Flavopiridol (Alvocidib) HCl

別名: NSC 649890, L86-8275, HMR-1275, DSP-2033 中文名稱：鹽酸夫拉平度

目錄號：S2679 Purity: 99.44%

Flavopiridol (Alvocidib) HCl與ATP競爭性抑制CDKs，作用于CDK1，CDK2，CDK4和CDK6，無細(xì)胞試驗中IC50為~40 nM。作用于CDK1/2/4/6比作用于CDK7選擇性高7.5倍。Flavopiridol最初被發(fā)現(xiàn)可抑制EGFR和PKA。Flavopiridol HCl 可誘導(dǎo)自噬和內(nèi)質(zhì)網(wǎng)應(yīng)激反應(yīng)。Flavopiridol HCl 可阻止HIV-1的復(fù)制。Phase 1/2。

Flavopiridol (Alvocidib) HCl Chemical Structure

CAS: 131740-09-5

規(guī)格	價格	庫存
10mM (1mL in DMSO)	819.17	現(xiàn)貨
10mg	903.08	現(xiàn)貨
25mg	1813.43	現(xiàn)貨
50mg	3121.42	現(xiàn)貨
1g	24488.1	現(xiàn)貨
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產(chǎn)品質(zhì)控

批次：純度： 99.44%

99.44

Flavopiridol (Alvocidib) HCl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
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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(fù)化合物庫細(xì)胞周期化合物庫	點擊展開

細(xì)胞實驗數(shù)據(jù)示例

細(xì)胞系	實驗類型	給藥濃度	孵育時間	活性描述	文獻(xiàn)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
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生物活性

產(chǎn)品描述

靶點

CDK1 ^[1] (Cell-free assay)	CDK2 ^[1] (Cell-free assay)	CDK4 ^[1] (Cell-free assay)	CDK6 ^[1] (Cell-free assay)	CDK7 ^[1] (Cell-free assay)
40 nM	40 nM	40 nM	40 nM	300 nM

體外研究(In Vitro)
體外研究活性	Flavopiridol最初被發(fā)現(xiàn)抑制表皮生長因子受體和蛋白激酶A的活性，IC50分別是21 μM and 122 μM。Flavopiridol是后來證明能夠抑制細(xì)胞的增殖，在多種生理相關(guān)濃度(IC50 = 66 nM)，在腫瘤細(xì)胞系美國國家癌癥研究所開發(fā)治療計劃中的60種人癌細(xì)胞系測試過。^[1] Flavopiridol以時間和濃度依賴性方式誘導(dǎo)人類乳腺癌細(xì)胞G1期阻滯并抑制CDK2和CDK4。^[2] Flavopiridol短時處理（約12小時）誘導(dǎo)造血細(xì)胞系的細(xì)胞凋亡，包括SUDHL4，SUDHL6（B細(xì)胞系），Jurkat和MOLT4（T細(xì)胞系）和HL60（髓細(xì)胞系）。^[3] 在克隆形成實驗中，F(xiàn)lavopiridol在23人腫瘤模型中表現(xiàn)高細(xì)胞毒性，平均IC70是8 ng/mL。^[4] 最近的一項研究表明Flavopiridol誘導(dǎo)人腦膠質(zhì)瘤T98G細(xì)胞系的AKT-Ser473磷酸化。^[5]
激酶實驗	重組CDKs激酶反應(yīng)
激酶實驗	CDKs的活性按如下方式在酶標(biāo)板中，40 μg GST-R b與不同量Flavopiridol和未標(biāo)記的ATP混合。反應(yīng)然后通過加入S100的餾分從表達(dá)重組人CDK的昆蟲細(xì)胞中得到的硫酸銨沉淀部分的開始。最終反應(yīng)條件為10 mM MgCl₂, 50 mM Tris-HCl (pH 7.5)和1 mM DTT。ATP的終濃度做相應(yīng)的調(diào)整。放射性標(biāo)記的ATP作為磷酸供體。該反應(yīng)在30℃下加入酶后進(jìn)行2.5分鐘，然后加入EDTA終止。GST-Rb用谷胱甘肽 - 瓊脂糖標(biāo)記和摻入的放射性通過液體閃爍計數(shù)測定。
細(xì)胞實驗	細(xì)胞系	SUDHL4, SUDHL6, Jurkat, MOLT4和HL60細(xì)胞
	濃度	0, 100 500, 5000 nM
	孵育時間	14小時
	方法	在密度為1 × 10⁶ cells/mL的細(xì)胞中不同時間加入不同濃度的Flavopiridol。提取DNA。細(xì)胞用冷的磷酸鹽緩沖鹽水（PBS）洗滌一次并在4℃條件下在3 mL裂解緩沖液（5 mM Tris-HCL [pH 7.5]; 20 mM EDTA; 0.5% Triton X-100）中裂解15分鐘。將細(xì)胞裂解物的染色質(zhì)（以26,000 g，4℃，20分鐘）離心分離。用苯酚，酚氯仿（1:1）和氯仿從上清液提取提取小的DNA片段。核酸在-20℃中在0.5M氯化鈉，90％的乙醇沉淀過夜。RNA由牛RNAaseA消化（60μg/mL）。連續(xù)反萃取和沉淀后，DNA溶解在10mM Tris-HCl（pH值7.5），1mM的EDTA，0.5％十二烷基硫酸鈉（SDS），而后在1.6％瓊脂糖凝膠上電泳。
實驗圖片	檢測方法	檢測指標(biāo)	實驗圖片	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		24572052
	Growth inhibition assay	Cell viability		31193061

體內(nèi)研究(In Vivo)
體內(nèi)研究活性	以最大耐受劑量10 mg/kg/day在第1-4天及7-11天給藥，F(xiàn)lavopiridol表現(xiàn)為PRXF1337腫瘤消退和PRXF1369腫瘤停滯為期4周。^[4] 用7.5 mg/kg Flavopiridol靜脈內(nèi)（IV）或腹膜內(nèi)連續(xù)注射5天后，12分之11的皮下（SC）人HL-60 移植鼠的腫瘤完全消退，F(xiàn)lavopiridol治療一療程后移植鼠數(shù)月無病。在SUDHL-4皮下注射淋巴瘤模型鼠中靜脈注射Flavopiridol （7.5 mg/kg），模型鼠的腫瘤大部分（8分之2）或者完全（8分之4）消退，兩只剩余動物無病超過60天。整體生長延遲73.2％。^[6]
動物實驗	Animal Models	人類前列腺癌異種移植，PRXFI337和PRXFI369，皮下種植在裸鼠中
	Dosages	10 mg/kg/d
	Administration	在days 1-4 and 7-11口服。

NCT Number	Recruitment	Conditions	Sponsor/Collaborators	Start Date	Phases
臨床試驗信息 (data from https://clinicaltrials.gov, updated on 2024-05-22)
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\|Waldenstr?m 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\|Waldenstr?m Macroglobulinemia	National Cancer Institute (NCI)	April 2003	Phase 1\|Phase 2

參考文獻(xiàn)
[1] Senderowicz AM, Oncologist, 2002, 7 Suppl 3:12-9. [2] Carlson BA, et al, Cancer Res, 1996, 56(13), 2973-2978. [3] Parker BW, et al, Blood, 1998, 91(2), 458-465. [4] Drees M, et al, Clin Cancer Res, 1997, 3(2), 273-279. [5] Caracciolo V, et al, Cell Cycle, 2012, 11(6), 1202-1216. [6] Arguello F,et al, Blood, 1998, 91(7), 2482-2490. + 展開

參考文獻(xiàn)

[1] Senderowicz AM, Oncologist, 2002, 7 Suppl 3:12-9.
[2] Carlson BA, et al, Cancer Res, 1996, 56(13), 2973-2978.
[3] Parker BW, et al, Blood, 1998, 91(2), 458-465.

[4] Drees M, et al, Clin Cancer Res, 1997, 3(2), 273-279.
[5] Caracciolo V, et al, Cell Cycle, 2012, 11(6), 1202-1216.
[6] Arguello F,et al, Blood, 1998, 91(7), 2482-2490.

+ 展開

化學(xué)信息&溶解度

分子量	438.3	分子式	C₂₁H₂₀ClNO₅.HCl
CAS號	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
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(fù)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(fù)凍融！	1個月-20°C溶于溶劑

體外溶解度
批次：

DMSO : 88 mg/mL ( (200.77 mM) ；DMSO吸濕會降低化合物溶解度，請使用新開封DMSO)

Water : 37 mg/mL (84.41 mM)

Ethanol : Insoluble

DMSO : 88 mg/mL ( (200.77 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 : 88 mg/mL ( (200.77 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(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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操作手冊

如果有其他問題，請給我們留言。

* 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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Flavopiridol (Alvocidib) HCl

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相關(guān)信號通路圖

細(xì)胞實驗數(shù)據(jù)示例

生物活性

化學(xué)信息&溶解度

實驗計算

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