米哚妥林|T3211

Midostaurin
120685-11-2

￥1490 5瓶起订

￥5790 50瓶起订

￥7910 100瓶起订

￥2390 10瓶起订

￥15900 500瓶起订

￥3970 25瓶起订

￥1870 1瓶起订

￥627 1瓶起订

上海更新日期：2024-09-14

TargetMol中国（陶术生物）

VIP12年

联系人：邵小姐

电话：021-021-33632979拨打

手机：15002134094 拨打

邮箱：marketing@targetmol.com

产品详情:

中文名称：: 米哚妥林

英文名称：: Midostaurin

CAS号：: 120685-11-2

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：: 99.56%

产品类别：: 抑制剂

货号：: T3211

Product Introduction

Bioactivity

名称	Midostaurin
描述	PKC412(Midostaurin (PKC412); CGP41231; CGP41251) is a broad spectrum protein kinase inhibitor. Midostaurin inhibits protein kinase C alpha (PKCalpha), vascular endothelial growth factor receptor 2 (VEGFR2), c-kit, platelet-derived growth factor receptor (PDGFR) and FMS-like tyrosine kinase 3 (FLT3) tyrosine kinases, which may result in disruption of the cell cycle, inhibition of proliferation, apoptosis, and inhibition of angiogenesis in susceptible tumors.
细胞实验	Each well is added with 5 mM WST-1 and 0.2 mM 1-methoxy PMS and the absorbance at 450 nm is measured by a Microplate Reader.(Only for Reference)
激酶实验	Cells are plated overnight and treated with 100 nM AZD3965 or vehicle for 24 hours. The cells are then washed, once in PBS and twice with lysis buffer (50 mM Mops, 100 mM KCl, 5 mM MgCl2, 1 mM EDTA, 0.1 mM DTT, 1 mM PMSF supplemented with 1× mini complete protease inhibitor cocktail tablets. The cells are harvested by scraping and centrifugation, and the pellet snap frozen without buffer in liquid nitrogen. Frozen aliquots of cells are thawed on ice and re-suspended in lysis buffer. Cells are lysed by 3 rounds of freezing in liquid nitrogen and thawing at 37°C for 2 minutes each. Lysates are subsequently centrifuged (13000 g, 10min, 4°C) until clear and then stored on ice. Enzyme activity in the cell lysates is determined using a micro-plate reader to measure either production or depletion of NADH/NADPH, through its absorbance at 340/10 nm, occurring as a result of direct or coupled enzyme reactions. The 96 well plates used for the assays are pre-heated to 37°C for 10 minutes prior to starting reactions, initiated by the addition of 5 μL cell lysate to 95 μL of reaction buffer (50 mM Mops pH 7.4, 100 mM KCl, 5 mM free magnesium). The standard reaction buffer is supplemented to assay the kinetics of the different enzymes. Absorbance values for controls are subtracted from absorbance of corresponding reactions. Graphpad prism 6 is used to plot V0 values against substrate concentration and determine Vmax and Km values. The Vmax is then normalised to the protein concentration in the cell lysate[1].
体外活性	Midostaurin(pkc412)是一种广谱蛋白激酶抑制剂。它与常见的PKC-α、-β、-γ、PDGFRβ、VEGF-R2、VEGF-R1以及细胞周期依赖性激酶1-细胞周期蛋白B复合体的ATP结合位点有强烈的相互作用。Midostaurin(pkc412)能够在亚微摩尔浓度下抑制各种人类和动物细胞系体外生长。此外，Midostaurin(pkc412)有效抑制了胶质母细胞瘤体外增殖，并诱导细胞在G2/M期积累及巨核形成，伴随广泛的碎片化和凋亡体生成。Midostaurin(pkc412)还能逆转肿瘤细胞体外p-糖蛋白介导的多药耐药性。[1]
体内活性	Midostaurin(pkc412)通过抑制肿瘤血管生成（通过其对VEGF受体酪氨酸激酶的影响）以及直接抑制肿瘤细胞增殖（通过其对PKCs的影响），可能抑制肿瘤生长。这种抗血管生成作用可能有助于midostaurin(pkc412)所展示的抗转移和广泛的抗肿瘤活性，以及与包括多柔比星、环磷酰胺、顺铂和吉西他滨在内的细胞毒性化合物的协同作用。口服时，midostaurin(pkc412)的最大耐受剂量为>300 mg/kg。[1]
存储条件	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice.
溶解度	DMSO : 55 mg/mL (96.38 mM)
关键字	CGP-41251 \| Nitric oxide synthases \| SCFR \| inhibit \| CGP-41231 \| Protein kinase C \| Inhibitor \| Apoptosis \| NO Synthase \| CD117 \| Midostaurin \| c-Kit \| VEGFR \| PKC-412 \| NOS \| PKC 412 \| CGP 41231 \| CGP41251 \| Vascular endothelial growth factor receptor \| PKC
相关产品	Darovasertib \| α-Vitamin E
相关库	经典已知活性库 \| 抗癌上市药物库 \| 已知活性化合物库 \| EMA 上市药物库 \| FDA 上市药物库 \| 药物功能重定位化合物库 \| 抗癌临床化合物库 \| 抗癌药物库

N-Benzoylstaurosporine|||PKC412|||CGP41231|||米哚妥林|||CGP 41251|||苯甲酰基十字孢碱

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