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Flavopiridol hydrochloride

产品编号 T2615Cas号 131740-09-5
别名 Alvocidib Hydrochloride, NSC 649890, MDL 107826A, HL 275, FLAVOPIRIDOL HCL, NSC 649890 HCl

Flavopiridol hydrochloride (MDL 107826A) 是一种CDK 的广谱抑制剂,与 ATP 竞争性地抑制 CDK1,CDK2 和 CDK4 的活性,IC50值分别为 30, 170, 100 nM。

Flavopiridol hydrochloride

Flavopiridol hydrochloride

纯度: 99.88%
产品编号 T2615 别名 Alvocidib Hydrochloride, NSC 649890, MDL 107826A, HL 275, FLAVOPIRIDOL HCL, NSC 649890 HClCas号 131740-09-5

Flavopiridol hydrochloride (MDL 107826A) 是一种CDK 的广谱抑制剂,与 ATP 竞争性地抑制 CDK1,CDK2 和 CDK4 的活性,IC50值分别为 30, 170, 100 nM。

规格价格库存数量
1 mg¥ 153现货
2 mg¥ 222现货
5 mg¥ 388现货
10 mg¥ 546现货
25 mg¥ 898现货
1 mL x 10 mM (in DMSO)¥ 427现货
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纯度:99.88%
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产品介绍

生物活性
产品描述
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.
靶点活性
CDK2:40 nM, CDK6:40 nM, CDK1:40 nM, CDK4:40 nM, CDK7:300 nM
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。
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.
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)
别名Alvocidib Hydrochloride, NSC 649890, MDL 107826A, HL 275, FLAVOPIRIDOL HCL, NSC 649890 HCl
化学信息
分子量438.3
分子式C21H21Cl2NO5
CAS No.131740-09-5
储存&溶解度
存储Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
溶解度信息
H2O: 43.8 mg/mL (100 mM)
DMSO: 43.8 mg/mL (100 mM)
溶液配制表
H2O/DMSO
1mg5mg10mg50mg
1 mM2.2815 mL11.4077 mL22.8154 mL114.0771 mL
5 mM0.4563 mL2.2815 mL4.5631 mL22.8154 mL
10 mM0.2282 mL1.1408 mL2.2815 mL11.4077 mL
20 mM0.1141 mL0.5704 mL1.1408 mL5.7039 mL
50 mM0.0456 mL0.2282 mL0.4563 mL2.2815 mL
100 mM0.0228 mL0.1141 mL0.2282 mL1.1408 mL

计算器

  • 摩尔浓度 计算器
  • 稀释 计算器
  • 配液 计算器
  • 分子量 计算器

体内实验配液计算器

请在以下方框中输入您的动物实验信息后点击计算,可以得到母液配置方法和体内配方的制备方法:
TargetMol | Animal experiments比如您的给药剂量是 10 mg/kg ,每只动物体重 20 g ,给药体积 100 μLTargetMol | Animal experiments 一共给药动物 10 只 ,您使用的配方为 5% TargetMol | reagent DMSO+ 30%PEG300+ 5%Tween 80 + 60% ddH2O. 那么您的工作液浓度为 2 mg/mL
母液配置方法: 2 mg 药物溶于 50 μLDMSOTargetMol | reagent ( 母液浓度为 40 mg/mL ), 如您需要配置的浓度超过该产品的溶解度,请先与我们联系。
体内配方的制备方法:50μLDMSOTargetMol | reagent 母液,添加 300 μLPEG300TargetMol | reagent 混匀澄清,再加 50μLTween 80, 混匀澄清,再加 600μLddH2OTargetMol | reagent 混匀澄清

以上为“体内实验配液计算器”的使用方法举例,并不是具体某个化合物的推荐配制方式,请根据您的实验动物和给药方式选择适当的溶解方案。

1 请输入动物实验的基本信息
mg/kg
g
μL
2 请输入动物体内配方组成,不同的产品配方组成不同,如有配方需求,可先联系我们提供正确的体内配方。
% DMSO
%
%Tween 80
%ddH2O

剂量转换

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