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CDK1CDK2CDK4CDK6,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

Flavopiridol (Alvocidib) HCl Chemical Structure

CAS: 131740-09-5

规格 价格 库存 购买数量
10mM (1mL in DMSO) 819.17 现货
10mg 903.08 现货
25mg 1813.43 现货
50mg 3121.42 现货
1g 24488.1 现货
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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
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生物活性

产品描述 Flavopiridol (Alvocidib) HCl与ATP竞争性抑制CDKs,作用于CDK1CDK2CDK4CDK6,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
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
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 24572052
Growth inhibition assay Cell viability 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)

体外溶解度
批次:

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

体内溶解度
批次:

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

摩尔浓度计算器

质量 浓度 体积 分子量

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

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,: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: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: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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