Flavopiridol (Alvocidib) HCl
别名: NSC 649890, L86-8275, HMR-1275, DSP-2033 中文名称：盐酸夫拉平度
Flavopiridol (Alvocidib) HCl与ATP竞争性抑制CDKs，作用于CDK1，CDK2，CDK4和CDK6，无细胞试验中IC50为~40 nM。作用于CDK1/2/4/6比作用于CDK7选择性高7.5倍。Flavopiridol最初被发现可抑制EGFR和PKA。Flavopiridol HCl 可诱导自噬和内质网应激反应。Flavopiridol HCl 可阻止HIV-1的复制。Phase 1/2。
Flavopiridol (Alvocidib) HCl Chemical Structure
CAS: 131740-09-5
产品质控
批次：
纯度：
99.44%
99.44
Flavopiridol (Alvocidib) HCl相关产品
相关信号通路图
细胞实验数据示例
| 细胞系 | 实验类型 | 给药浓度 | 孵育时间 | 活性描述 | 文献信息 |
|---|---|---|---|---|---|
| DR-U2OS-GFP | Reduction of homologous recombination in | 0.1 uM | 56 hrs | Reduction of homologous recombination in human DR-U2OS-GFP cells expressing I-SceI nuclease assessed as reduction of RAD51 level at 0.1 uM after 56 hrs by immunoblotting | 21417417 |
| KOPN8 | Induction of apoptosis in | 0.5 uM | 3 to 24 hrs | Induction of apoptosis in human KOPN8 cells assessed as upregulation of cleaved PARP level at 0.5 uM after 3 to 24 hrs by Western blot analysis | 29407975 |
| KOPN8 | Induction of apoptosis in | 0.5 uM | 1 hr | Induction of apoptosis in human KOPN8 cells assessed as upregulation of cleaved PARP level at 0.5 uM pre-treated with NAC for 1 hr and measured after 3 to 24 hrs by Western blot analysis | 29407975 |
| human A2780 cell line | Proliferation assay | 72 h | Antiproliferative effect against human A2780 cell line was determined in a whole cell 72 hr cytotoxicity assay, IC50=71 nM | 15027863 | |
| A2780 | Inhibition of cdk-mediated Rb phosphorylation at | 24 hrs | Inhibition of cdk-mediated Rb phosphorylation at thr821 in human A2780 cells after 24 hrs | 18469809 | |
| A2780 | Inhibition of cdk-mediated Rb phosphorylation at | 24 hrs | Inhibition of cdk-mediated Rb phosphorylation at ser807/811 in human A2780 cells after 24 hrs | 18469809 | |
| A2780 | Inhibition of cdk9-mediated RNA pol2 CTD phosphorylation at | 24 hrs | Inhibition of cdk9-mediated RNA pol2 CTD phosphorylation at ser2 in human A2780 cells after 24 hrs | 18469809 | |
| A2780 | Inhibition of cdk7-mediated RNA pol2 CTD phosphorylation at | 24 hrs | Inhibition of cdk7-mediated RNA pol2 CTD phosphorylation at ser5 in human A2780 cells after 24 hrs | 18469809 | |
| A2780 | Induction of apoptosis in | 24 hrs | Induction of apoptosis in human A2780 cells assessed as appearance of Mcl1 protein level after 24 hrs | 18469809 | |
| NCI60 | Antiproliferative activity against | 72 hrs | Antiproliferative activity against human NCI60 cells after 72 hrs by sulforhodamine B assay, GI50=0.0747μM | 21080703 | |
| NCI60 | Antiproliferative activity against | 72 hrs | Antiproliferative activity against human NCI60 cells assessed as lethal effect after 72 hrs by sulforhodamine B assay, LC50=0.904μM | 21080703 | |
| A2780 | Cytotoxicity against | 24 hrs | Cytotoxicity against human A2780 cells after 24 hrs by MTT assay, GI50=0.023μM | 23301767 | |
| MRC5 | Cytotoxicity against | 72 hrs | Cytotoxicity against human MRC5 cells after 72 hrs by MTT assay, GI50=0.028μM | 23301767 | |
| A2780 | Cytotoxicity against | 72 hrs | Cytotoxicity against human A2780 cells after 72 hrs by MTT assay, GI50=0.029μM | 23301767 | |
| A2780 | Cytotoxicity against | 48 hrs | Cytotoxicity against human A2780 cells after 48 hrs by MTT assay, GI50=0.031μM | 23301767 | |
| MRC5 | Cytotoxicity against | 48 hrs | Cytotoxicity against human MRC5 cells after 48 hrs by MTT assay, GI50=0.039μM | 23301767 | |
| MRC5 | Cytotoxicity against | 24 hrs | Cytotoxicity against human MRC5 cells after 24 hrs by MTT assay, GI50=0.049μM | 23301767 | |
| HMEC1 | Cytotoxicity against | 24 hrs | Cytotoxicity against human HMEC1 cells after 24 hrs by MTT assay, GI50=0.061μM | 23301767 | |
| HMEC1 | Cytotoxicity against | 48 hrs | Cytotoxicity against human HMEC1 cells after 48 hrs by MTT assay, GI50=0.062μM | 23301767 | |
| HMEC1 | Cytotoxicity against | 72 hrs | Cytotoxicity against human HMEC1 cells after 72 hrs by MTT assay, GI50=0.066μM | 23301767 | |
| A2780 | Inhibition of CDK9 in | 24 hrs | Inhibition of CDK9 in human A2780 cells assessed as reduction of RNAPII CTD phosphorylation at Ser2 at GI50 concentration after 24 hrs by Western blotting analysis | 23301767 | |
| A2780 | Cell cycle arrest in | 24 hrs | Cell cycle arrest in human A2780 cells assessed as accumulation at G2/M phase at less than GI50 after 24 hrs by flow cytometric analysis | 23301767 | |
| A2780 | Inhibition of CDK9 in | 24 hrs | Inhibition of CDK9 in human A2780 cells assessed as downregulation of MCL1 at GI50 to 5XGI50 concentration after 24 hrs by Western blotting analysis | 23301767 | |
| A2780 | Inhibition of CDK9 in | 24 hrs | Inhibition of CDK9 in human A2780 cells assessed as downregulation of HDM2 at GI50 to 5XGI50 concentration after 24 hrs by Western blotting analysis | 23301767 | |
| A2780 | Induction of apoptosis in | 24 hrs | Induction of apoptosis in human A2780 cells assessed as induction of PARP cleavage at GI50 to 5XGI50 concentration after 24 hrs by Western blotting analysis | 23301767 | |
| Sf9 | Inhibition of CDK2/cyclin E1 (unknown origin) expressed in | 15 mins | Inhibition of CDK2/cyclin E1 (unknown origin) expressed in Sf9 insect cells using UlightCFFKNIVTPRTPPPSQGK-amide substrate after 15 mins by autoradiography, IC50=0.13μM | 25914804 | |
| A549 | Antiproliferative activity against | 3 days | Antiproliferative activity against human A549 cells after 3 days by SRB method, GI50=0.14μM | 25914804 | |
| DU145 | Antiproliferative activity against | 3 days | Antiproliferative activity against human DU145 cells after 3 days by SRB method, GI50=0.15μM | 25914804 | |
| KB | Antiproliferative activity against | 3 days | Antiproliferative activity against human KB cells after 3 days by SRB method, GI50=0.16μM | 25914804 | |
| KBVIN | Antiproliferative activity against | 3 days | Antiproliferative activity against human KBVIN cells after 3 days by SRB method, GI50=0.18μM | 25914804 | |
| HCT116 | Antiproliferative activity against | 72 hrs | Antiproliferative activity against human HCT116 cells after 72 hrs by Celltiter-Glo reagent based assay in presence of 10% fetal bovine serum, EC50=0.034μM | 26985305 | |
| HCT116 | Antiproliferative activity against | 72 hrs | Antiproliferative activity against human HCT116 cells after 72 hrs by Celltiter-Glo reagent based assay in presence of 0.625% fetal bovine serum, EC50=0.059μM | 26985305 | |
| Sf9 | Inhibition of human | 10 mins | Inhibition of human His6-tagged CDK9/cyclin T1 expressed in baculovirus infected sf9 cells using GST-CTD as substrate after 10 mins in presence of [gamma-32P]ATP by SDS-PAGE analysis, IC50=0.0025μM | 27171036 | |
| HeLa | Cytotoxicity against | 72 hrs | Cytotoxicity against human HeLa cells assessed as decrease in cell viability after 72 hrs by MTT assay, CC50=0.12μM | 27171036 | |
| HCT116 | Antiproliferative activity against | 72 hrs | Antiproliferative activity against human HCT116 cells assessed as growth inhibition in presence of 0.625% FBS after 72 hrs, EC50=0.059μM | 27326333 | |
| HepG2 | Antiproliferative activity against | 72 hrs | Antiproliferative activity against human HepG2 cells after 72 hrs by CelTiter-Glo assay, EC50=0.1464μM | 29407975 | |
| KOPN8 | Antiproliferative activity against | 72 hrs | Antiproliferative activity against human KOPN8 cells after 72 hrs by CelTiter-Glo assay, EC50=0.1926μM | 29407975 | |
| SEM | Antiproliferative activity against | 72 hrs | Antiproliferative activity against human SEM cells after 72 hrs by CelTiter-Glo assay, EC50=0.2043μM | 29407975 | |
| UOCB1 | Antiproliferative activity against | 72 hrs | Antiproliferative activity against human UOCB1 cells after 72 hrs by CelTiter-Glo assay, EC50=0.2084μM | 29407975 | |
| insect cells | Inhibition of human | 2.5 mins | Inhibition of human CDK4/cyclin D1 expressed in insect cells after 2.5 mins by liquid scintillation counting analysis, IC50=0.02μM | 30733087 | |
| Caco-2 | Toxicity assay | 48 hrs | Toxicity against Caco-2 cells determined at 48 hours by intracellular ATP concentration using the CellTiter-Glo Luminescent Cell Viability Assay, CC50=0.06μM | ChEMBL | |
| Caco-2 | Function assay | 48 hrs | Determination of IC50 values for inhibition of SARS-CoV-2 induced cytotoxicity of Caco-2 cells after 48 hours by high content imaging, IC50=0.59μM | ChEMBL | |
| LNCaP human prostate carcinoma cell | Proliferation assay | Inhibition of LNCaP human prostate carcinoma cell proliferation | 12190313 | ||
| HCT116/VP35 human colon carcinoma cell | Proliferation assay | Inhibition of HCT116/VP35 human colon carcinoma cell proliferation, IC50=17 nM | 12190313 | ||
| HCT116 human colon carcinoma cell | Proliferation assay | Inhibition of HCT116 human colon carcinoma cell proliferation, IC50=18 nM | 12190313 | ||
| HCT116/VM46 human colon carcinoma cell | Proliferation assay | Inhibition of HCT116/VM46 human colon carcinoma cell proliferation, IC50=21 nM | 12190313 | ||
| A2780/DDP-R human ovarian carcinoma cell | Proliferation assay | Inhibition of A2780/DDP-R human ovarian carcinoma cell proliferation, IC50=38 nM | 12190313 | ||
| ABAE human fibroblast cell | Proliferation assay | Inhibition of ABAE human fibroblast cell proliferation, IC50=45 nM | 12190313 | ||
| HL60 human leukemia cell | Proliferation assay | Inhibition of HL60 human leukemia cell proliferation, IC50=46 nM | 12190313 | ||
| Hs 27 human fibroblast cell | Proliferation assay | Inhibition of Hs 27 human fibroblast cell proliferation, IC50=51 nM | 12190313 | ||
| CCRF-CEM human leukemia cell | Proliferation assay | Inhibition of CCRF-CEM human leukemia cell proliferation, IC50=52 nM | 12190313 | ||
| OVCAR-3 human ovarian carcinoma cell | Proliferation assay | Inhibition of OVCAR-3 human ovarian carcinoma cell proliferation, IC50=54 nM | 12190313 | ||
| A2780/DDP-S human ovarian carcinoma cell | Proliferation assay | Inhibition of A2780/DDP-S human ovarian carcinoma cell proliferation, IC50=56 nM | 12190313 | ||
| A2780/TAX-S human ovarian carcinoma cell | Proliferation assay | Inhibition of A2780/TAX-S human ovarian carcinoma cell proliferation, IC50=65 nM | 12190313 | ||
| LS174T human colon carcinoma cell | Proliferation assay | Inhibition of LS174T human colon carcinoma cell proliferation, IC50=65 nM | 12190313 | ||
| MCF-7 human breast carcinoma cell | Proliferation assay | Inhibition of MCF-7 human breast carcinoma cell proliferation, IC50=66 nM | 12190313 | ||
| PC3 human prostate carcinoma cell | Proliferation assay | Inhibition of PC3 human prostate carcinoma cell proliferation, IC50=66 nM | 12190313 | ||
| MLF mouse lung fibroblast cell | Proliferation assay | Inhibition of MLF mouse lung fibroblast cell proliferation, IC50=72 nM | 12190313 | ||
| LX-1 human lung carcinoma | Proliferation assay | Inhibition of LX-1 human lung carcinoma proliferation, IC50=75 nM | 12190313 | ||
| A431 human squamous cell | Proliferation assay | Inhibition of A431 human squamous cell carcinoma cell proliferation, IC50=75 nM | 12190313 | ||
| SKBR-3 human breast carcinoma cell | Proliferation assay | Inhibition of SKBR-3 human breast carcinoma cell proliferation, IC50=77 nM | 12190313 | ||
| A2780/TAX-R human ovarian carcinoma cell | Proliferation assay | Inhibition of A2780/TAX-R human ovarian carcinoma cell proliferation, IC50=78 nM | 12190313 | ||
| M109 mouse lung carcinoma cell | Proliferation assay | Inhibition of M109 mouse lung carcinoma cell proliferation, IC50=80 nM | 12190313 | ||
| CACO-2 human colon carcinoma cell | Proliferation assay | Inhibition of CACO-2 human colon carcinoma cell proliferation, IC50=86 nM | 12190313 | ||
| A549 human lung carcinoma cell | Proliferation assay | Inhibition of A549 human lung carcinoma cell proliferation, IC50=96 nM | 12190313 | ||
| MIP human colon carcinoma cell | Function assay | Inhibition of MIP human colon carcinoma cell line, IC50=0.12 μM | 12190313 | ||
| K562 human leukemia cell | Proliferation assay | Inhibition of K562 human leukemia cell proliferation, IC50=0.13 μM | 12190313 | ||
| PC3 cell | Function assay | Inhibition of PC3 cell clonogenic assay, IC50=10 μM | 11063609 | ||
| HCT116 cell | Function assay | Inhibition of HCT116 cell clonogenic assay, IC50=13 μM | 11063609 | ||
| A2780 cell | Function assay | Inhibition of A2780 cell clonogenic assay， IC50=15 μM | 11063609 | ||
| Mia PaCa-2 cell | Function assay | Inhibition of Mia PaCa-2 cell clonogenic assay, IC50=36 μM | 11063609 | ||
| MCF-7 tumor cell | Proliferation assay | Inhibition of MCF-7 tumor cell proliferation | 10843211 | ||
| human ovarian (A2780) cancer cell | Cytotoxic assay | Cytotoxic effect on human ovarian (A2780) cancer cell line, IC50=71 nM | 15125971 | ||
| ID8 | Antiproliferative activity against | Antiproliferative activity against ID8 cells, IC50=0.007μM | 17123821 | ||
| MCF7 | Antiproliferative activity against | Antiproliferative activity against MCF7 cells, IC50=0.026μM | 17123821 | ||
| Sf9 | Inhibition of recombinant cyclin A/CDK2 expressed in | Inhibition of recombinant cyclin A/CDK2 expressed in Sf9 cells, IC50=0.012μM | 17904366 | ||
| A2780 | Inhibition of cdk-mediated NPM phosphorylation at | Inhibition of cdk-mediated NPM phosphorylation at thr199 in human A2780 cells | 18469809 | ||
| MT4 | Antiviral activity against | Antiviral activity against Human immunodeficiency virus 1 NL 4-3 infected in MT4 cells measured on day 4 post infection by p24 assay, EC50=0.015μM | 25914804 | ||
| MT4 | Cytotoxicity against | Cytotoxicity against human MT4 cells, IC50=0.067μM | 25914804 | ||
| Sf21 | Inhibition of recombinant human | Inhibition of recombinant human full length C-terminal His6-tagged CDK9/cyclin T1 expressed in baculovirus infected Sf21 insect cells using PDKtide as substrate, IC50=0.011μM | 27171036 | ||
| Sf21 | Inhibition of full length human | Inhibition of full length human N-terminal His6-tagged CDK6/N-terminal GST-tagged cyclin D3 expressed in sf21 cells using histone H1 substrate, IC50=0.395μM | 27171036 | ||
| Sf21 | Inhibition of recombinant human | Inhibition of recombinant human full length C-terminal His6-tagged CDK7/cyclin H/N-terminal GST-tagged MAT1 expressed in baculovirus infected Sf21 insect cells using cdk7 substrate peptide, IC50=0.514μM | 27171036 | ||
| TC32 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for TC32 cells | 29435139 | ||
| DAOY | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for DAOY cells | 29435139 | ||
| SJ-GBM2 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SJ-GBM2 cells | 29435139 | ||
| A673 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for A673 cells | 29435139 | ||
| SK-N-MC | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for SK-N-MC cells | 29435139 | ||
| BT-37 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-37 cells | 29435139 | ||
| NB-EBc1 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for NB-EBc1 cells | 29435139 | ||
| BT-12 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for BT-12 cells | 29435139 | ||
| OHS-50 | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for OHS-50 cells | 29435139 | ||
| RD | qHTS assay | qHTS of pediatric cancer cell lines to identify multiple opportunities for drug repurposing: Primary screen for RD cells | 29435139 | ||
| 点击查看更多细胞系数据 | |||||
生物活性
| 产品描述 | Flavopiridol (Alvocidib) HCl与ATP竞争性抑制CDKs，作用于CDK1，CDK2，CDK4和CDK6，无细胞试验中IC50为~40 nM。作用于CDK1/2/4/6比作用于CDK7选择性高7.5倍。Flavopiridol最初被发现可抑制EGFR和PKA。Flavopiridol HCl 可诱导自噬和内质网应激反应。Flavopiridol HCl 可阻止HIV-1的复制。Phase 1/2。 | ||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | Flavopiridol最初被发现抑制表皮生长因子受体和蛋白激酶A的活性，IC50分别是21 μM and 122 μM。Flavopiridol是后来证明能够抑制细胞的增殖，在多种生理相关浓度(IC50 = 66 nM)，在肿瘤细胞系美国国家癌症研究所开发治疗计划中的60种人癌细胞系测试过。[1] 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。[2] Flavopiridol短时处理（约12小时）诱导造血细胞系的细胞凋亡，包括SUDHL4，SUDHL6（B细胞系），Jurkat和MOLT4（T细胞系）和HL60（髓细胞系）。[3] 在克隆形成实验中，Flavopiridol在23人肿瘤模型中表现高细胞毒性，平均IC70是8 ng/mL。[4] 最近的一项研究表明Flavopiridol诱导人脑胶质瘤T98G细胞系的AKT-Ser473磷酸化。[5] | |||
|---|---|---|---|---|
| 激酶实验 | 重组CDKs激酶反应 | |||
| CDKs的活性按如下方式在酶标板中，40 μg GST-R b与不同量Flavopiridol和未标记的ATP混合。反应然后通过加入S100的馏分从表达重组人CDK的昆虫细胞中得到的硫酸铵沉淀部分的开始。最终反应条件为10 mM MgCl2, 50 mM Tris-HCl (pH 7.5)和1 mM DTT。ATP的终浓度做相应的调整。放射性标记的ATP作为磷酸供体。该反应在30℃下加入酶后进行2.5分钟，然后加入EDTA终止。GST-Rb用谷胱甘肽 - 琼脂糖标记和掺入的放射性通过液体闪烁计数测定。 | ||||
| 细胞实验 | 细胞系 | SUDHL4, SUDHL6, Jurkat, MOLT4和HL60细胞 | ||
| 浓度 | 0, 100 500, 5000 nM | |||
| 孵育时间 | 14小时 | |||
| 方法 | 在密度为1 × 106 cells/mL的细胞中不同时间加入不同浓度的Flavopiridol。提取DNA。细胞用冷的磷酸盐缓冲盐水（PBS）洗涤一次并在4℃条件下在3 mL裂解缓冲液（5 mM Tris-HCL [pH 7.5]; 20 mM EDTA; 0.5% Triton X-100）中裂解15分钟。将细胞裂解物的染色质（以26,000 g，4℃，20分钟）离心分离。用苯酚，酚氯仿（1:1）和氯仿从上清液提取提取小的DNA片段。核酸在-20℃中在0.5M氯化钠，90％的乙醇沉淀过夜。RNA由牛RNAaseA消化（60μg/mL）。连续反萃取和沉淀后，DNA溶解在10mM Tris-HCl（pH值7.5），1mM的EDTA，0.5％十二烷基硫酸钠（SDS），而后在1.6％琼脂糖凝胶上电泳。 | |||
| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | CDK2 / CDK4 / Cyclin A / p21 / p27 / Rb p-ERK / ERK / p-p38 / p-4EBP1 / 4EBP1 / p-S6 p-RNAPII / p-eIF4E / Mnk1 Cleaved caspase-8 / Cleaved caspase-9 / Cleaved caspase-3 |
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24572052 | |
| Growth inhibition assay | Cell viability |
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31193061 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | 以最大耐受剂量10 mg/kg/day在第1-4天及7-11天给药，Flavopiridol表现为PRXF1337肿瘤消退和PRXF1369肿瘤停滞为期4周。[4] 用7.5 mg/kg Flavopiridol静脉内（IV）或腹膜内连续注射5天后，12分之11的皮下（SC）人HL-60 移植鼠的肿瘤完全消退，Flavopiridol治疗一疗程后移植鼠数月无病。在SUDHL-4皮下注射淋巴瘤模型鼠中静脉注射Flavopiridol （7.5 mg/kg），模型鼠的肿瘤大部分（8分之2）或者完全（8分之4）消退，两只剩余动物无病超过60天。整体生长延迟73.2％。[6] | |
|---|---|---|
| 动物实验 | Animal Models | 人类前列腺癌异种移植，PRXFI337和PRXFI369，皮下种植在裸鼠中 |
| Dosages | 10 mg/kg/d | |
| Administration | 在days 1-4 and 7-11口服。 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT00112723 | Terminated | Adult Lymphocyte Depletion Hodgkin Lymphoma|Adult Lymphocyte Predominant Hodgkin Lymphoma|Adult Mixed Cellularity Hodgkin Lymphoma|Adult Nodular Sclerosis Hodgkin Lymphoma|Anaplastic Large Cell Lymphoma|Angioimmunoblastic T-cell Lymphoma|Extranodal Marginal Zone B-cell Lymphoma of Mucosa-associated Lymphoid Tissue|Nodal Marginal Zone B-cell Lymphoma|Recurrent Adult Diffuse Large Cell Lymphoma|Recurrent Adult Diffuse Mixed Cell Lymphoma|Recurrent Adult Diffuse Small Cleaved Cell Lymphoma|Recurrent Adult Grade III Lymphomatoid Granulomatosis|Recurrent Adult Hodgkin Lymphoma|Recurrent Adult T-cell Leukemia/Lymphoma|Recurrent Cutaneous T-cell Non-Hodgkin Lymphoma|Recurrent Grade 1 Follicular Lymphoma|Recurrent Grade 2 Follicular Lymphoma|Recurrent Grade 3 Follicular Lymphoma|Recurrent Mantle Cell Lymphoma|Recurrent Marginal Zone Lymphoma|Recurrent Mycosis Fungoides/Sezary Syndrome|Recurrent Small Lymphocytic Lymphoma|Refractory Multiple Myeloma|Splenic Marginal Zone Lymphoma|Stage I Multiple Myeloma|Stage II Multiple Myeloma|Stage III Multiple Myeloma|Waldenström Macroglobulinemia |
National Cancer Institute (NCI) |
December 2005 | Phase 1|Phase 2 |
| NCT00098371 | Terminated | B-cell Chronic Lymphocytic Leukemia|Prolymphocytic Leukemia|Refractory Chronic Lymphocytic Leukemia |
National Cancer Institute (NCI) |
April 2005 | Phase 2 |
| NCT00101231 | Terminated | Adult Acute Basophilic Leukemia|Adult Acute Eosinophilic Leukemia|Adult Acute Megakaryoblastic Leukemia (M7)|Adult Acute Minimally Differentiated Myeloid Leukemia (M0)|Adult Acute Monoblastic Leukemia (M5a)|Adult Acute Monocytic Leukemia (M5b)|Adult Acute Myeloblastic Leukemia With Maturation (M2)|Adult Acute Myeloblastic Leukemia Without Maturation (M1)|Adult Acute Myeloid Leukemia With 11q23 (MLL) Abnormalities|Adult Acute Myeloid Leukemia With Inv(16)(p13;q22)|Adult Acute Myeloid Leukemia With t(16;16)(p13;q22)|Adult Acute Myeloid Leukemia With t(8;21)(q22;q22)|Adult Acute Myelomonocytic Leukemia (M4)|Adult Erythroleukemia (M6a)|Adult Pure Erythroid Leukemia (M6b)|Blastic Phase Chronic Myelogenous Leukemia|Recurrent Adult Acute Lymphoblastic Leukemia|Recurrent Adult Acute Myeloid Leukemia|Relapsing Chronic Myelogenous Leukemia |
National Cancer Institute (NCI) |
October 2004 | Phase 1 |
| NCT00058240 | Completed | B-cell Chronic Lymphocytic Leukemia|Recurrent Small Lymphocytic Lymphoma|Refractory Chronic Lymphocytic Leukemia|Waldenström Macroglobulinemia |
National Cancer Institute (NCI) |
April 2003 | Phase 1|Phase 2 |
化学信息&溶解度
| 分子量 | 438.3 | 分子式 | C21H20ClNO5.HCl |
| CAS号 | 131740-09-5 | SDF | Download Flavopiridol (Alvocidib) HCl SDF |
| Smiles | CN1CCC(C(C1)O)C2=C(C=C(C3=C2OC(=CC3=O)C4=CC=CC=C4Cl)O)O.Cl | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 88 mg/mL ( (200.77 mM) ；DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : 37 mg/mL (84.41 mM) Ethanol : Insoluble |
摩尔浓度计算器 |
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体内溶解度 现配现用，请按从左到右的顺序依次添加，澄清后再加入下一溶剂 |
动物体内配方计算器 | ||||
实验计算
动物体内配方计算器（澄清溶液）
第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量）
mg/kg
g
μL
只
第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系Selleck为您提供正确的澄清溶液配方）
% DMSO
%
% Tween 80
% ddH2O
%DMSO
%
计算结果：
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于μL DMSO溶液（母液浓度mg/mL，注：如该浓度超过该批次药物DMSO溶解度，请先联系Selleck）；
体内配方配制方法：取μL DMSO母液，加入μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入μL ddH2O，混匀澄清。
体内配方配制方法：取μL DMSO母液，加入μL Corn oil，混匀澄清。
注意：1. 首先保证母液是澄清的；
2.一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
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