Flavopiridol (Alvocidib)

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

目錄號：S1230 Purity: 99.92%

Flavopiridol (Alvocidib)與ATP競爭性抑制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可誘導自噬和內(nèi)質(zhì)網(wǎng)應激反應。Flavopiridol可阻滯HIV-1的復制。Phase 1/2。

Flavopiridol (Alvocidib) Chemical Structure

CAS: 146426-40-6

規(guī)格	價格	庫存
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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產(chǎn)品質(zhì)控

批次：純度： 99.92%

99.92

Flavopiridol (Alvocidib)相關(guān)產(chǎn)品

相關(guān)靶點	CDK1 CDK2 CDK3 CDK4 CDK5 CDK6 CDK7 CDK9 CLK Cdc CDK8 CDK12 CDK13 CDK19 CDK11 CDK/cyclin complexes	點擊展開
相關(guān)產(chǎn)品	Ro-3306 Dinaciclib Roscovitine SNS-032 (BMS-387032) Flavopiridol (Alvocidib) HCl AT7519 LDC000067 PHA-767491 HCl THZ1 2HCl XL413 JNJ-7706621 AZD5438 Purvalanol A Milciclib BS-181 HCl K03861 (AUZ454) PHA-793887 BMS-265246 AT7519 HCl AZD4573 MSC2530818 Riviciclib hydrochloride (P276-00) CVT-313 TG003 Kenpaullone R547 Atuveciclib (BAY-1143572) YKL-5-124 LDC4297 Enitociclib (BAY 1251152) PF-06873600 Wogonin SU9516 SEL120 (SEL120-34A) hydrochloride THZ531 Senexin A Samuraciclib (ICEC0942) hydrochloride LY2857785 ON123300 CDK2-IN-73 (CDK2-IN-4) NU2058 BRD6989 HLM006474 AS2863619 CDKI-73 MC180295 ML167 Simurosertib Simurosertib NSC95397 NU6027	點擊展開
相關(guān)化合物庫	激酶抑制劑庫 PI3K/Akt 抑制劑庫 MAPK抑制劑庫 DNA損傷/ DNA修復化合物庫細胞周期化合物庫	點擊展開

細胞實驗數(shù)據(jù)示例

細胞系	實驗類型	給藥濃度	孵育時間	活性描述	文獻信息
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

特性

Flavopiridol是第一個應用于人臨床實驗的細胞周期蛋白依賴性激酶抑制劑。

靶點

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)	點擊更多
20 nM	30 nM	20-40 nM	40 nM	60 nM	點擊更多

體外研究(In Vitro)
體外研究活性	作為CDK廣譜抑制劑，F(xiàn)lavopiridol可以抑制細胞周期進展，使其停在G1期或G2期。0.3 μM Flavopiridol作用于MCF-7或MDA-MB-468細胞，通過抑制CDK4或CDK2激酶活性，而誘導細胞周期停在G1 期。^[4] Flavopiridol 作用于無關(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 細胞集落生長，IC50分別為 13 nM, 15 nM, 10 nM, 和 36 nM。^[1] Flavopiridol作用于多種腫瘤細胞系，具有細胞毒性，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重復序列在 Ser2 Ser5位點磷酸化。^[3]
激酶實驗	CDK 激酶實驗
激酶實驗	CDK1/cyclin B1 激酶實驗中, 激酶反應包含100 ng表達 GST-CDK1/cyclin B1(人)復合體的桿狀病毒, 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 激酶實驗中, 激酶反應包含5 ng表達 GST-CDK2/cyclin E (人)復合體的桿狀病毒, 0.5 μg GST-RB 融合蛋白(成視網(wǎng)膜細胞瘤蛋白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激酶實驗中, 激酶反應含150 ng 表達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)。30^oC下， CDK1 和CDK2反應溫育45分鐘， CDK4反應溫育1小時，加入終濃度為15%的冰凍三氯乙酸(TCA) 終止反應。使用Filtermate通用收集器，收集TCA沉淀物轉(zhuǎn)移到GF/C 非過濾板上，使用TopCount 96孔液體閃爍計數(shù)器測量過濾數(shù)。Flavopiridol溶于 10 mM二甲基甲酰胺(DMF) 中，測定六種濃度，每種重復測三次。實驗中 DMF終濃度為 2%。通過回歸曲線分析獲得IC50值，變異系數(shù)為 16%。測定Flavopiridol作用于 CDK6的活性, 進行過濾-結(jié)合實驗。反應混合物按如下結(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開始反應。反應在30^oC下溫育20分鐘。25 μL等分的上清液點樣到 Whatman P81 磷酸纖維素膜上。使用1% 磷酸溶液沖洗過濾器5次。在1 mL閃爍液存在時測定濕過濾器。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中測定Cdk9活性。在相同buffer中使用37 nM純化激酶，在200 μM ATP 存在時，10 μM 髓鞘蛋白（MBP）作為底物，進行Cdk7檢測實驗。使用強陰離子交換劑-為基礎(chǔ)的檢測實驗或閃爍接近實驗測定Flavopiridol 作用于CDK9和CDK7的效果。通過劑量反應曲線計算IC50值。
細胞實驗	細胞系	MCF-7, LNCAP, PC3, HCT116, CACO-2, A549, HL60, K562, 等等
	濃度	溶于DMSO,終濃度為 ~10 μM
	孵育時間	72小時
	方法	使用不同濃度 Flavopiridol 處理細胞72小時，加入四唑染料，MTS和吩嗪硫酸甲酯。3 小時后,在492 nm處測定吸光值,與存活細胞數(shù)成比例。結(jié)果表示為IC50值。為了分析細胞周期，細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,再沖洗，使用PI染色，隨后進行RNA酶處理，最后使用流式細胞儀分析。
實驗圖片	檢測方法	檢測指標	實驗圖片	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，細胞對數(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型膠原對應的增殖維持不變。^[6]
動物實驗	Animal Models	腹腔注射P388 腹水白血病細胞的雌性Balb/c×DBA/2J F1小鼠,皮下移植A2780, Br-cycE, 或A431細胞的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
臨床試驗信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
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

參考文獻
[1] Kim KS, et al. J Med Chem, 2000, 43(22), 4126-4134. [2] Lu H, et al. J Med Chem, 2005, 48(3), 737-743. [3] Montagnoli A, et al. Nat Chem Biol, 2008, 4(6), 357-365. [4] Carlson BA, et al. Cancer Res, 1996, 56(13), 2973-2978. [5] Kim KS, et al. J Med Chem, 2002, 45(18), 3905-3927. [6] Sekine C, et al. J Immunol, 2008, 180(3), 1954-1961. [7] Motwani M, et al. Clin Cancer Res, 2001, 7(12), 4209-4219. [8] Montagnoli A, et al. Nat Chem Biol. 2008, 4(6):357-65. [9] Sedlacek HH. Crit Rev Oncol Hematol. 2001, 38(2):139-70. + 展開

參考文獻

[1] Kim KS, et al. J Med Chem, 2000, 43(22), 4126-4134.
[2] Lu H, et al. J Med Chem, 2005, 48(3), 737-743.
[3] Montagnoli A, et al. Nat Chem Biol, 2008, 4(6), 357-365.

[4] Carlson BA, et al. Cancer Res, 1996, 56(13), 2973-2978.
[5] Kim KS, et al. J Med Chem, 2002, 45(18), 3905-3927.
[6] Sekine C, et al. J Immunol, 2008, 180(3), 1954-1961.
[7] Motwani M, et al. Clin Cancer Res, 2001, 7(12), 4209-4219.
[8] Montagnoli A, et al. Nat Chem Biol. 2008, 4(6):357-65.
[9] Sedlacek HH. Crit Rev Oncol Hematol. 2001, 38(2):139-70.

+ 展開

化學信息&溶解度

分子量	401.84	分子式	C₂₁H₂₀ClNO₅
CAS號	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
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復凍融！	1年-80°C溶于溶劑
儲存條件(自收到貨起)	3年-20°C粉狀	儲備液保存和期限建議分裝儲備液，避免反復凍融！	1個月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 80 mg/mL ( (199.08 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

DMSO : 80 mg/mL ( (199.08 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : Insoluble

Ethanol : Insoluble

摩爾濃度計算器

體內(nèi)溶解度
批次：

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

動物體內(nèi)配方計算器

實驗計算

摩爾濃度計算器

質(zhì)量	濃度	體積	分子量
=	×	×

稀釋計算器分子量計算器

動物體內(nèi)配方計算器（澄清溶液）

第一步：請輸入基本實驗信息（考慮到實驗過程中的損耗，建議多配一只動物的藥量）

給藥劑量 mg/kg 動物平均體重 g 每只動物給藥體積 μL 動物數(shù)量只

第二步：請輸入動物體內(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，請聯(lián)系Selleck為您提供正確的澄清溶液配方）

% DMSO + % + % Tween 80 + % ddH2O

%DMSO+ %

計算結(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：如該濃度超過該批次藥物DMSO溶解度，請先聯(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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操作手冊

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* 必填項

C1=C0/X	C1:	LOG(C1):
C2=C1/X	C2:	LOG(C2):
C3=C2/X	C3:	LOG(C3):
C4=C3/X	C4:	LOG(C4):
C5=C4/X	C5:	LOG(C5):
C6=C5/X	C6:	LOG(C6):
C7=C6/X	C7:	LOG(C7):
C8=C7/X	C8:	LOG(C8):

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