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Flavopiridol (Alvocidib)

別名: NSC 649890, HMR-1275, L86-8275 中文名稱：夫拉平度

Flavopiridol (Alvocidib)與ATP競(jìng)爭(zhēng)性抑制CDKs，包括CDK1、CDK2、CDK4、CDK6和CDK9的IC50范圍為20-100 nM。作用于CDK1、2、4、6、9比作用于CDK7更具有選擇性。Flavopiridol最初被發(fā)現(xiàn)能抑制EGFR和PKA。Flavopiridol可誘導(dǎo)自噬和內(nèi)質(zhì)網(wǎng)應(yīng)激反應(yīng)。Flavopiridol可阻滯HIV-1的復(fù)制。Phase 1/2。

Flavopiridol (Alvocidib) Chemical Structure

Flavopiridol (Alvocidib) Chemical Structure

CAS: 146426-40-6

規(guī)格 價(jià)格 庫(kù)存 購(gòu)買(mǎi)數(shù)量
10mM (1mL in DMSO) 810.81 現(xiàn)貨
5mg 647.01 現(xiàn)貨
25mg 1386.75 現(xiàn)貨
100mg 4668.25 現(xiàn)貨
1g 22686.3 現(xiàn)貨
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Flavopiridol (Alvocidib)相關(guān)產(chǎn)品

相關(guān)信號(hào)通路圖

CDK Signaling Pathways

CDK信號(hào)通路圖

細(xì)胞實(shí)驗(yàn)數(shù)據(jù)示例

細(xì)胞系 實(shí)驗(yàn)類型 給藥濃度 孵育時(shí)間 活性描述 文獻(xiàn)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

產(chǎn)品描述 Flavopiridol (Alvocidib)與ATP競(jìng)爭(zhēng)性抑制CDKs，包括CDK1、CDK2、CDK4、CDK6和CDK9的IC50范圍為20-100 nM。作用于CDK1、2、4、6、9比作用于CDK7更具有選擇性。Flavopiridol最初被發(fā)現(xiàn)能抑制EGFR和PKA。Flavopiridol可誘導(dǎo)自噬和內(nèi)質(zhì)網(wǎng)應(yīng)激反應(yīng)。Flavopiridol可阻滯HIV-1的復(fù)制。Phase 1/2。
特性 Flavopiridol是第一個(gè)應(yīng)用于人臨床實(shí)驗(yàn)的細(xì)胞周期蛋白依賴性激酶抑制劑。
靶點(diǎn)
CDK9 [8]
(Cell-free assay)		 CDK1 [8]
(Cell-free assay)		 CDK4 [9]
(Cell-free assay)		 CDK2 [8]
(Cell-free assay)		 CDK6 [9]
(Cell-free assay)		 點(diǎn)擊更多
20 nM 30 nM 20-40 nM 40 nM 60 nM
體外研究(In Vitro)
體外研究活性 作為CDK廣譜抑制劑，F(xiàn)lavopiridol可以抑制細(xì)胞周期進(jìn)展，使其停在G1期或G2期。0.3 μM Flavopiridol作用于MCF-7或MDA-MB-468細(xì)胞，通過(guò)抑制CDK4或CDK2激酶活性，而誘導(dǎo)細(xì)胞周期停在G1 期。[4] Flavopiridol 作用于無(wú)關(guān)激酶，如MAP, PAK, PKC, 和 EGFR，活性低很多，IC50 >14 μM。Flavopiridol 顯著抑制HCT116, A2780, PC3, 和 Mia PaCa-2 細(xì)胞集落生長(zhǎng)，IC50分別為 13 nM, 15 nM, 10 nM, 和 36 nM。[1] Flavopiridol作用于多種腫瘤細(xì)胞系，具有細(xì)胞毒性，IC50為作用于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為 280 nm。[2]與其他CDKs相比, Flavopiridol抑制CDK7活性時(shí)效果稍弱，IC50為875 nM。 Flavopiridol (0.5 μM) 抑制pSer807/811 Rb 和pThr199 NPM,而在pThr821 Rb上觀察到輕微變化。Flavopiridol也降低全部RNA聚合酶 II 水平, 及 RNA聚合酶 II在 CTD重復(fù)序列在 Ser2 Ser5位點(diǎn)磷酸化。[3]
激酶實(shí)驗(yàn) CDK 激酶實(shí)驗(yàn)
CDK1/cyclin B1 激酶實(shí)驗(yàn)中, 激酶反應(yīng)包含100 ng表達(dá) GST-CDK1/cyclin B1(人)復(fù)合體的 桿狀病毒, 1 μg 組蛋白 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 激酶實(shí)驗(yàn)中, 激酶反應(yīng)包含5 ng表達(dá) GST-CDK2/cyclin E (人)復(fù)合體的桿狀病毒, 0.5 μg GST-RB 融合蛋白(成視網(wǎng)膜細(xì)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激酶實(shí)驗(yàn)中, 激酶反應(yīng)含150 ng 表達(dá)GST-CDK4/cyclin D1 (人)的桿狀病毒, 280 ng Stag-cyclin D1, 0.5 μg GST-RB 融合蛋白(成視網(wǎng)膜細(xì)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反應(yīng)溫育45分鐘， CDK4反應(yīng)溫育1小時(shí)，加入終濃度為15%的冰凍三氯乙酸(TCA) 終止反應(yīng)。 使用Filtermate通用收集器，收集TCA沉淀物轉(zhuǎn)移到GF/C 非過(guò)濾板上， 使用TopCount 96孔液體閃爍計(jì)數(shù)器測(cè)量過(guò)濾數(shù)。Flavopiridol溶于 10 mM二甲基甲酰胺(DMF) 中，測(cè)定六種濃度，每種重復(fù)測(cè)三次。實(shí)驗(yàn)中 DMF終濃度為 2%。通過(guò)回歸曲線分析獲得IC50值，變異系數(shù)為 16%。測(cè)定Flavopiridol作用于 CDK6的活性, 進(jìn)行過(guò)濾-結(jié)合實(shí)驗(yàn)。 反應(yīng)混合物按如下結(jié)合： 2 μL CDK6 (0.7 mg/μL), 5 μL 組蛋白 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 釩酸鈉), 在50% DMSO中稀釋的 3 μL 濃度不斷增長(zhǎng)的Flavopiridol ，及6 μL 33P-ATP (1 mCi/mL)，非放射性 ATP，濃度為90 μM，(終濃度為15 μM)。加入33P-ATP開(kāi)始反應(yīng)。 反應(yīng)在30oC下溫育20分鐘。25 μL等分的上清液點(diǎn)樣到 Whatman P81 磷酸纖維素膜上。使用1% 磷酸溶液沖洗過(guò)濾器5次。 在1 mL閃爍液存在時(shí)測(cè)定濕過(guò)濾器。使用 50 nM 重組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中測(cè)定Cdk9活性。在相同buffer中使用37 nM純化激酶，在200 μM ATP 存在時(shí)，10 μM 髓鞘蛋白（MBP）作為底物，進(jìn)行Cdk7檢測(cè)實(shí)驗(yàn)。使用強(qiáng)陰離子交換劑-為基礎(chǔ)的檢測(cè)實(shí)驗(yàn)或閃爍接近實(shí)驗(yàn)測(cè)定Flavopiridol 作用于CDK9和CDK7的效果。通過(guò)劑量反應(yīng)曲線計(jì)算IC50值。
細(xì)胞實(shí)驗(yàn) 細(xì)胞系 MCF-7, LNCAP, PC3, HCT116, CACO-2, A549, HL60, K562, 等等
濃度 溶于DMSO,終濃度為 ~10 μM
孵育時(shí)間 72小時(shí)
方法

使用不同濃度 Flavopiridol 處理細(xì)胞72小時(shí)，加入四唑染料，MTS和吩嗪硫酸甲酯。3 小時(shí)后,在492 nm處測(cè)定吸光值,與存活細(xì)胞數(shù)成比例。結(jié)果表示為IC50值。為了分析細(xì)胞周期，細(xì)胞在仲甲醛和乙醇中混合，沖洗，然后再懸浮在TdT 酶和 FITC-dUTP染色液中,再?zèng)_洗，使用PI染色，隨后進(jìn)行RNA酶處理，最后使用流式細(xì)胞儀分析。
實(shí)驗(yàn)圖片 檢測(cè)方法 檢測(cè)指標(biāo) 實(shí)驗(yàn)圖片 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 31193061
Growth inhibition assay Cell viability 31193061
體內(nèi)研究(In Vivo)
體內(nèi)研究活性 Flavopiridol按7.5 mg/kg劑量處理P388 小鼠白血病，持續(xù)7天，具有輕微抗癌活性，導(dǎo)致%T/C值為110,且有效作用于皮下抑制人A2780卵巢癌的裸鼠，細(xì)胞對(duì)數(shù)殺滅(LCK)為1.5 。[5] Flavopiridol按 1-2.5 mg/kg 劑量處理小鼠，持續(xù)10天，通過(guò)抑制滑膜增生和關(guān)節(jié)損傷，而顯著抑制膠原性關(guān)節(jié)炎，這種作用存在劑量依賴性，然而抗II型膠原(CII) 抗體的血清濃度，和II型膠原對(duì)應(yīng)的增殖維持不變。[6]
動(dòng)物實(shí)驗(yàn) Animal Models 腹腔注射P388 腹水白血病細(xì)胞的雌性Balb/c×DBA/2J F1小鼠,皮下移植A2780, Br-cycE, 或A431細(xì)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

化學(xué)信息&溶解度

分子量 401.84 分子式

C21H20ClNO5
CAS號(hào) 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
儲(chǔ)存條件(自收到貨起)

體外溶解度
批次：

DMSO : 80 mg/mL ( (199.08 mM) ；DMSO吸濕會(huì)降低化合物溶解度，請(qǐng)使用新開(kāi)封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計(jì)算器

體內(nèi)溶解度
批次：

現(xiàn)配現(xiàn)用，請(qǐng)按從左到右的順序依次添加，澄清后再加入下一溶劑

 動(dòng)物體內(nèi)配方計(jì)算器

實(shí)驗(yàn)計(jì)算

摩爾濃度計(jì)算器

質(zhì)量 濃度 體積 分子量

動(dòng)物體內(nèi)配方計(jì)算器（澄清溶液）

第一步：請(qǐng)輸入基本實(shí)驗(yàn)信息（考慮到實(shí)驗(yàn)過(guò)程中的損耗，建議多配一只動(dòng)物的藥量）

mg/kg g μL 只

第二步：請(qǐng)輸入動(dòng)物體內(nèi)配方組成（配方適用于不溶于水的藥物；不同批次藥物配方比例不同，請(qǐng)聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO % % Tween 80 % ddH2O
%DMSO %

計(jì)算結(jié)果：

工作液濃度： mg/ml；

DMSO母液配制方法： mg 藥物溶于μL DMSO溶液（母液濃度mg/mL，注：如該濃度超過(guò)該批次藥物DMSO溶解度，請(qǐng)先聯(lián)系Selleck）；

體內(nèi)配方配制方法：取μL DMSO母液，加入μL PEG300，混勻澄清后加入μL Tween 80，混勻澄清后加入μL ddH2O，混勻澄清。

體內(nèi)配方配制方法：取μL DMSO母液，加入μL Corn oil，混勻澄清。

注意：1. 首先保證母液是澄清的；
2.一定要按照順序依次將溶劑加入，進(jìn)行下一步操作之前必須保證上一步操作得到的是澄清的溶液，可采用渦旋、超聲或水浴加熱等物理方法助溶。

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