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网站主页 化工产品目录 生物化工 氨基酸及其衍生物 丙氨酸类衍生物 1-[[4-[(4-氟-2-甲基-1H-吲哚-5-基)氧基]-5-甲基吡咯并[2,1-F][1,2,4]三嗪-6-基]氧基]-2-丙醇 L-丙氨酸酯 丙氨酸布立尼布
  • 丙氨酸布立尼布|T2576|TargetMol

丙氨酸布立尼布|T2576|TargetMol

Brivanib (alaninate)
649735-63-7
￥483 1mg 起订
￥1160 5mg 起订
￥2090 10mg 起订
上海 更新日期：2024-12-02

TargetMol中国（陶术生物）

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邮箱：marketing@targetmol.com

产品详情:

中文名称：
丙氨酸布立尼布
英文名称：
Brivanib (alaninate)
CAS号：
649735-63-7
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.
纯度规格：
99.66%
产品类别：
抑制剂
货号：
T2576

Product Introduction

Bioactivity

名称Brivanib (alaninate)
描述Brivanib Alaninate (BMS-582664) is the alaninate salt of a vascular endothelial growth factor receptor 2 (VEGFR2) inhibitor with potential antineoplastic activity. Brivanib strongly binds to and inhibits VEGFR2, a tyrosine kinase receptor expressed almost exclusively on vascular endothelial cells; inhibition of VEGFR2 may result in inhibition of tumor angiogenesis, inhibition of tumor cell growth, and tumor regression.
细胞实验Cells are grown in 100 μL of minimal growth medium and 1.0% heat-inactivated fetal bovine serum in 96-well collagen IV coated plates at a density of 2 × 103 per well in a 37 ℃/5% CO2 environment. Twenty-four hours later, serum is adjusted to 10%, and BMS-582664 at various dilutions are added to each well in a final volume of minimal growth media that contains 10% serum. Forty-eight hours later, 0.5 μCi of [3H]thymidine is added in a volume of 20 μL of minimal media for 24 hours. Plates are washed once in PBS. Upon removal of PBS, Trypsin is added to cells which are subsequently harvested onto glass-fiber filters using an automated harvestor. Incorporated tritium is quantified using a β-counter. Dose?response curves are generated to determine the IC50 value, which is defined as the concentration of drug required to inhibit 50% of tritium incorporation when compared to untreated serum-stimulated cells.(Only for Reference)
激酶实验Kinase inhibition assays: For the VEGFR2, Flk1 and FGFR1 kinase assays, BMS-582664 is dissolved in DMSO and diluted with water/10% DMSO to a final DMSO concentration of 2%. The kinase reactions consists of 8 ng of enzymes with GST tag, 75 μg/mL substrate, 1 μM ATP, and 0.04 μCi [γ-33P]ATP in 50 μL total reaction volume (kinase buffer:? 20 mM Tris, pH 7.0, 25 μg/mL BSA, 1.5 mM MnCl2, 0.5 mM dithiothreitol). In all cases, the reactions are incubated for 60 min at 27℃ and terminated with the addition of cold trichloroacetic acid (TCA) to a final concentration of 15%. The percent inhibition from the kinase assays is determined by nonlinear regression analyses, and data are reported as the inhibitory concentration required to achieve 50% inhibition relative to control reactions (IC50).
体外活性25 mg/kg BMS-582664在大鼠中AUC为13.4 μM×hr,Cmax为6.4 μM.50 mg/kg BMS-582664在小鼠中AUC为136 μM×hr,Cmax为41 μM.50 mg/kg和100 mg/kg BMS-582664作用于携带病患衍生的移植瘤06-0606 的小鼠,抑制肿瘤生长速度分别为55% 和13%.口服60 mg/kg BMS-582664显著降低携带病患衍生的移植瘤06-0606 的小鼠中肿瘤重量,促进细胞凋亡,降低微血管密度,抑制细胞增殖,并下调细胞周期调控.小鼠口服60 mg/kg BMS-582664,迅速吸收,Tmax为1小时,半衰期 (t1/2)为2.7小时,平均滞留时间为3.6小时.60 mg/kg和90 mg/kg BMS-582664剂量依赖性抑制携带H3396移植瘤的无胸腺小鼠中肿瘤生长,肿瘤生长抑制率分别为85%和97%.80 mg/kg和107 mg/kg.BMS-582664 处理携带L2987非小细胞肺癌移植瘤的无胸腺小鼠,剂量依赖性抑制肿瘤生长,肿瘤生长抑制率分别为85% 和 97%.100 mg/kg BMS-582664抑制两种携带移植瘤的小鼠模型（L2987和HCT116）中血管内皮细胞的增长.
体内活性BMS-582664固态稳定性较高,在50°C下放置干燥剂的12周期间仅有0.3％降解,在pH为6.5时也具有较好的液态稳定性。2 μM BMS-582664明显抑制VEGF和 bFGF刺激的SK-HEP1细胞和HepG-2细胞中VEGFR-2,FGFR-1,ERK1/2和Akt的磷酸化,而BMS-582664单独作用于未经刺激的细胞,则不影响ERK1/2,Akt,VEGFR-2和FGFR-1的磷酸化水平。BMS-582664抑制VEGF和FGF刺激的HUVECs 增殖,IC50分别为40 nM和276 nM。BMS-582664抑制CYP2C19,CYP3A4(BFC)和CYP3A4 (BzRes)细胞,IC50分别为2.4 μM,0.51 μM和1.6 μM。
存储条件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度Ethanol : 82 mg/mL (185.7 mM)
DMSO : 82 mg/mL (185.7 mM)
关键字BMS 582664 | Inhibitor | Autophagy | Vascular endothelial growth factor receptor | BMS582664 | Brivanib (alaninate) | alaninate | VEGFR | Brivanib | inhibit
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丙氨酸布立尼布|||Brivanib Alaninate|||BMS-582664|TargetMol

公司简介

上海陶术生物科技有限公司为美国Target Molecule Corp. ( Target Mol ) 在上海建立的全资子公司。我们与美国波士顿、德国慕尼黑的同事一起，为北美、欧洲和亚洲从事药物研发和生物学研究的科学家提供优质的产品和专业的服务。公司下设筛选事业部，化学事业部，生物事业部和新材料部。 从虚拟筛选到实体化合物分子供应；从商业化产品销售到个性化定制合成；从对明确靶点的分子筛选到对明确分子的多靶点筛选，从高通量筛选到化学结构优化，我们都可以满足您的科研用品及技术服务的需求。 经过在中国市场五年的精心耕耘，我们已成为筛选化合物领域优秀的供应商，为超过五百家学校和各类企业提供了品质卓越的小分子化合物和药物筛

成立日期 (12年)
注册资本 566.2651万人民币
员工人数 100-500人
年营业额 ￥ 1亿以上
经营模式 贸易,试剂,定制,服务
主营行业 化学试剂,生物活性小分子

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