化合物 BGT226|T6072|TargetMol

價格	￥413	￥997	￥1620
包裝	1mg	5mg	10mg

最小起訂量	1mg
發(fā)貨地	上海
更新日期	2024-12-12

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產(chǎn)品詳情

中文名稱:化合物 BGT226	英文名稱:BGT226 maleate
CAS:1245537-68-1	品牌: TargetMol
產(chǎn)地: 美國	保存條件: Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
純度規(guī)格: 98.78%	產(chǎn)品類別: 抑制劑
貨號: T6072

Product Introduction

Bioactivity

名稱	BGT226 maleate
描述	BGT226 maleate (NVP-BGT226) is a class I PI3K/mTOR inhibitor for PI3Kα/β/γ (IC50: 4/63/38 nM) .
細胞實驗	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)
體外活性	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.
體內(nèi)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]
存儲條件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	Ethanol : < 1 mg/mL (insoluble or slightly soluble) DMSO : 60 mg/mL (92.22 mM), Sonication is recommended. H2O : < 1 mg/mL (insoluble or slightly soluble)
關鍵字	PI3K \| BGT-226 \| mTOR \| NVP-BGT-226 \| Apoptosis \| Mammalian target of Rapamycin \| Phosphoinositide 3-kinase \| inhibit \| BGT 226 Maleate \| NVP-BGT 226 \| BGT 226 \| BGT226 Maleate \| BGT226 maleate \| Autophagy \| BGT-226 maleate \| Inhibitor \| BGT-226 Maleate
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相關庫	抑制劑庫 \| 經(jīng)典已知活性庫 \| 抗癌活性化合物庫 \| 已知活性化合物庫 \| 激酶抑制劑庫 \| 含氟化合物庫 \| 抗衰老化合物庫 \| 藥物功能重定位化合物庫 \| 抗癌臨床化合物庫 \| 抗癌藥物庫

關鍵字： NVP-BGT226 (maleate)|||NVP-BGT226|||BGT226|TargetMol

公司簡介

TargetMol Chemicals Inc. 總部位于馬薩諸塞州波士頓，致力于為全球生化領域科學家的研究提供專業(yè)的產(chǎn)品和服務。TargetMol?品牌的客戶群分布于40多個國家和地區(qū)，已發(fā)展成為全球知名的化合物庫和小分子化合物研究供應商。 TargetMol?可提供160多種滿足不同需求的化合物庫，以及多種類型的生化試劑產(chǎn)品，包括12000多種抑制劑、16000多種天然產(chǎn)物和各類多肽、抗體、生命科學試劑盒等，此外，我們還建設有CADD（計算機輔助藥物設計）研究中心、藥理實驗室、藥化合成平臺三大技術中心，全方位滿足客戶的定制需求。憑借我們優(yōu)質的產(chǎn)品和服務、快速高效的全球供應鏈和專業(yè)的技術支持，我們將有效幫助您縮短研發(fā)周期，取得更成功的結果。

成立日期	2013-04-18 （12年）	注冊資本	566.265100萬人民幣
員工人數(shù)	100-500人	年營業(yè)額	￥ 1億以上
主營行業(yè)	天然產(chǎn)物,生化試劑,分子生物學,分子砌塊,生物技術服務	經(jīng)營模式	貿(mào)易,工廠,試劑,定制,服務

TargetMol中國（陶術生物）

VIP 3年

公司成立：12年
注冊資本：566.265100萬人民幣
企業(yè)類型：有限責任公司(自然人投資或控股)
主營產(chǎn)品：小分子抑制劑、藥物篩選化合物庫、藥物篩選等
公司地址：靜安區(qū)江場三路238號8樓

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化合物 BGT226|T6072|TargetMol相關廠家報價

產(chǎn)品名稱	價格		公司名稱	報價日期
PI3K I型抑制劑（NVP-BGT226）	詢價	VIP6年	上海澤葉生物科技有限公司	2025-01-10
aladdin 阿拉丁 N125612 BGT226 (NVP-BGT226) maleate 1245537-68-1 ≥98%	￥1029.90	VIP1年	上海阿拉丁生化科技股份有限公司	2024-11-29
aladdin 阿拉丁 B408695 BGT226 (NVP-BGT226) maleate 1245537-68-1 10mM in DMSO	￥2396.90	VIP13年	上海阿拉丁生化科技股份有限公司	2024-10-31
NVP-BGT226	￥1400		南京百鑫德諾生物科技有限公司	2024-09-26

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