| 货号 (SKU) | 包装规格 | 是否现货 | 价格 | 数量 |
|---|---|---|---|---|
| F407926-1ml |
1ml |
现货  |
|
| 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。 |
| 储存温度 | -80℃储存 |
| 运输条件 | 超低温冰袋运输 |
| 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 |
| 产品介绍 |
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 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 lines： Concentrations：Dissolved in DMSO, final concentrations ~10 μM Incubation Time：72 hours Powder Purity:≥98% |
| ALogP | 3.3 |
|---|
| 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= |
| 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; |
|---|
| 象形图 | GHS07 |
|---|---|
| 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。 |
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