Flavopiridol (Alvocidib)
别名: NSC 649890, HMR-1275, L86-8275 中文名称：夫拉平度
Flavopiridol (Alvocidib)与ATP竞争性抑制CDKs，包括CDK1、CDK2、CDK4、CDK6和CDK9的IC50范围为20-100 nM。作用于CDK1、2、4、6、9比作用于CDK7更具有选择性。Flavopiridol最初被发现能抑制EGFR和PKA。Flavopiridol可诱导自噬和内质网应激反应。Flavopiridol可阻滞HIV-1的复制。Phase 1/2。
Flavopiridol (Alvocidib) Chemical Structure
CAS: 146426-40-6
客户使用Selleck的Flavopiridol (Alvocidib)发表文献119篇
产品质控
批次：
纯度：
99.92%
99.92
Flavopiridol (Alvocidib)相关产品
相关信号通路图
CDK抑制剂选择性比较
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 |
|---|---|---|---|---|---|
| A2780 | Function assay | 330 nM | 24 hr | Percentage A2780 cells in sb-G1 after 24 hr r at 330 nM (IC50), Cell cycle = 0.001 μM. | 12190313 |
| A2780 | Apoptosis assay | 330 nM | 24 hr | Apoptotic A2780 cells after 24 hr r at 330 nM (IC50), Cell cycle = 0.001 μM. | 12190313 |
| A2780 | Function assay | 2980 nM | 24 hr | Percentage A2780 cells in sub-G1 after 24 hr r at 2980 nM (IC90), Cell cycle = 0.002 μM. | 12190313 |
| A2780 | Apoptosis assay | 2980 nM | 24 hr | Apoptotic A2780 cells after 24 hr r at 2980 nM (IC90), Cell cycle = 0.009 μM. | 12190313 |
| A2780 | Function assay | 2980 nM | 24 hr | Percentage A2780 cells in S-phase after 24 hr r at 2980 nM (IC90), Cell cycle = 0.012 μM. | 12190313 |
| A2780 | Function assay | 330 nM | 24 hr | Percentage A2780 cells in S-phase after 24 hr r at 330 nM (IC50), Cell cycle = 0.016 μM. | 12190313 |
| A2780 | Function assay | 330 nM | 24 hr | Percentage A2780 cells in G2/M after 24 hr r at 330 nM (IC50), Cell cycle = 0.023 μM. | 12190313 |
| A2780 | Function assay | 2980 nM | 24 hr | Percentage A2780 cells in G2/M after 24 hr r at 2980 nM (IC90), Cell cycle = 0.025 μM. | 12190313 |
| A2780 | Function assay | 330 nM | 24 hr | Percentage A2780 cells in G1 after 24 hr r at 330 nM (IC50), Cell cycle = 0.06 μM. | 12190313 |
| A2780 | Function assay | 2980 nM | 24 hr | Percentage A2780 cells in G1 after 24 hr r at 2980 nM (IC90), Cell cycle = 0.061 μM. | 12190313 |
| DR-U2OS-GFP | Function assay | 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 | Apoptosis assay | 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 | Apoptosis assay | 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 | |
| human A2780 cells | Function assay | 24 h | Inhibition of cdk-mediated Rb phosphorylation at thr821 in human A2780 cells after 24 hrs | 18469809 | |
| human NCI60 cells | Proliferation assay | 72 h | Antiproliferative activity against human NCI60 cells after 72 hrs by sulforhodamine B assay, GI50=74.7 nM | 21080703 | |
| human NCI60 cells | Proliferation assay | 72 h | Antiproliferative activity against human NCI60 cells assessed as lethal effect after 72 hrs by sulforhodamine B assay, LC50=0.904 μM | 21080703 | |
| human A2780 cells | Cytotoxic assay | 24 h | Cytotoxicity against human A2780 cells after 24 hrs by MTT assay, GI50=23 nM | 23301767 | |
| human MRC5 cells | Cytotoxic assay | 72 h | Cytotoxicity against human MRC5 cells after 72 hrs by MTT assay, GI50=28 nM | 23301767 | |
| human A2780 cells | Cytotoxic assay | 72 h | Cytotoxicity against human A2780 cells after 72 hrs by MTT assay, GI50=29 nM | 23301767 | |
| human A2780 cells | Cytotoxic assay | 48 h | Cytotoxicity against human A2780 cells after 48 hrs by MTT assay, GI50=31 nM | 23301767 | |
| human MRC5 cells | Cytotoxic assay | 48 h | Cytotoxicity against human MRC5 cells after 48 hrs by MTT assay, GI50=39 nM | 23301767 | |
| human MRC5 cells | Cytotoxic assay | 24 h | Cytotoxicity against human MRC5 cells after 24 hrs by MTT assay, GI50=49 nM | 23301767 | |
| human HMEC1 cells | Cytotoxic assay | 24 h | Cytotoxicity against human HMEC1 cells after 24 hrs by MTT assay, GI50=61 nM | 23301767 | |
| human HMEC1 cells | Cytotoxic assay | 48 h | Cytotoxicity against human HMEC1 cells after 48 hrs by MTT assay, GI50=62 nM | 23301767 | |
| human HMEC1 cells | Cytotoxic assay | 72 h | Cytotoxicity against human HMEC1 cells after 72 hrs by MTT assay, GI50=66 nM | 23301767 | |
| A2780 | Function assay | 24 hrs | Inhibition of cdk-mediated Rb phosphorylation at ser807/811 in human A2780 cells after 24 hrs | 18469809 | |
| A2780 | Function assay | 24 hrs | Inhibition of cdk9-mediated RNA pol2 CTD phosphorylation at ser2 in human A2780 cells after 24 hrs | 18469809 | |
| A2780 | Function assay | 24 hrs | Inhibition of cdk7-mediated RNA pol2 CTD phosphorylation at ser5 in human A2780 cells after 24 hrs | 18469809 | |
| A2780 | Apoptosis assay | 24 hrs | Induction of apoptosis in human A2780 cells assessed as appearance of Mcl1 protein level after 24 hrs | 18469809 | |
| A2780 | Function assay | 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 assay | 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 | Function assay | 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 | Apoptosis assay | 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 | |
| A2780 | Function assay | 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 | |
| Sf9 | Function assay | 15 mins | Inhibition of CDK2/cyclin E1 (unknown origin) expressed in Sf9 insect cells using UlightCFFKNIVTPRTPPPSQGK-amide substrate after 15 mins by autoradiography, IC50 = 0.13 μM. | 25914804 | |
| A549 | Antiproliferative assay | 3 days | Antiproliferative activity against human A549 cells after 3 days by SRB method, GI50 = 0.14 μM. | 25914804 | |
| DU145 | Antiproliferative assay | 3 days | Antiproliferative activity against human DU145 cells after 3 days by SRB method, GI50 = 0.15 μM. | 25914804 | |
| KB | Antiproliferative assay | 3 days | Antiproliferative activity against human KB cells after 3 days by SRB method, GI50 = 0.16 μM. | 25914804 | |
| KBVIN | Antiproliferative assay | 3 days | Antiproliferative activity against human KBVIN cells after 3 days by SRB method, GI50 = 0.18 μM. | 25914804 | |
| HCT116 | Antiproliferative assay | 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 = 0.034 μM. | 26985305 | |
| HCT116 | Antiproliferative assay | 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 = 0.059 μM. | 26985305 | |
| Sf9 | Function assay | 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 = 0.0025 μM. | 27171036 | |
| HeLa | Cytotoxicity assay | 72 hrs | Cytotoxicity against human HeLa cells assessed as decrease in cell viability after 72 hrs by MTT assay, CC50 = 0.12 μM. | 27171036 | |
| HepG2 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human HepG2 cells after 72 hrs by CelTiter-Glo assay, EC50 = 0.1464 μM. | 29407975 | |
| KOPN8 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human KOPN8 cells after 72 hrs by CelTiter-Glo assay, EC50 = 0.1926 μM. | 29407975 | |
| SEM | Antiproliferative assay | 72 hrs | Antiproliferative activity against human SEM cells after 72 hrs by CelTiter-Glo assay, EC50 = 0.2043 μM. | 29407975 | |
| UOCB1 | Antiproliferative assay | 72 hrs | Antiproliferative activity against human UOCB1 cells after 72 hrs by CelTiter-Glo assay, EC50 = 0.2084 μM. | 29407975 | |
| MIP human colon carcinoma cell | Function assay | Inhibition of MIP human colon carcinoma cell line, IC50=0.12 μM | 12190313 | ||
| A549 human lung carcinoma cell | Proliferation assay | Inhibition of A549 human lung carcinoma cell proliferation, IC50=96 nM | 12190313 | ||
| CACO-2 human colon carcinoma cell | Proliferation assay | Inhibition of CACO-2 human colon carcinoma cell proliferation, IC50=86 nM | 12190313 | ||
| M109 mouse lung carcinoma cell | Proliferation assay | Inhibition of M109 mouse lung carcinoma cell proliferation, IC50=80 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 | ||
| SKBR-3 human breast carcinoma cell | Proliferation assay | Inhibition of SKBR-3 human breast carcinoma cell proliferation, IC50=77 nM | 12190313 | ||
| A431 human squamous cell | Proliferation assay | Inhibition of A431 human squamous cell carcinoma cell proliferation, IC50=75 nM | 12190313 | ||
| LX-1 human lung carcinoma | Proliferation assay | Inhibition of LX-1 human lung carcinoma proliferation, IC50=75 nM | 12190313 | ||
| MLF mouse lung fibroblast cell | Proliferation assay | Inhibition of MLF mouse lung fibroblast cell proliferation, IC50=72 nM | 12190313 | ||
| PC3 human prostate carcinoma cell | Proliferation assay | Inhibition of PC3 human prostate carcinoma cell proliferation, IC50=66 nM | 12190313 | ||
| MCF-7 human breast carcinoma cell | Proliferation assay | Inhibition of MCF-7 human breast carcinoma cell proliferation, IC50=66 nM | 12190313 | ||
| LS174T human colon carcinoma cell | Proliferation assay | Inhibition of LS174T human colon carcinoma cell proliferation, IC50=65 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 | ||
| A2780/DDP-S human ovarian carcinoma cell | Proliferation assay | Inhibition of A2780/DDP-S human ovarian carcinoma cell proliferation, IC50=56 nM | 12190313 | ||
| OVCAR-3 human ovarian carcinoma cell | Proliferation assay | Inhibition of OVCAR-3 human ovarian carcinoma cell proliferation, IC50=54 nM | 12190313 | ||
| CCRF-CEM human leukemia cell | Proliferation assay | Inhibition of CCRF-CEM human leukemia cell proliferation, IC50=52 nM | 12190313 | ||
| Hs 27 human fibroblast cell | Proliferation assay | Inhibition of Hs 27 human fibroblast cell proliferation, IC50=51 nM | 12190313 | ||
| HL60 human leukemia cell | Proliferation assay | Inhibition of HL60 human leukemia cell proliferation, IC50=46 nM | 12190313 | ||
| ABAE human fibroblast cell | Proliferation assay | Inhibition of ABAE human fibroblast cell proliferation, IC50=45 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 | ||
| HCT116/VM46 human colon carcinoma cell | Proliferation assay | Inhibition of HCT116/VM46 human colon carcinoma cell proliferation, IC50=21 nM | 12190313 | ||
| HCT116 human colon carcinoma cell | Proliferation assay | Inhibition of HCT116 human colon carcinoma cell proliferation, IC50=18 nM | 12190313 | ||
| HCT116/VP35 human colon carcinoma cell | Proliferation assay | Inhibition of HCT116/VP35 human colon carcinoma cell proliferation, IC50=17 nM | 12190313 | ||
| LNCaP human prostate carcinoma cell | Proliferation assay | Inhibition of LNCaP human prostate carcinoma cell proliferation | 12190313 | ||
| Mia PaCa-2 cell | Function assay | Inhibition of Mia PaCa-2 cell clonogenic assay, IC50=36 μM | 11063609 | ||
| A2780 cell | Function assay | Inhibition of A2780 cell clonogenic assay， IC50=15 μM | 11063609 | ||
| HCT116 cell | Function assay | Inhibition of HCT116 cell clonogenic assay, IC50=13 μM | 11063609 | ||
| PC3 cell | Function assay | Inhibition of PC3 cell clonogenic assay, IC50=10 μM | 11063609 | ||
| MCF-7 tumor cell | Proliferation assay | Inhibition of MCF-7 tumor cell proliferation | 10843211 | ||
| K562 human leukemia cell | Proliferation assay | Inhibition of K562 human leukemia cell proliferation, IC50=0.13 μM | 12190313 | ||
| human ovarian (A2780) cancer cell | Cytotoxic assay | Cytotoxic effect on human ovarian (A2780) cancer cell line, IC50=71 nM | 15125971 | ||
| ID8 cells | Proliferation assay | Antiproliferative activity against ID8 cells, IC50=7 nM | 17123821 | ||
| MCF7 cells | Proliferation assay | Antiproliferative activity against MCF7 cells, IC50=26 nM | 17123821 | ||
| Sf9 cells | Function assay | Inhibition of recombinant cyclin A/CDK2 expressed in Sf9 cells, IC50=12 nM | 17904366 | ||
| human A2780 cells | Function assay | Inhibition of cdk-mediated NPM phosphorylation at thr199 in human A2780 cells | 18469809 | ||
| MT4 | Antiproliferative assay | Antiviral activity against Human immunodeficiency virus 1 NL 4-3 infected in MT4 cells measured on day 4 post infection by p24 assay, EC50 = 0.015 μM. | 25914804 | ||
| MT4 | Cytotoxicity assay | Cytotoxicity against human MT4 cells, IC50 = 0.067 μM. | 25914804 | ||
| Sf21 | Function assay | 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 = 0.011 μM. | 27171036 | ||
| sf21 | Function assay | 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 = 0.395 μM. | 27171036 | ||
| Sf21 | Function assay | 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 = 0.514 μM. | 27171036 | ||
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生物活性
| 产品描述 | Flavopiridol (Alvocidib)与ATP竞争性抑制CDKs，包括CDK1、CDK2、CDK4、CDK6和CDK9的IC50范围为20-100 nM。作用于CDK1、2、4、6、9比作用于CDK7更具有选择性。Flavopiridol最初被发现能抑制EGFR和PKA。Flavopiridol可诱导自噬和内质网应激反应。Flavopiridol可阻滞HIV-1的复制。Phase 1/2。 | |||||||||||
|---|---|---|---|---|---|---|---|---|---|---|---|---|
| 特性 | Flavopiridol是第一个应用于人临床实验的细胞周期蛋白依赖性激酶抑制剂。 | |||||||||||
| 靶点 |
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| 体外研究(In Vitro) | ||||
| 体外研究活性 | 作为CDK广谱抑制剂，Flavopiridol可以抑制细胞周期进展，使其停在G1期或G2期。0.3 μM Flavopiridol作用于MCF-7或MDA-MB-468细胞，通过抑制CDK4或CDK2激酶活性，而诱导细胞周期停在G1 期。[4] Flavopiridol 作用于无关激酶，如MAP, PAK, PKC, 和 EGFR，活性低很多，IC50 >14 μM。Flavopiridol 显著抑制HCT116, A2780, PC3, 和 Mia PaCa-2 细胞集落生长，IC50分别为 13 nM, 15 nM, 10 nM, 和 36 nM。[1] Flavopiridol作用于多种肿瘤细胞系，具有细胞毒性，IC50为作用于LNCAP 的 16 nM 到作用于 K562的130 nM。[5] Flavopiridol也有效抑制糖原合成激酶-3(GSK-3) 的活性，IC50为 280 nm。[2]与其他CDKs相比, Flavopiridol抑制CDK7活性时效果稍弱，IC50为875 nM。 Flavopiridol (0.5 μM) 抑制pSer807/811 Rb 和pThr199 NPM,而在pThr821 Rb上观察到轻微变化。Flavopiridol也降低全部RNA聚合酶 II 水平, 及 RNA聚合酶 II在 CTD重复序列在 Ser2 Ser5位点磷酸化。[3] | |||
|---|---|---|---|---|
| 激酶实验 | CDK 激酶实验 | |||
| CDK1/cyclin B1 激酶实验中, 激酶反应包含100 ng表达 GST-CDK1/cyclin B1(人)复合体的 杆状病毒, 1 μg 组蛋白 HI, 0.2 μCi [γ-33P]ATP, 25 μM ATP溶于 50 μL 激酶buffer (50 mM Tris, pH 8.0, 10 mM MgCl2, 1 mM EGTA, 0.5 mM DTT)。CDK2/cyclin E 激酶实验中, 激酶反应包含5 ng表达 GST-CDK2/cyclin E (人)复合体的杆状病毒, 0.5 μg GST-RB 融合蛋白(成视网膜细胞瘤蛋白776-928 氨基酸), 0.2 μCi [γ-33P]ATP, 25 μM ATP溶于 50 μL 激酶buffer (50 mM Hepes, pH 8.0, 10 mM MgCl2, 1 mM EGTA, 2 mM DTT)。CDK4/cyclin D1激酶实验中, 激酶反应含150 ng 表达GST-CDK4/cyclin D1 (人)的杆状病毒, 280 ng Stag-cyclin D1, 0.5 μg GST-RB 融合蛋白(成视网膜细胞瘤蛋白776-928 氨基酸), 0.2 μCi [γ-33P]ATP, 25 μM ATP 溶于50 μL激酶 buffer (50 mM Hepes, pH 8.0, 10 mM MgCl2, 1 mM EGTA, 2 mM DTT)。30oC下， CDK1 和CDK2反应温育45分钟， CDK4反应温育1小时，加入终浓度为15%的冰冻三氯乙酸(TCA) 终止反应。 使用Filtermate通用收集器，收集TCA沉淀物转移到GF/C 非过滤板上， 使用TopCount 96孔液体闪烁计数器测量过滤数。Flavopiridol溶于 10 mM二甲基甲酰胺(DMF) 中，测定六种浓度，每种重复测三次。实验中 DMF终浓度为 2%。通过回归曲线分析获得IC50值，变异系数为 16%。测定Flavopiridol作用于 CDK6的活性, 进行过滤-结合实验。 反应混合物按如下结合： 2 μL CDK6 (0.7 mg/μL), 5 μL 组蛋白 H1 (6 mg/mL), 14 μL 激酶 buffer (60 mM β-甘油磷酸, 30 mM p-磷酸硝基苯酯, 25 mM MOPS (pH 7.0), 5 mM EGTA, 15 mM MgCl2, 1 mM DTT, 0.1 mM 钒酸钠), 在50% DMSO中稀释的 3 μL 浓度不断增长的Flavopiridol ，及6 μL 33P-ATP (1 mCi/mL)，非放射性 ATP，浓度为90 μM，(终浓度为15 μM)。加入33P-ATP开始反应。 反应在30oC下温育20分钟。25 μL等分的上清液点样到 Whatman P81 磷酸纤维素膜上。使用1% 磷酸溶液冲洗过滤器5次。 在1 mL闪烁液存在时测定湿过滤器。使用 50 nM 重组Cdk9/cyclin T在 50 mM HEPES pH 7.5, 10 mM MgCl2, 1 mM DTT, 3 μM Na3VO4, 150 μM RNA 聚合酶CDT 肽和80 μM ATP中测定Cdk9活性。在相同buffer中使用37 nM纯化激酶，在200 μM ATP 存在时，10 μM 髓鞘蛋白（MBP）作为底物，进行Cdk7检测实验。使用强阴离子交换剂-为基础的检测实验或闪烁接近实验测定Flavopiridol 作用于CDK9和CDK7的效果。通过剂量反应曲线计算IC50值。 | ||||
| 细胞实验 | 细胞系 | MCF-7, LNCAP, PC3, HCT116, CACO-2, A549, HL60, K562, 等等 | ||
| 浓度 | 溶于DMSO,终浓度为 ~10 μM | |||
| 孵育时间 | 72小时 | |||
| 方法 | 使用不同浓度 Flavopiridol 处理细胞72小时，加入四唑染料，MTS和吩嗪硫酸甲酯。3 小时后,在492 nm处测定吸光值,与存活细胞数成比例。结果表示为IC50值。为了分析细胞周期，细胞在仲甲醛和乙醇中混合，冲洗，然后再悬浮在TdT 酶和 FITC-dUTP染色液中,再冲洗，使用PI染色，随后进行RNA酶处理，最后使用流式细胞仪分析。 |
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| 实验图片 | 检测方法 | 检测指标 | 实验图片 | PMID |
| Western blot | Cleaved caspase-8 / Cleaved caspase-9 / Cleaved caspase-3 p-RNAPII / p-eIF4E / Mnk1 p-ERK / ERK / p-p38 / p-4EBP1 / 4EBP1 / p-S6 CDK2 / CDK4 / Cyclin A / p21 / p27 / Rb |
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31193061 | |
| Growth inhibition assay | Cell viability |
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31193061 | |
| 体内研究(In Vivo) | ||
| 体内研究活性 | Flavopiridol按7.5 mg/kg剂量处理P388 小鼠白血病，持续7天，具有轻微抗癌活性，导致%T/C值为110,且有效作用于皮下抑制人A2780卵巢癌的裸鼠，细胞对数杀灭(LCK)为1.5 。[5] Flavopiridol按 1-2.5 mg/kg 剂量处理小鼠，持续10天，通过抑制滑膜增生和关节损伤，而显著抑制胶原性关节炎，这种作用存在剂量依赖性，然而抗II型胶原(CII) 抗体的血清浓度，和II型胶原对应的增殖维持不变。[6] | |
|---|---|---|
| 动物实验 | Animal Models | 腹腔注射P388 腹水白血病细胞的雌性Balb/c×DBA/2J F1小鼠,皮下移植A2780, Br-cycE, 或A431细胞的Balb/c nu/nu裸鼠 |
| Dosages | ~7.5 mg/kg/day | |
| Administration | 腹腔注射 | |
| NCT Number | Recruitment | Conditions | Sponsor/Collaborators | Start Date | Phases |
|---|---|---|---|---|---|
| NCT03441555 | Completed | Acute Myeloid Leukemia (AML) |
AbbVie|Sumitomo Pharma America Inc. |
May 30 2018 | Phase 1 |
| NCT03298984 | Completed | Acute Myeloid Leukemia |
Sumitomo Pharma America Inc. |
September 25 2017 | Phase 1 |
化学信息&溶解度
| 分子量 | 401.84 | 分子式 | C21H20ClNO5 |
| CAS号 | 146426-40-6 | SDF | Download Flavopiridol (Alvocidib) SDF |
| Smiles | CN1CCC(C(C1)O)C2=C(C=C(C3=C2OC(=CC3=O)C4=CC=CC=C4Cl)O)O | ||
| 储存条件(自收到货起) | |||
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体外溶解度 |
DMSO : 80 mg/mL ( (199.08 mM)； DMSO吸湿会降低化合物溶解度，请使用新开封DMSO) Water : Insoluble 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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