Flavopiridol (L86-8275) HCl

CAS: 131740-09-5 货号: F407830 分子式: C21H20ClNO5.HCl 分子量: 438.3 EC号: 634-346-4
有货
级别和纯度: 10mM in DMSO
别名
盐酸黄酮吡啶醇(L86-8275)
储存条件
-80℃储存
运输条件
特低温运输
★
规格
库存
价格
数量
1ml
F407830-1ml
现货 Stock Image
¥501.90
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为什么选择此级别

,适用于对基线干扰要求严格的色谱和分析工作流程。

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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。

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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。

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文献证明

在色谱分析、有机合成和交叉偶联反应领域已被 0 篇同行评审文献引用。

概述


Information

Flavopiridol HCl (L86-8275, NSC 649890, Alvocidib, HMR-1275, DSP-2033) competes with ATP to inhibit CDKs includingCDK1,CDK2,CDK4andCDK6withIC50of ~ 40 nM in cell-free assays. It is 7.5-fold more selective for CDK1/2/4/6 than CDK7. Flavopiridol is initiall
In vitro

Flavopiridol is initially found to inhibit the epidermal growth factor receptor and protein kinase A (IC50 = 21 and 122 μM). Flavopiridol is later shown to inhibit cell proliferation, at more physiologically relevant concentrations (IC50 = 66 nM) when Flavopiridol is tested in the National Cancer Institute Development Therapeutics Program panel of 60 human tumor cell lines. Flavopiridol induces G1 arrest with inhibition of CDK2 and CDK4 in human breast carcinoma cells in a time and concentration dependent manner. Short time treatment of Flavopiridol (~12 hours) induce apoptosis in hematopoietic cell lines including SUDHL4, SUDHL6 (B-cell lines), Jurkat and MOLT4 (T-cell lines ), and HL60 (myeloid). In the clonogenic assay, Flavopiridol functions as a highly potent cytotoxic compound with a mean IC70 with 8 ng/mL in 23 human tumor models. A recent study shows Flavopiridol treatment induces a substantial AKT-Ser473 phosphorylation in human glioblastoma T98G cell line.

In vivo

At the maximal tolerated dose of 10 mg/kg/day administered p.o. on days 1-4 and 7-11, Flavopiridol effects tumor regression in PRXF1337 and tumor stasis lasting for 4 weeks in PRXF1369. After treatment with 7.5 mg/kg Flavopiridol bolus intravenous (IV) or intraperitoneal on each of 5 consecutive days, 11 out of 12 advanced stage subcutaneous (s.c.) human HL-60 xenografts undergo complete regressions, and animals remain disease-free several months after one course of Flavopiridol treatment. SUDHL-4 s.c. lymphomas treated with flavopiridol at 7.5 mg/kg bolus IV for 5 days undergo either major (two out of eight mice) or complete (four out of eight mice) regression, with two animals remaining disease-free for more than 60 days. The overall growth delay is 73.2%. Daily IV or IP administration of flavopiridol resultsin peak plasma levels of about 7 µM, followed by a progressive decline to approximately 100 nM in 8 hours.
Cell Data

cell lines:INS-1E

Concentrations:0, 100 500, 5000 nM

Incubation Time:14 hours

Powder Purity:≥99%

规格

别名
盐酸黄酮吡啶醇(L86-8275)
英文别名
NSC 649890, Alvocidib, HMR-1275, DSP-2033 | 2-(2-chlorophenyl)-5,7-dihydroxy-8-((3S,4R)-3-hydroxy-1-methylpiperidin-4-yl)-4H-chromen-4-one hydrochloride
规格或纯度
10mM in DMSO
英文名称
Flavopiridol (L86-8275) HCl
生化机理
Flavopiridol HCl(L86-8275、NSC 649890、Alvocidib、HMR-1275、DSP-2033)与 ATP 竞争抑制 CDK(包括 CDK1、CDK2、CDK4 和 CDK6),在无细胞检测中的 IC50 为 40 nM。它对 CDK1/2/4/6 的选择性是 CDK7 的 7.5 倍。最初发现黄酮哌啶醇能抑制表皮生长因子受体和 PKA。盐酸黄连素可诱导自噬和 ER 应激。盐酸黄酮哌啶醇能阻止 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
名称和识别符
EC号
634-346-4
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.Cl
分子量
438.3
Reaxy-Rn
25500302
Reaxys-RN link address
https://www.reaxys.com/reaxys/secured/hopinto.do?context=S&query=IDE.XRN=25500302&ln=

技术文档

📋 安全数据表 (SDS)

全面的危险、操作、储存及法规合规文件。

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🔬 规格说明书

该级别的完整质量属性和验收标准。

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高级数据

化学和物理性质
溶解性
Solubility (25°C) In vitro DMSO: 100 mg/mL (316.1 mM);    
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):
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常见问题

本产品应如何储存?
请于?80 °C条件下保存。需超低温保存以维持规定的有效期。
本产品的 CAS 号、分子式和分子量是多少?
本产品的 CAS 号为 131740-09-5,分子式为 C21H21Cl2NO5,分子量为 438.3 g/mol。
本产品如何运输?
本产品采用干冰配冷袋冷冻运输。收货后请立即拆包,并按上述储存条件保存;处理干冰时请戴隔热手套并保持通风。