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- CAS号：
942425-68-5
- 规格：
1mLx10mM(inDMSO)/1mg/5mg/10mg/25mg/50mg/100mg/200mg/500mg
| 规格： | 1mLx10mM(inDMSO) | 产品价格： | ￥364.0 |
|---|---|---|---|
| 规格： | 1mg | 产品价格： | ￥164.0 |
| 规格： | 5mg | 产品价格： | ￥330.0 |
| 规格： | 10mg | 产品价格： | ￥462.0 |
| 规格： | 25mg | 产品价格： | ￥750.0 |
| 规格： | 50mg | 产品价格： | ￥1064.0 |
| 规格： | 100mg | 产品价格： | ￥1728.0 |
| 规格： | 200mg | 产品价格： | ￥2576.0 |
| 规格： | 500mg | 产品价格： | ￥4136.0 |
Product Introduction
Bioactivity
| 名称 | PHA-767491 hydrochloride |
| 描述 | PHA-767491 hydrochloride (CAY-10572 hydrochloride) is an effective ATP-competitive dual Cdc7/CDK9 inhibitor (IC50: 10/34 nM). It has ~20-fold selectivity against GSK3-β and CDK1/2, 50-fold selectivity against CDK5 and MK2, 100-fold selectivity against CHK2 and PLK1. |
| 细胞实验 | For assays in 96 well plates 2500 cells are plated per well. After 24 hours, cells are treated with small molecule inhibitors and incubated for 72 hours at 37°C. Subsequently the cells are lysed and the ATP content is measured as an indicator of metabolically active cells using the CellTiter-Glo assay. IC50 values are calculated using the GraphPad software. For assays in six-well plates, 100,000 cells are plated per well. After 24 hours, cells are treated with small molecule inhibitors and incubated for varying time points. Cells are trypsinized and a suspension is made in 5 mL of phosphate buffered saline. 30 μL of this suspension is mixed with 30 μL of CellTiter-Glo reagent followed by a 10-minute incubation at room temperature. Luminescence is measured using EnVision 2104 Multilabel Reader and BioTek Synergy Neo Microplate Reader. |
| 激酶实验 | 20 ng of purified human DDK is pre-incubated with increasing concentrations of each DDK inhibitor for 5 min. Then 10 μCi (γ)-32P ATP and 1.5 μM cold ATP are added in a buffer containing 50 mM Tris-HCl (pH 7.5), 10 mM MgCl2, and 1 mM DTT and incubated for 30 min at 30°C. The proteins are denatured in 1X Laemmli buffer at 100°C followed by SDS-PAGE and autoradiography on HyBlot CL film. Auto-phosphorylation of DDK is used as an indicator of its kinase activity. 32P-labeled bands are quantified using ImageJ and the IC50 values are calculated using GraphPad. |
| 体外活性 | PHA-767491对HCC1954细胞（IC50：0.64μM）和Colo-205细胞（IC50：1.3μM）的增殖具有抑制作用，并且是体外DDK抑制剂（IC50：18.6nM）。PHA-767491（2μM）在24小时内完全消除HCC1954细胞中Mcm2的磷酸化[1]。PHA-767491与5-FU联合使用时，表现出更强的细胞毒性，并通过显著增加caspase 3激活和poly(ADP-Ribose) polymerase分裂来诱导HCC细胞中显著的凋亡。PHA-767491直接抵消了5-FU诱导的Chk1磷酸化，并减少了抗凋亡蛋白myeloid leukemia cell line的表达[2]。PHA-767491（0-10μM）以时间和剂量依赖的方式减少了U87-MG和U251-MG细胞的活性（IC50：约2.5μM）。 |
| 体内活性 | PHA-767491 降低了 Chk1 磷酸化，并在裸鼠 HCC 移植瘤组织切片中增加了原位细胞凋亡。 |
| 存储条件 | Powder: -20°C for 3 years | In solvent: -80°C for 1 year Shipping with blue ice/Shipping at ambient temperature. |
| 溶解度 | 10% DMSO+40% PEG300+5% Tween 80+45% Saline : 1 mg/mL (4 mM), Sonication is recommended. 10% DMSO+90% Saline : 1.04 mg/mL (4.17 mM), Solution. H2O : 25 mg/mL (100.12 mM), Sonication is recommended. DMSO : 10.42 mg/mL (41.73 mM), Sonication is recommended. |
| 关键字 | PHA-767491 Hydrochloride | PHA-767491 | PHA767491 | PHA 767491 | GSK-3β | GSK3 | Cdk9 | Cdk2 | Cdk1 | CDK | Cdc7 | CAY10572 Hydrochloride | CAY-10572 | CAY10572 | CAY 10572 Hydrochloride | CAY 10572 | Apoptosis |
| 相关产品 | Formamide | Urea | Dimethyl phthalate | Aceglutamide | Alginic acid | Cysteamine hydrochloride | Metronidazole | Sildenafil citrate | Citric Acid Triammonium | Stavudine | Tamoxifen | Ethyl linoleate |
| 相关库 | Inhibitor Library | Bioactive Compound Library | Anti-Cancer Active Compound Library | Bioactive Compounds Library Max | Kinase Inhibitor Library | Anti-Aging Compound Library | Membrane Protein-targeted Compound Library | Anti-Neurodegenerative Disease Compound Library | Immunology/Inflammation Compound Library | Drug Repurposing Compound Library | Anti-Cancer Clinical Compound Library | Anti-Cancer Drug Library |
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/毫升，或双抗--青霉素100单位/毫升，链霉素100微克/毫升。 五、植物血凝素（PHA） 非增殖期的细胞不能制备染色体，如人外周血淋巴细胞，但在离体培养过程中，在PHA的作用下，可被刺激转化为淋巴母细胞而进入有丝分裂。经实验测定其分裂高峰分别于培养后44—48小时和68—72小时。 PHA有粘多糖，蛋白质两种重要成分。粘多糖促使有丝分裂，蛋白质起凝集作用。PHA激活的细胞数随其浓度而增加，直至全部免疫活性细胞均被激活为止，但PHA浓度过高会引起
。经实验测定其分裂高峰分别于培养后44-48小时和68-72小时。PHA有粘多糖，蛋白质两种重要成分。粘多糖促使有丝分裂，蛋白质起凝集作用。PHA激活的细胞数随其浓度而增加，直至全部免疫活性细胞均被激活为止，但PHA浓度过高会引起凝集，一般采用4%浓度为好。
成分和比例： RPMI-1640 84ml 小牛血清 15ml PHA 3支 肝素钠 1ml 卡那霉素 终浓度为100单位/ml 以5% NaHCO3（无菌）或1N HCl调pH至7.2－7.4。 用刻度吸管将培养液分装入培养瓶（10ml/瓶），4℃备用。 2．采血：酒精消毒皮肤，肘静脉采血0.3—0.5ml，立刻将注射针直接穿过培养瓶的橡胶塞，向10ml培养基中注入30—40滴全血，轻摇匀后置37℃恒温箱培养。 3．培养：时间为68小时。培养期间，定期轻摇匀，使细胞充分接触培养
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化合物 PHA767491 HCl【942425-68-5】
￥164 - 4136
