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  • 化合物 Flavopiridol hydrochloride|T2615|TargetMol

化合物 Flavopiridol hydrochloride|T2615|TargetMol

Flavopiridol hydrochloride
131740-09-5
153 1mg 起订
222 2mg 起订
388 5mg 起订
上海 更新日期:2024-12-02

TargetMol中国(陶术生物)

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产品详情:

中文名称:
化合物 Flavopiridol hydrochloride
英文名称:
Flavopiridol hydrochloride
CAS号:
131740-09-5
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:
99.88%
产品类别:
抑制剂
货号:
T2615

Product Introduction

Bioactivity

名称Flavopiridol hydrochloride
描述Flavopiridol hydrochloride (MDL 107826A) is a synthetic N-methylpiperidinyl chlorophenyl flavone compound. As an inhibitor of cyclin-dependent kinase, alvocidib induces cell cycle arrest by preventing phosphorylation of cyclin-dependent kinases (CDKs) and by down-regulating cyclin D1 and D3 expression, resulting in G1 cell cycle arrest and apoptosis. This agent is also a competitive inhibitor of adenosine triphosphate activity.
细胞实验Cells grown at a density of 1 × 106 cells/mL are exposed to Flavopiridol for different concentrations and time periods. DNA is extracted. Briefly, cells are washed once with cold phosphate-buffered saline (PBS) and lysed with 3 mL lysis buffer (5 mM Tris-HCL [pH 7.5]; 20 mM EDTA; 0.5% Triton X-100) for 15 minutes at 4 °C. The chromatin of the cell lysates is isolated by centrifugation (20 minutes at 26,000 g, 4 °C). The supernatants containing small DNA fragments are extracted sequentially with phenol, phenol:chloroform (1:1), and chloroform. Nucleic acids are precipitated in 0.5 M NaCl, 90% ethanol at -20 °C overnight. RNA is then digested by bovine RNAaseA (60 μg/mL). After sequential reextraction and reprecipitation, DNA is dissolved in 10 mM Tris-HCL (pH 7.5), 1 mM EDTA, 0.5% sodium dodecyl sulfate (SDS) before electrophoresis on 1.6% agarose gel. (Only for Reference)
激酶实验Recombinant CDKs Kinase Reactions: CDKs activities are determined in microtiter plates as follows. Forty μg Gst-Rb are mixed with different amounts of Flavopiridol and unlabeled ATP. Reactions are then started by the addition of an ammonium sulfate cut of the S100 fraction obtained from insect cells expressing recombinant human CDKs. The final reaction conditions are 10 mM MgCl2, 50 mM Tris-HCl (pH 7.5), and 1 mM DTT. The final concentration of ATP is adjusted accordingly. Radiolabeled ATP is used as a phosphoryl donor. The reaction is carried out for 2.5 minutes at 30 °C after addition of enzyme and then terminated with the addition of EDTA. The Gst-Rb is then captured with glutathione-Sepharose and the incorporated radioactivity is determined by liquid scintillation counting.
体外活性在SUDHL-4皮下注射淋巴瘤模型的老鼠中静脉注射7.5 mg/kg Flavopiridol,模型鼠的肿瘤大部分(8分之2)或者完全(8分之4)消退,其中两只动物保持无病状持续60天以上,整体生长延迟73.2%.每天以最大耐受剂量10 mg/kg 口服给药Flavopiridol,在第1-4天及7-11天,影响PRXF1337的肿瘤消退,在PRXF1369中肿瘤停滞持续4周.用7.5 mg/kg Flavopiridol静脉内、或腹膜内连续注射Flavopiridol5天后,12个晚期皮下(sc)人HL-60异种移植鼠中的11个肿瘤完全消退,治疗一疗程后移植鼠数月无病.
体内活性Flavopiridol以时间和浓度依赖性方式诱导人类乳腺癌细胞G1期阻滞并抑制CDK2和CDK4。 Flavopiridol约12小时的短时处理,会诱导造血细胞系(包括SUDHL4,SUDHL6(B细胞系),Jurkat和MOLT4(T细胞系)和HL60(骨髓))的细胞凋亡。一项研究Flavopiridol处理可诱导人成胶质细胞瘤T98 g细胞系产生大量的AKT-Ser473磷酸化。在克隆形成实验中,Flavopiridol在23人肿瘤模型中作为高效的细胞毒性化合物,平均IC70是8 ng/mL。
存储条件Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度H2O : 43.8 mg/mL (100 mM)
DMSO : 43.8 mg/mL (100 mM)
关键字Human immunodeficiency virus | HIV | Inhibitor | Autophagy | NSC649890 | NSC-649890 | CDK | Alvocidib | HL-275 | inhibit | HMR 1275 | L86-8275 | HMR-1275 | HMR1275 | Flavopiridol | Flavopiridol hydrochloride | Flavopiridol Hydrochloride | Cyclin dependent kinase | HL275
相关产品Guanidine hydrochloride | Naringin | Valproic Acid | Gefitinib | Aceglutamide | Emtricitabine | Hydroxychloroquine | Lamivudine | Dextran sulfate sodium salt (MW 4500-5500) | Stavudine | Paeonol | Sodium 4-phenylbutyrate
相关库抑制剂库 | 血脑屏障通透化合物库 | 经典已知活性库 | 已知活性化合物库 | 抗感染化合物库 | 黄酮类天然产物库 | 激酶抑制剂库 | 抗衰老化合物库 | 抗病毒库 | 药物功能重定位化合物库
NSC 649890 HCl|||NSC 649890|||MDL 107826A|||HL 275|||FLAVOPIRIDOL HCL|||Alvocidib Hydrochloride|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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