl transferase-mediated dUTP nick end labeling (TUNEL) assay and the analysis of caspase 3/7 and PARP indicates that NVP-BGT226 induces cancer cell death through an apoptosis-independent pathway. NVP-BGT226 induces autophagy as indicated by the aggregation and upregulation of the microtubule-associated protein light chain 3B-II, and p62 degradation. Gene silencing of Beclin1 or cotreatment of the autophagosome inhibitor, 3-methyladenine, inhibits the NVP-BGT226-induced autophagy and leads to the retrieval of colony survival.[2] NVP-BGT226 inhibits growth in common myeloma cell lines and primary myeloma cells (such as NCI-H929, U266, RPMI-8226 and OPM2 MM cell lines) at nanomolar concentrations in a time-dependent and dose-dependent manner. NVP-BGT226 inhibits phosphorylation of protein kinase B (Akt), P70S6k and 4E-BP-1 in a time-dependent and dose-dependent manner.
体内活性In a xenografted animal model, NVP-BGT226 significantly delays tumor growth in a dose-dependent manner, along with suppressed cytoplasmic expression of p-p70 S6 kinase and the presence of autophagosome formation. NVP-BGT226 inhibits tumor growth in a dose-dependent manner in a FaDu cell xenografted mouse model. Oral administration of NVP-BGT226 at 2.5 and 5 mg/kg for 3 weeks causes 34.7% and 76.1% reduction of the tumor growth on day 21, respectively (compared with control). NVP-BGT226 displays comparable inhibition against tumor growth to rapamycin. The final volume of both groups is significantly smaller than those treated with LY294002 (a PI3K inhibitor) or the control. [2]
存储条件Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature.
溶解度Ethanol : < 1 mg/mL (insoluble or slightly soluble)
DMSO : 60 mg/mL (92.22 mM), Sonication is recommended.
10% DMSO+40% PEG300+5% Tween 80+45% Saline : 2 mg/mL (3.07 mM), Sonication is recommended.
H2O : < 1 mg/mL (insoluble or slightly soluble)
关键字PI3Kγ | PI3Kβ | PI3Kα | PI3K | Phosphoinositide 3-kinase | NVP-BGT-226 | NVP-BGT 226 | mTOR | Mammalian target of Rapamycin | Inhibitor | inhibit | BGT-226 maleate | BGT226 Maleate | BGT-226 | BGT 226 Maleate | BGT 226 | Autophagy | Apoptosis
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相关库抑制剂库 | 经典已知活性库 | 抗癌活性化合物库 | 已知活性化合物库 | 临床失败化合物库 | 激酶抑制剂库 | 神经再生化合物库 | 抗衰老化合物库 | 免疫/炎症分子化合物库 | 药物功能重定位化合物库 | 抗癌临床化合物库 | 抗癌药物库
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关键字: NVP-BGT226 (maleate)|||NVP-BGT226|||BGT226|TargetMol

公司简介

TargetMol Chemicals Inc. 总部位于马萨诸塞州波士顿,致力于为全球生化领域科学家的研究提供专业的产品和服务。TargetMol?品牌的客户群分布于40多个国家和地区,已发展成为全球知名的化合物库和小分子化合物研究供应商。 TargetMol?可提供160多种满足不同需求的化合物库,以及多种类型的生化试剂产品,包括12000多种抑制剂、16000多种天然产物和各类多肽、抗体、生命科学试剂盒等,此外,我们还建设有CADD(计算机辅助药物设计)研究中心、药理实验室、药化合成平台三大技术中心,全方位满足客户的定制需求。 凭借我们优质的产品和服务、快速高效的全球供应链和专业的技术支持,我们将有效帮助您缩短研发周期,取得更成功的结果。
成立日期 2013-04-18 (14年) 注册资本 566.265100万人民币
员工人数 100-500人 年营业额 ¥ 1亿以上
主营行业 天然产物,生化试剂,分子生物学,分子砌块,生物技术服务 经营模式 贸易,工厂,试剂,定制,服务
  • TargetMol中国(陶术生物)
VIP 4年
  • 公司成立:14年
  • 注册资本:566.265100万人民币
  • 企业类型:有限责任公司(自然人投资或控股)
  • 主营产品:小分子抑制剂、药物筛选化合物库、药物筛选等
  • 公司地址:静安区江场三路238号8楼
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