计算溶液所需的质量、体积或浓度。
| 活性类型 | 活性值-log(M) | 作用机制 | 期刊 | 参考文献(PubMed IDs) |
|---|
有货
为什么选择此级别
Moligand™ 级 ，适用于对基线干扰要求严格的色谱和分析工作流程。
储存与运输
-80℃储存。特低温运输 。请查阅批次 COA 获取详细规格。
质量文档
SDS、COA、产品数据表及规格说明书均可下载。可通过批号查询获取批次 COA。
文献证明
在色谱分析、有机合成和交叉偶联反应领域已被 1 篇同行评审文献引用。
概述
Flavopiridol能与ATP竞争抑制CDK，对CDK1，CDK2，CDK4和CDK6的IC50为40 nM，同时对EGFR和PKA也有一定抑制性。A synthetic flavonoid derivative, potent inhibitor of CDKs.
Information
Flavopiridol (L86-8275, Alvocidib, NSC 649890, HMR-1275) competes with ATP to inhibit CDKs includingCDK1,CDK2,CDK4,CDK6, andCDK9with IC50 values in the 20-100 nM range. It is more selective for CDK1, 2, 4, 6, 9 versus CDK7. Flavopiridol is initially found
In vitro
Flavopiridol displays less activity against unrelated kinases such as MAP, PAK, PKC, and EGFR with IC50 of >14 μM. Flavopiridol significantly inhibits the colony growth of HCT116, A2780, PC3, and Mia PaCa-2 cells with IC50 of 13 nM, 15 nM, 10 nM and 36 nM, respecitively. Flavopiridol also potently inhibits the activity of Glycogen synthase kinase-3 (GSK-3) with an IC50 of 280 nm. Compared with other CDKs, Flavopiridol inhibits the activity of CDK7 less potently with IC50 of 875 nM. Flavopiridol (0.5 μM) inhibits both pSer807/811 Rb and pThr199 NPM, whereas mild changes are observed at pThr821 Rb. Flavopiridol also decreases the overall RNA polymerase II level, as well as the phosphorylation of RNA polymerase II on the CTD repeats at Ser2 Ser5. As a broad spectrum CDK inhibitor, Flavopiridol can inhibit cell cycle progression in either G1 or G2. Flavopiridol (0.3 μM) induces G1 arrest in either MCF-7 or MDA-MB-468 cells by inhibition of the CDK4 or CDK2 kinase activity. Flavopiridol exhibits potent cytotoxicity against a wide variety of tumor cell lines with IC50 values ranging form 16 nM for LNCAP to 130 nM for K562.
In vivo
Administration of Flavopiridol at 7.5 mg/kg for 7 days displays slight antitumor activity against P388 murine leukemia, resulting in %T/C value of 110, and active against the human A2780 ovarian carcinoma implanted sc in nude mice, producing 1.5 log cell kill (LCK). Flavopiridol treatment at 1-2.5 mg/kg for 10 days significantly suppresses collagen-induced arthritis in mice in a dose-dependent manner, by inhibiting synovial hyperplasia and joint destruction, whereas serum concentrations of anti-collagen type II (CII) Abs and proliferative responses to CII are maintained. In the p21-intact Hct116 xenografts in nude mice, administration of CPT-11 (100 mg/kg) followed by Flavopiridol (3 mg/kg) 7 and 16 hours later significantly inhibits tumor regression by 86% and 82%, respectively, displaying >2 fold inhibition compared with CPT-11 alone by 40 %. The combination produces ~30% complete response rate (CR) in contrast to CPT-11 alone where no CR is found.
Cell Data
cell lines：
Concentrations：Dissolved in DMSO, final concentrations ~10 μM
Incubation Time：72 hours
Powder Purity:≥98%
规格
英文别名
NSC 649890 HCl, HMR-1275, Alvocidib | 2-(2-chlorophenyl)-5,7-dihydroxy-8-((3S,4R)-3-hydroxy-1-methylpiperidin-4-yl)-4H-chromen-4-one
规格或纯度
Moligand™, 10mM in DMSO
英文名称
Flavopiridol (L86-8275)
生化机理
Flavopiridol（L86-8275、Alvocidib、NSC 649890、HMR-1275）与 ATP 竞争抑制 CDK，包括 CDK1、CDK2、CDK4、CDK6 和 CDK9，IC50 值在 20-100 nM 范围内。与 CDK7 相比，它对 CDK1、2、4、6 和 9 的选择性更高。最初发现黄酮哌啶醇能抑制表皮生长因子受体（EGFR）和 PKA。黄酮哌啶醇能诱导自噬和 ER 应激。黄酮哌啶醇可阻止 HIV-1 复制。1/2阶段。
储存条件
-80℃储存
运输条件
特低温运输
作用类型
抑制剂
作用机制
细胞周期蛋白依赖性激酶 7 抑制剂
名称和识别符
分子类型
小分子
Isomeric SMILES
CN1CC[C@@H]([C@@H](C1)O)C2=C(C=C(C3=C2OC(=CC3=O)C4=CC=CC=C4Cl)O)O
分子量
401.85
Reaxy-Rn
8448533
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=8448533&ln=
技术文档
高级数据
产品属性
| ALogP | 3.3 |
|---|
关联靶点（人）
CDK7
Tchem
细胞周期蛋白依赖性激酶 7(Cyclin-dependent kinase 7)
(3 活性数据)
ERCC2
Tchem
通用转录和DNA修复因子IIH解旋酶亚基XPD(General transcription and DNA repair factor IIH helicase subunit XPD)
(1 活性数据)
CDK9
Tchem
细胞周期蛋白依赖性激酶9(Cyclin-dependent kinase 9)
(10 活性数据)
CDKL5
Tchem
细胞周期蛋白依赖性激酶类 5(Cyclin-dependent kinase-like 5)
(1 活性数据)
CDK4
Tclin
细胞周期蛋白依赖性激酶4(Cyclin-dependent kinase 4)
(3 活性数据)
CDK17
Tchem
细胞周期蛋白依赖性激酶 17(Cyclin-dependent kinase 17)
(1 活性数据)
PYGM
Tchem
糖原磷酸化酶，肌肉形式(Glycogen phosphorylase, muscle form)
(1 活性数据)
CILK1
Tchem
丝氨酸/苏氨酸蛋白激酶 ICK(Serine/threonine-protein kinase ICK)
(1 活性数据)
MAK
Tchem
丝氨酸/苏氨酸蛋白激酶 MAK(Serine/threonine-protein kinase MAK)
(1 活性数据)
CAMKK1
Tchem
钙/钙调蛋白依赖性蛋白激酶激酶 1(Calcium/calmodulin-dependent protein kinase kinase 1)
(1 活性数据)
LARP7
Tchem
La相关蛋白7(La-related protein 7)
(1 活性数据)
化学和物理性质
溶解性
Solubility (25°C) In vitro Ethanol: 31.5 mg/mL (100.17 mM); DMSO: 22 mg/mL (69.96 mM); Water: Insoluble;
安全和危险性（GHS）
象形图
信号词
Warning
危险声明
H302: 吞食有害
预防措施声明
P501: 将内容物/容器处理到。。。
P264: 处理后要彻底洗手。
P270: 使用本产品时，请勿进食、饮水或吸烟。
P330: 漱口
P301+P317: 如果被吞咽：请寻求医疗帮助。
质检证书（CoA,COO,BSE/TSE 和分析图谱)
C of A & Other Certificates(BSE/TSE, COO):
输入批号以搜索分析图谱:
通过匹配包装上的批号来查找并下载产品的 COA，每批产品都进行了严格的验证，您可放心使用！
| 批号(Lot Number) | 证书类型 | 货号 |
|---|---|---|
 H2426075 |
分析证书 | F407926 |
技术文档和文章
此产品的引用文献
引用文献
| 1. Mengling Huang, Abrar Ahmed, Wei Wang, Xue Wang, Cui Ma, Haowei Jiang, Wei Li, Lili Jing. (2022) Negative Elongation Factor (NELF) Inhibits Premature Granulocytic Development in Zebrafish. INTERNATIONAL JOURNAL OF MOLECULAR SCIENCES, 23 (7): (3833). [PMID:35409193] [10.3390/ijms23073833] |
溶液计算器
产品仅提供给经过验证的企业、机构和合格的专业人员用于研发。不适用于人类、动物、诊断或治疗。
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危险品化学品经营许可证（带存储）