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生物化工
抑制劑
蛋白酪氨酸激酶
3-[(4-喹啉甲基)氨基]-N-[4-(三氟甲氧基)苯基]-2-噻吩甲酰胺
噻爾非尼
噻爾非尼|T2624|TargetMol
價(jià)格
¥
328
¥
455
¥
689
包裝
1mg
2mg
5mg
最小起訂量
1mg
發(fā)貨地
上海
更新日期
2024-12-12
QQ交談
微信洽談
產(chǎn)品詳情
中文名稱:
噻爾非尼
英文名稱:
OSI-930
CAS:
728033-96-3
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:
99.76%
產(chǎn)品類別:
抑制劑
貨號:
T2624
2024-12-12
噻爾非尼
OSI-930
1mg/328RMB;2mg/455RMB;5mg/689RMB
328
TargetMol
美國
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
99.76%
抑制劑
Product Introduction
Bioactivity
名稱
OSI-930
描述
OSI-930, an orally active inhibitor of c-Kit and the vascular endothelial growth factor receptor-2 (VEGFR-2), targets cancer cell proliferation and blood vessel growth (angiogenesis) in tumors.
細(xì)胞實(shí)驗(yàn)
For assays of cell proliferation and apoptosis, cells are seeded into 96-well plates and incubated for 2 to 3 days in the presence of OSI-930 at various concentrations. Inhibition of cell growth is determined by luminescent quantitation of the intracellular ATP content using CellTiterGlo. Induction of caspase-dependent apoptosis by OSI-930 is quantitated by an enzymatic caspase 3/7 assay. Inhibition of angiogenesis by OSI-930 is monitored using the rat aortic ring endothelial sprout outgrowth assay. Sections of aorta are prepared from CO2-euthanized male rats and cultured in vitro in a collagen matrix in the presence or absence of OSI-930. The collagen matrix is prepared from type 1 rat tail collagen solubilized in 0.1% acetic acid at 3 mg/mL, which is combined with 0.125 volume collagen buffer (0.05 N NaOH, 200 mM HEPES, 260 mM NaHCO3), 0.125 volume of medium 199, 0.0125 volume of 1 M NaOH, and 1% GlutaMax. Aortic rings are embedded in 0.4 mL of this matrix in six-well plates, to which 0.5 mL endothelial basal medium and the appropriate amount of OSI-930 is added; the rings are then incubated for 10 days and the resultant angiogenic sprout outgrowth is digitally quantitated from images by measurement of the sprout-containing area within a series of concentric rings around the aortic tissue area.(Only for Reference)
激酶實(shí)驗(yàn)
Protein kinase assays : Protein kinase assays are either done in-house by ELISA-based assay methods (Kit, KDR, PDGFRα, and PDGFRβ) or by a radiometric method. In-house ELISA assays used poly(Glu:Tyr) as the substrate bound to the surface of 96-well assay plates; phosphorylation is then detected using an antiphosphotyrosine antibody conjugated to HRP. The bound antibody is then quantitated using ABTS as the peroxidase substrate by measuring the absorbance at 405/490 nm. All assays uses purified recombinant kinase catalytic domains that are either expressed in insect cells or in bacteria. The Kit and EGFR protein used for in-house assays are prepared internally; other enzymes are obtained. Recombinant Kit protein is expressed as an NH2-terminal glutathione S-transferase fusion protein in insect cells and is initially purified as a nonphosphorylated (nonactivated) enzyme with a relatively high Km for ATP (400 μM). In some assays, an activated (tyrosine phosphorylated) form of the enzyme is prepared by incubation with 1 mM ATP for 1 hour at 30 °C. The phosphorylated protein is then passed through a desalting column to remove the majority of the ATP and stored at ?80 °C in buffer containing 50% glycerol. The resultant preparation has a considerably higher specific activity and a lower Km for ATP (25 μM) than the initial nonphosphorylated preparation. The inhibition of Kit autophosphorylation by OSI-930 is assayed by incubation of the nonphosphorylated enzyme at 30 °C in the presence of 200 μM ATP and various concentrations of OSI-930. The reaction is stopped by removal of aliquots into SDS-PAGE sample buffer followed by heating to 100 °C for 5 minutes. The degree of phosphorylation of Kit is then determined by immunoblotting for both total Kit and phosphorylated Kit.
體外活性
在HMC-1, NCI-SNU-5, COLO-205和U251移植瘤模型中,口服OSI-930(200 mg/kg)能夠夠抑制腫瘤細(xì)胞增殖.
體內(nèi)活性
在HMC-1 細(xì)胞系中(IC50=14 nM),OSI-930抑制細(xì)胞增殖,誘導(dǎo)細(xì)胞凋亡。OSI-930能夠抑制多種重組受體酪氨酸激酶,Kit(IC50=80 nM), KDR(IC50=9 nM), Flt( IC50=8 nM), CSF-1R(IC50=15 nM), c-Raf (IC50=41 nM)和Lck(IC50=22 nM)。
存儲條件
Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度
DMSO : 82 mg/mL (184.9 mM)
Ethanol : 3 mg/mL (6.76 mM)
關(guān)鍵字
CSF-1R | Inhibitor | CD117 | Vascular endothelial growth factor receptor | CSF1R | colony stimulating factor 1 receptor | antitumor | c-Fms | SCFR | c-Kit | VEGFR | selective | OSI930 | CSF-1 receptor | OSI-930 | Apoptosis | inhibit
相關(guān)產(chǎn)品
L-Glutamic acid | Metronidazole | 5-Fluorouracil | Dextran sulfate sodium salt (MW 4500-5500) | Stavudine | Tributyrin | Myricetin | Sorafenib | L-Ascorbic acid | Acetylcysteine | Salicylic acid | Sodium 4-phenylbutyrate
相關(guān)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 | 膜蛋白靶向化合物庫 | 藥物功能重定位化合物庫 | 疼痛相關(guān)化合物庫 | 抗癌臨床化合物庫 | 抗癌藥物庫
關(guān)鍵字:
噻爾非尼|||OSI 930|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(lǐng)域科學(xué)家的研究提供專業(yè)的產(chǎn)品和服務(wù)。TargetMol?品牌的客戶群分布于40多個(gè)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(yīng)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(xué)試劑盒等,此外,我們還建設(shè)有CADD(計(jì)算機(jī)輔助藥物設(shè)計(jì))研究中心、藥理實(shí)驗(yàn)室、藥化合成平臺三大技術(shù)中心,全方位滿足客戶的定制需求。 憑借我們優(yōu)質(zhì)的產(chǎn)品和服務(wù)、快速高效的全球供應(yīng)鏈和專業(yè)的技術(shù)支持,我們將有效幫助您縮短研發(fā)周期,取得更成功的結(jié)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?duì)I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(xué),分子砌塊,生物技術(shù)服務(wù)
經(jīng)營模式
貿(mào)易,工廠,試劑,定制,服務(wù)
TargetMol中國(陶術(shù)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(zé)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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