Panobinostat (LBH589)

别名: NVP-LBH589 中文名称:帕比司他

Panobinostat (LBH589, NVP-LBH589)是一种新型的,广谱HDAC抑制剂,无细胞试验中IC50为5 nM。Panobinostat (LBH589) 可诱导自噬和凋亡。Panobinostat 可以有效地破坏体内 HIV 的潜伏期。Phase 3。

Panobinostat (LBH589) Chemical Structure

Panobinostat (LBH589) Chemical Structure

CAS: 404950-80-7

规格 价格 库存 购买数量
10mM (1mL in DMSO) RMB 953.44 现货
10mg RMB 731.86 现货
50mg RMB 2189.52 现货
200mg RMB 5485.18 现货
1g RMB 12039.3 现货
更大包装 有超大折扣

400-668-6834

info@selleck.cn

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客户使用Selleck的Panobinostat (LBH589)发表文献380

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批次: 纯度: 99.96%
99.70

Panobinostat (LBH589)相关产品

相关信号通路图

HDAC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
SK-N-BE Apoptosis Assay 0–40 nM 48 h potently induced apoptosis in a dose-dependent fashion 24098799
SK-N-SH Apoptosis Assay 0–40 nM 48 h potently induced apoptosis in a dose-dependent fashion 24098799
SK-N-DZ Apoptosis Assay 0–80 nM 48 h potently induced apoptosis in a dose-dependent fashion 24098799
SK-N-AS Apoptosis Assay 0–80 nM 48 h potently induced apoptosis in a dose-dependent fashion 24098799
SK-N-BE Growth Inhibition Assay 0–80 nM 48 h IC50=75.4 nM 24098799
SK-N-SH Growth Inhibition Assay 0–80 nM 48 h IC50=72.3 nM 24098799
SK-N-DZ Growth Inhibition Assay 0–80 nM 48 h IC50=21.9 nM 24098799
SK-N-AS Growth Inhibition Assay 0–80 nM 48 h IC50=27.4 nM 24098799
OS-RC-2 Apoptosis Assay 50 nM 48 h induces cell apoptosis 24144737
OS-RC-2 Growth Inhibition Assay 50 nM 48 h induces G2/M arrest 24144737
OS-RC-2 Cell Viability Assay 0-1000 nM 24/48/72 h decreases cell viability in both time- and dose-dependent manner 24144737
PC3-AR Function Assay 0-100 nM 24 h suppresses expression of activated ATM, Akt and Erk1/2 protein 24163230
PC3 Function Assay 0-100 nM 24 h suppresses expression of activated ATM, Akt and Erk1/2 protein 24163230
PC3-AR Growth Inhibition Assay 0-100 nM 24/48 h induces cell cycle arrest in the G2M phase 24163230
PC3 Growth Inhibition Assay 0-100 nM 24/48 h induces accumulation of subG1 population 24163230
PC3-AR Apoptosis Assay 0-100 nM 24/48 h induces apoptosis in both time- and dose-dependent manner 24163230
PC3 Apoptosis Assay 0-100 nM 24/48 h induces apoptosis in a dose-dependent manner 24163230
U937 Apoptosis Assay 0–40 nM  48 h induces apoptosis in a dose-dependent manner 24244429
OCI-AML3  Apoptosis Assay 0–40 nM  48 h induces apoptosis in a dose-dependent manner 24244429
CTS Apoptosis Assay 0–40 nM  48 h induces apoptosis in a dose-dependent manner 24244429
MCF-7 Function Assay 5-50 nM 24 h reduced the level of expression of ERα, PR and FoxA1  24366407
MCF-7  Morphological Crystal Violet (CV) Assay 10 nM 3 d alters cell morphology  24810497
BT-549 Morphological Crystal Violet (CV) Assay 10 nM 3 d alters cell morphology  24810497
MDA-MB-231 Morphological Crystal Violet (CV) Assay 10 nM 3 d alters cell morphology  24810497
769-P Apoptosis Assay 50 nM 48 h induces cell apoptosis 25176354
ACHN Apoptosis Assay 50 nM 48 h induces cell apoptosis 25176354
Caki-1 Apoptosis Assay 50 nM 48 h induces cell apoptosis 25176354
769-P Colony Formation Assay 50 nM 7-14 d suppressed colony formation significantly combined with with bortezomib   25176354
ACHN Colony Formation Assay 50 nM 7-14 d suppressed colony formation significantly combined with with bortezomib   25176354
Caki-1 Colony Formation Assay 50 nM 7-14 d suppressed colony formation significantly combined with with bortezomib   25176354
769-P Growth Inhibition Assay 25/50 nM 48 h inhibits cell growth in a dose dependent manner synergistically with bortezomib 25176354
ACHN Growth Inhibition Assay 25/50 nM 48 h inhibits cell growth in a dose dependent manner synergistically with bortezomib 25176354
Caki-1 Growth Inhibition Assay 25/50 nM 48 h inhibits cell growth in a dose dependent manner synergistically with bortezomib 25176354
786-O  Apoptosis Assay 50 nM 48 h induces cell apoptosis combined ritonavir 25279191
769-P Apoptosis Assay 50 nM 48 h induces cell apoptosis combined ritonavir 25279191
ACHN Apoptosis Assay 50 nM 48 h induces cell apoptosis combined ritonavir 25279191
Caki-1 Apoptosis Assay 50 nM 48 h induces cell apoptosis combined ritonavir 25279191
786-O  Growth Inhibition Assay 10/25/50 nM 48 h inhibits cell growth in a dose dependent manner synergistically with ritonavir 25279191
769-P Growth Inhibition Assay 10/25/50 nM 48 h inhibits cell growth in a dose dependent manner synergistically with ritonavir 25279191
ACHN Growth Inhibition Assay 10/25/50 nM 48 h inhibits cell growth in a dose dependent manner synergistically with ritonavir 25279191
Caki-1 Growth Inhibition Assay 10/25/50 nM 48 h inhibits cell growth in a dose dependent manner synergistically with ritonavir 25279191
RPMI-8226vr10  Function Assay 1 μM 24 h increases caspase-3 activity 2.5-fold 25612941
ML-1 Function Assay 1 μM 24 h increases caspase-3 activity 4-fold 25612941
RPMI-8226vr10  Function Assay 0-1 μM 24 h induces DNA fragmentation in a dose-dependent manner 25612941
ML-1 Function Assay 0-1 μM 24 h induces DNA fragmentation in a dose-dependent manner 25612941
AML3 Function Assay 0-1 μM 24 h induces DNA fragmentation in a dose-dependent manner 25612941
NCI-H23 Growth Inhibition Assay 10 nM 48 h enhances cisplatin sensitivity  25944617
HCC827 Growth Inhibition Assay 10 nM 48 h enhances cisplatin sensitivity  25944617
RPMI 8226  Apoptosis Assay 4 nM 24/48 h induces cell apoptosis in a time-dependent manner 26000292
H929 Cell Survival Assay 2/4/6 nM 48 h induces a significant decrease in the cell growth 26000292
U266 Cell Survival Assay 2/4/6 nM 48 h induces a significant decrease in the cell growth 26000292
OPM2 Cell Survival Assay 2/4/6 nM 48 h induces a significant decrease in the cell growth 26000292
RPMI 8226 Cell Survival Assay 2/4/6 nM 48 h induces a significant decrease in the cell growth 26000292
G401 Function Assay 50/100 nM 24 h induces cell cycle disorder  26176219
SK-NEP-1 Function Assay 50/100 nM 24 h induces cell cycle disorder  26176219
G401 Function Assay 50/100 nM 24 h shows the induction of DNA fragmentation 26176219
SK-NEP-1 Function Assay 50/100 nM 24 h shows the induction of DNA fragmentation 26176219
G401 Apoptosis Assay 50/100 nM 24 h induces cell apoptosis in a dose-dependent manner 26176219
SK-NEP-1 Apoptosis Assay 50/100 nM 24 h induces cell apoptosis in a dose-dependent manner 26176219
G401 Cell Viability Assay 50 nM 1–4 d reduces cell survival in a time dependent manner 26176219
SK-NEP-1 Cell Viability Assay 50 nM 1–4 d reduces cell survival in a time dependent manner 26176219
G401 Growth Inhibition Assay 0.01–10.0 μM 24 h IC50=143.02 nM 26176219
SK-NEP-1 Growth Inhibition Assay 0.01–10.0 μM 24 h IC50=76.34 nM 26176219
NCI-H460  Growth Inhibition Assay 10/20/30 nM 72 h enhances the antiproliferative effect of erlotinib 26675484
A549  Growth Inhibition Assay 10/15/20 nM 72 h enhances the antiproliferative effect of erlotinib 26675484
HCC827 Growth Inhibition Assay 5/7.5/10 nM 72 h enhances the antiproliferative effect of erlotinib 26675484
HepG2 Function Assay 50 nM 24-72 h induced activation of caspase 3 after 24 h  26702784
HT29 Function Assay 50 nM 24-72 h induced activation of caspase 3 after 48 h  26702784
HepG2 Growth Inhibition Assay 0-10 μM 0-4 d inhibits cell growth in both time- and dose-dependent manner 26702784
HT29 Growth Inhibition Assay 0-10 μM 0-4 d inhibits cell growth in both time- and dose-dependent manner 26702784
SK-N-AS Function Assay 0–80 nM 48 h induces a dose-dependent cleavage of caspase 3 and PARP 24098799
SK-N-DZ Function Assay 0–80 nM 48 h induces a dose-dependent cleavage of caspase 3 and PARP 24098799
SK-N-SH Function Assay 0–40 nM 48 h induces a dose-dependent cleavage of caspase 3 and PARP 24098799
SK-N-BE Function Assay 0–40 nM 48 h induces a dose-dependent cleavage of caspase 3 and PARP 24098799
HCC-LM3 Growth Inhibition Assay 1-1000 nM 24/48/72 h inhibits cell growth in both time- and dose-dependent manner 24093956
HepG2 Growth Inhibition Assay 1-1000 nM 24/48/72 h inhibits cell growth in both time- and dose-dependent manner 24093956
SMMC-7721 Growth Inhibition Assay 1-1000 nM 24/48/72 h inhibits cell growth in both time- and dose-dependent manner 24093956
HCC-LM3 Apoptosis Assay 50 nM 48 h induces cell apoptosis significantly in a caspase-dependent manner by cleavage of caspases 3, 8 and 9 24093956
HepG2 Apoptosis Assay 50 nM 48 h induces cell apoptosis significantly in a caspase-dependent manner by cleavage of caspases 3, 8 and 9 24093956
SMMC-7721 Apoptosis Assay 50 nM 48 h induces cell apoptosis significantly in a caspase-dependent manner by cleavage of caspases 3, 8 and 9 24093956
HCC-LM3 Function Assay 50/100 nM 24 h decreases the levels of p-STAT3 and p-Akt  24093956
HepG2 Function Assay 50/100 nM 24 h decreases the levels of p-STAT3 and p-Akt  24093956
SMMC-7721 Function Assay 50/100 nM 24 h decreases the levels of p-STAT3 and p-Akt  24093956
HCC-LM3 Function Assay 50/100 nM 24 h downregulates Bcl-xL expression 24093956
HepG2 Function Assay 50/100 nM 24 h downregulates Bcl-xL expression 24093956
SMMC-7721 Function Assay 50/100 nM 24 h downregulates Bcl-xL expression 24093956
FaDu Growth Inhibition Assay 100 nM 8/10/12 h displayed a significant and prolonged G2/M arrest at 8 and 12 h post release 24026482
FaDu Function Assay 100 nM 2/4/8/12 h induced p21Waf1/Cip1 expression 24026482
PC-3  Growth Inhibition Assay 0-10 μM 24/48/72 h inhibits cell growth in both time- and dose-dependent manner 23991216
LNCaP Growth Inhibition Assay 0-5 μM 24/48/72 h inhibits cell growth in both time- and dose-dependent manner 23991216
RWPE-1  Growth Inhibition Assay 0-20 μM 24/48/72 h inhibits cell growth in both time- and dose-dependent manner 23991216
Capan-1 Function Assay 25/50/100 nM 8/24/48 h downregulated Ron mRNA and protein expression and downstream signaling 23922886
L3.6pl Function Assay 25/50/100 nM 8/24/48 h downregulated Ron mRNA and protein expression and downstream signaling 23922886
CFPAC-1  Function Assay 25/50/100 nM 8/24/48 h downregulated Ron mRNA and protein expression and downstream signaling 23922886
Capan-1 Growth Inhibition Assay 25/50/100 nM 48 h reduces cell growth in a dose-dependent manner 23922886
L3.6pl Growth Inhibition Assay 25/50/100 nM 48 h reduces cell growth in a dose-dependent manner 23922886
CFPAC-1  Growth Inhibition Assay 25/50/100 nM 48 h reduces cell growth in a dose-dependent manner 23922886
Capan-1 Apoptosis Assay 25/50/100 nM 48 h induces cell growth in a dose-dependent manner 23922886
L3.6pl Apoptosis Assay 25/50/100 nM 48 h induces cell growth in a dose-dependent manner 23922886
CFPAC-1  Apoptosis Assay 25/50/100 nM 48 h induces cell growth in a dose-dependent manner 23922886
HN22 Growth Inhibition Assay 0-20 nM 24/48 h inhibits cell viability in both time- and dose- dependent manner 23877235
HSC4  Growth Inhibition Assay 0-20 nM 24/48 h inhibits cell viability in both time- and dose- dependent manner 23877235
HN22 Apoptosis Assay 0-20 nM 48 h induces cell apoptosis 23877235
HSC4  Apoptosis Assay 0-20 nM 48 h induces cell apoptosis 23877235
HN22 Growth Inhibition Assay 0-20 nM 48 h induces G1 phase cell cycle arrest  23877235
HSC4  Growth Inhibition Assay 0-20 nM 48 h induces G1 phase cell cycle arrest  23877235
HN22 Function Assay 0-20 nM 48 h suppresses Sp1 expression  23877235
HSC4  Function Assay 0-20 nM 48 h suppresses Sp1 expression  23877235
U937 Function assay 1 uM 24 hrs Inhibition of HDAC6 in human U937 cells assessed as increase of intracellular acetylated alpha-tubulin level at 1 uM after 24 hrs by Western blot analysis 24694055
U937 Function assay 1 uM 24 hrs Inhibition of HDAC1 in human U937 cells assessed as increase of intracellular acetylated histone H3 level at 1 uM after 24 hrs by Western blot analysis 24694055
U937 Function assay 1 uM 24 hrs Inhibition of HDAC2 in human U937 cells assessed as increase of intracellular acetylated histone H3 level at 1 uM after 24 hrs by Western blot analysis 24694055
U937 Function assay 1 uM 24 hrs Inhibition of HDAC3 in human U937 cells assessed as increase of intracellular acetylated histone H4 level at 1 uM after 24 hrs by Western blot analysis 24694055
MV4-11 Function assay 10 to 1000 nM 6 hrs Inhibition of HDAC6 in human MV4-11 cells assessed as upregulation of alpha tubulin acetylation at 10 to 1000 nM after 6 hrs by Western blot analysis 26443078
HCT116 Function assay 10 to 1000 nM 6 hrs Inhibition of HDAC6 in human HCT116 cells assessed as upregulation of alpha tubulin acetylation at 10 to 1000 nM after 6 hrs by Western blot analysis 26443078
HCT116 Function assay 10 to 1000 nM 6 hrs Inhibition of HDAC1/2/3 in human HCT116 cells assessed as upregulation of histone H3 acetylation at 10 to 1000 nM after 6 hrs by Western blot analysis 26443078
MV4-11 Function assay 10 to 1000 nM 6 hrs Inhibition of HDAC1/2/3 in human MV4-11 cells assessed as upregulation of histone H3 acetylation at 10 to 1000 nM after 6 hrs by Western blot analysis 26443078
MV4-11 Function assay 50 nM 24 hrs Induction of HDAC6 degradation in human MV4-11 cells at 50 nM after 24 hrs by Western blot method 29589441
MV4-11 Function assay 50 nM 2 to 24 hrs Inhibition of HDAC6 in human MV4-11 cells assessed as induction of alpha-tubulin hyperacetylation at 50 nM after 2 to 24 hrs by Western blot method 29589441
MV4-11 Cell cycle arrest assay 30 to 50 nM 24 hrs Cell cycle arrest in human MV4-11 cells assessed as accumulation at sub-G1 phase at 30 to 50 nM after 24 hrs by propidium iodide staining-based flow cytometric method 29589441
MV4-11 Apoptosis assay 30 nM 24 to 48 hrs Induction of apoptosis in human MV4-11 cells at 30 nM after 24 to 48 hrs by Annexin V-PI staining based flow cytometry 29738953
SK-N-DZ Growth Inhibition Assay 24 h IC50=17.1 ± 0.4 nM 25308916
SK-N-AS Growth Inhibition Assay 24 h IC50=37.1 ± 2.4 nM 25308916
SK-N-BE (2), MK  PAN Growth Inhibition Assay 24 h IC50=382.0 ± 43.2 nM 25308916
SK-N-BE (2), PAN  MK Growth Inhibition Assay 24 h IC50=104.0 ± 7.8 nM 25308916
SK-N-BE (2) Growth Inhibition Assay 24 h IC50=104.0 ± 7.8 nM 25308916
HCT8 Growth Inhibition Assay 72 h IC50=12.9 ± 1.9 nM 23299388
H630 Growth Inhibition Assay 72 h IC50=12.4 ± 3.1 nM 23299388
cH630 5-FU-res Growth Inhibition Assay 72 h IC50=15.5 ± 1.2 nM 23299388
HCT116 Growth Inhibition Assay 72 h IC50=10.7 ± 2.2 nM 23299388
HCT116 p53−/− Growth Inhibition Assay 72 h IC50=8.6 ± 1.7 nM 23299388
dHCT116 p21−/− Growth Inhibition Assay 72 h IC50=5.9 ± 1.3 nM 23299388
HT29 Growth Inhibition Assay 72 h IC50=16.3 ± 2.3 nM 23299388
LoVo Growth Inhibition Assay 72 h IC50=5.1 ± 0.6 nM 23299388
RKO Growth Inhibition Assay 72 h IC50=7.9 ± 2.2 nM 23299388
SW480 Growth Inhibition Assay 72 h IC50=17.5 ± 0.8 nM 23299388
eSW620 Growth Inhibition Assay 72 h IC50=9.1 ± 2.1 nM 23299388
COLO205 Antiproliferative assay 96 hrs Antiproliferative activity against human COLO205 cells after 96 hrs by celltiter 96 assay, IC50 = 0.018 μM. 21634430
PC3 Antiproliferative assay 96 hrs Antiproliferative activity against human PC3 cells after 96 hrs by celltiter 96 assay, IC50 = 0.024 μM. 21634430
A2780 Antiproliferative assay 96 hrs Antiproliferative activity against human A2780 cells after 96 hrs by celltiter 96 assay, IC50 = 0.035 μM. 21634430
HCT116 Antiproliferative assay 96 hrs Antiproliferative activity against human HCT116 cells after 96 hrs by celltiter 96 assay, IC50 = 0.048 μM. 21634430
B16 Growth inhibition assay 48 hrs Growth inhibition of mouse B16 cells incubated for 48 hrs by MTT assay, GI50 = 0.15 μM. 23009203
HuH7 Cytotoxicity assay 3 days Cytotoxicity against human HuH7 cells assessed as inhibition of cell viability after 3 days by CellTiter 96 assay, CC50 = 0.0035 μM. 25490700
Sf9 Function assay 15 mins Inhibition of full length C-terminal His/FLAG-tagged human recombinant HDAC1 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured a, IC50 = 0.00126 μM. 27186676
Sf9 Function assay 15 mins Inhibition of full length C-terminal His-tagged human recombinant HDAC3/NCOR2 (395 to 489 residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substr, IC50 = 0.00227 μM. 27186676
MV4-11 Cytotoxicity assay 24 hrs Cytotoxicity against human MV4-11 cells assessed as growth inhibition after 24 hrs by MTT assay, IC50 = 0.00297 μM. 27186676
Sf9 Function assay 15 mins Inhibition of full length human recombinant HDAC2 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence a, IC50 = 0.00328 μM. 27186676
HCT116 Cytotoxicity assay 24 hrs Cytotoxicity against human HCT116 cells assessed as growth inhibition after 24 hrs by MTT assay, IC50 = 0.00336 μM. 27186676
Sf9 Function assay 15 mins Inhibition of full length human recombinant HDAC6 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence a, IC50 = 0.00416 μM. 27186676
Sf9 Inhibition of human 15 mins Inhibition of human recombinant HDAC10 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence assay, IC50 = 0.00445 μM. 27186676
Sf9 Function assay 15 mins Inhibition of full length C-terminal His-tagged human recombinant HDAC8 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after , IC50 = 0.00486 μM. 27186676
A2780S Cytotoxicity assay 24 hrs Cytotoxicity against human A2780S cells assessed as growth inhibition after 24 hrs by MTT assay, IC50 = 0.00832 μM. 27186676
A2780S Function assay 6 hrs Inhibition of HDAC6 in human A2780S cells assessed as tubulin acetylation incubated for 6 hrs by cytoblot assay, EC50 = 0.15071 μM. 27186676
A2780S Function assay 6 hrs Inhibition of HDAC1/2/3 in human A2780S cells assessed as histone H3 acetylation incubated for 6 hrs by cytoblot assay, EC50 = 0.1695 μM. 27186676
Sf9 Function assay 15 mins Inhibition of human recombinant HDAC5 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence assay, IC50 = 0.1903 μM. 27186676
Sf9 Function assay 15 mins Inhibition of N-terminal GST/C-terminal His-tagged human recombinant HDAC4 (627 to 1084 residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrat, IC50 = 0.3378 μM. 27186676
Sf9 Function assay 15 mins Inhibition of C-terminal His-tagged human recombinant HDAC9 (604 to 1066 residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition meas, IC50 = 0.8878 μM. 27186676
Sf9 Function assay 15 mins Inhibition of full length human recombinant HDAC11 expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measured after 1 hr by fluorescence , IC50 = 4.112 μM. 27186676
Sf9 Function assay 15 mins Inhibition of N-terminal GST-tagged human recombinant HDAC7 (518 to end residues) expressed in baculovirus infected insect Sf9 cells using Ac-peptide-AMC as substrate assessed as release of AMC preincubated for 15 mins followed by substrate addition measu, IC50 = 4.354 μM. 27186676
Sf9 Function assay 60 mins Inhibition full length human recombinant HDAC2 expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate after 60 mins by fluorescence assay, IC50 = 0.002 μM. 27377864
Sf9 Function assay 60 mins Inhibition of human recombinant HDAC6 expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate after 60 mins by fluorescence assay, IC50 = 0.002 μM. 27377864
Sf9 Function assay 60 mins Inhibition of N-terminal GST-tagged full length human recombinant HDAC5 expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate after 60 mins by fluorescen, IC50 = 0.092 μM. 27377864
Sf9 Function assay 60 mins Inhibition of C-terminal His-tagged full length human recombinant HDAC8 expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate after 60 mins by fluorescen, IC50 = 0.231 μM. 27377864
Sf9 Function assay 60 mins Inhibition of C-terminal His-tagged human recombinant HDAC9 (604 to 1066 residues) expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate after 60 mins by, IC50 = 2.68 μM. 27377864
Sf9 Function assay 60 mins Inhibition of N-terminal GST-tagged human recombinant HDAC7 (518 to end residues) expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate after 60 mins by , IC50 = 2.83 μM. 27377864
HEK293 Cytotoxicity assay 48 hrs Cytotoxicity against HEK293 cells after 48 hrs by resazurin assay, IC50 = 0.07 μM. 28241112
NFF Cytotoxicity assay 72 hrs Cytotoxicity against human NFF cells after 72 hrs by SRB assay, IC50 = 0.07 μM. 28241112
HUT78 Apoptosis assay 18 hrs Pro-apoptotic activity in human HUT78 cells after 18 hrs by caspase-Glo 3/7 assay, EC50 = 0.0043 μM. 30122227
NFF Cytotoxicity assay 72 hrs Cytotoxicity against human NFF cells after 72 hrs by sulforhodamine B assay, IC50 = 0.07 μM. 30245402
HEK293 Cytotoxicity assay 48 hrs Cytotoxicity against HEK293 cells after 48 hrs by resazurin dye based assay, IC50 = 0.07 μM. 30245402
M14 Apoptosis assay 24 to 48 hrs Induction of apoptosis human M14 cells assessed as caspase activity after 24 to 48 hrs using DEVD peptide as substrate by ApoTox-Glo triplex assay 24471466
Raji Cytotoxicity assay 24 hrs Cytotoxicity against human Raji cells assessed as growth inhibition after 24 hrs by MTT assay 27186676
Ramos Cytotoxicity assay 24 hrs Cytotoxicity against human Ramos cells assessed as growth inhibition after 24 hrs by MTT assay 27186676
U266 Cytotoxicity assay 24 hrs Cytotoxicity against human U266 cells assessed as growth inhibition after 24 hrs by MTT assay 27186676
RPMI8226 Cytotoxicity assay 24 hrs Cytotoxicity against human RPMI8226 cells assessed as growth inhibition after 24 hrs by MTT assay 27186676
HBL1 Cytotoxicity assay 24 hrs Cytotoxicity against human HBL1 cells assessed as growth inhibition after 24 hrs by MTT assay 27186676
MM1S Cytotoxicity assay 24 hrs Cytotoxicity against human MM1S cells assessed as growth inhibition after 24 hrs by MTT assay 27186676
OCI-LY1 Cytotoxicity assay 24 hrs Cytotoxicity against human OCI-LY1 cells assessed as growth inhibition after 24 hrs by MTT assay 27186676
SUDHL4 Cytotoxicity assay 24 hrs Cytotoxicity against human SUDHL4 cells assessed as growth inhibition after 24 hrs by MTT assay 27186676
THP89GFP Growth Inhibition Assay EC50=19.34 ± 6.43 nM 26563568
J89GFP Growth Inhibition Assay EC50=49.85 ± 12.65 nM 26563568
Cal62 Growth Inhibition Assay IC50=33 ± 4 nM 23824064
Hth7 Growth Inhibition Assay IC50=15 ± 2 nM 23824064
Hth83 Growth Inhibition Assay IC50=34 ± 5 nM 23824064
C643 Growth Inhibition Assay IC50=71 ± 10 nM 23824064
SW1736 Growth Inhibition Assay IC50=35 ± 8 nM 23824064
T241 Growth Inhibition Assay IC50=65 ± 7 nM 23824064
T351 Growth Inhibition Assay IC50=50 ± 10 nM 23824064
BHP2-7 Growth Inhibition Assay IC50=37 ± 6 nM 23824064
T238 Growth Inhibition Assay IC50=1,500 ± 200 nM 23824064
S2 Function assay Inhibition of Plasmodium falciparum HDAC1 expressed in Drosophila melanogaster S2 cells, IC50 = 0.0018 μM. 19317450
HEK293 Function assay Inhibition of HDAC3 (unknown origin) expressed in HEK293 cells using [3H]acetylated human histone H4 peptide as substrate by scintillation counting, IC50 = 0.0021 μM. 22344701
HEK293 Function assay Inhibition of HDAC1 (unknown origin) expressed in HEK293 cells using [3H]acetylated human histone H4 peptide as substrate by scintillation counting, IC50 = 0.0025 μM. 22344701
HEK293 Function assay Inhibition of HDAC6 (unknown origin) expressed in HEK293 cells using [3H]acetylated human histone H4 peptide as substrate by scintillation counting, IC50 = 0.011 μM. 22344701
SF21 Function assay Inhibition of flag-tagged HDAC2 (unknown origin) expressed in SF21 cells using [3H]acetylated human histone H4 peptide as substrate by scintillation counting, IC50 = 0.013 μM. 22344701
HEK293 Function assay Inhibition of HDAC4 (unknown origin) expressed in HEK293 cells using [3H]acetylated human histone H4 peptide as substrate by scintillation counting, IC50 = 0.2 μM. 22344701
SF9 Function assay Inhibition of his-strep-tagged HDAC8 (unknown origin) expressed in SF9 cells using [3H]acetylated human histone H4 peptide as substrate by scintillation counting, IC50 = 0.28 μM. 22344701
HeLa Function assay Inhibition of HDAC in human HeLa cells using Fluor de Lys as substrate by fluorescence assay, IC50 = 0.03 μM. 23639537
Sf9 Function assay Inhibition of C-terminal His-tagged and C-terminal FLAG-tagged full length human recombinant HDAC1 expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as substrate , IC50 = 0.001 μM. 27377864
Sf9 Function assay Inhibition of N-terminal GST-tagged and C-terminal His-tagged human recombinant HDAC4 (627 to 1084 residues ) expressed in baculovirus coexpressed in fall armyworm Sf9 cells using carboxyfluorescein (FAM)-labeled acetylated/ trifluoroacetylated peptide as, IC50 = 0.373 μM. 27377864
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生物活性

产品描述 Panobinostat (LBH589, NVP-LBH589)是一种新型的,广谱HDAC抑制剂,无细胞试验中IC50为5 nM。Panobinostat (LBH589) 可诱导自噬和凋亡。Panobinostat 可以有效地破坏体内 HIV 的潜伏期。Phase 3。
靶点
HDAC (MOLT-4 cells) [1] HDAC (Reh cells) [1]
5 nM 20 nM
体外研究(In Vitro)
体外研究活性 LBH589诱导MOLT-4和Reh细胞凋亡,这种作用具有时间和剂量依赖性。而且,LBH589作用于MOLT-4细胞比作用于Reh细胞更有效。LBH589明显阻止MOLT-4 和Reh细胞的生长,处理48小时,具有剂量依赖性。与对照组细胞相比,用LBH589处理的细胞,在细胞周期的G2/M期的细胞数量增多2到3倍。LBH589与组蛋白H3K9和H4K8的乙酰化作用相关,LBH589也降低c-Myc的表达水平,具有剂量依赖性。LBH589也增强p21的表达水平。最低剂量的LBH589(10 nM)处理Reh细胞,最初增强c-Myc的表达水平,之后一直降低c-Myc的表达水平。此外,LBH589促进mRNA水平的促凋亡和DNA修复基因的大量增多。在GADD45G启动子作用下,LBH589诱导乙酰化的组蛋白H3 和H4水平的增多。[1]此外, LBH589抑制非小细胞肺癌细胞系生长,如人类H1299,L55和A549,IC50分别为5,11和30 nM;间皮瘤细胞生长,如人类OK-6和 Ok-5,IC50分别为5和7 nM;及小细胞肺癌细胞系生长,如人类RG-1和LD-T,IC50分别为4和5 nM。[2]
细胞实验 细胞系 MOLT-4细胞和Reh(前体B细胞)
浓度 50 nM
孵育时间 48小时
方法 没有处理的细胞和LBH589处理的细胞[人类急性成淋巴细胞性白血病MOLT-4(T 细胞)和Reh(前体-B细胞)]用膜联蛋白V和碘化丙啶染色,然后加入膜联蛋白V-FITC细胞凋亡检测试剂盒I。通过流式细胞仪测定细胞凋亡和不能存活细胞的百分比。用CyAn ADP Violet细胞计数器收集至少5×104个细胞。根据所有的膜联蛋白V-阳性和膜联蛋白V/PI-阳性细胞细胞计算凋亡百分比,根据所有的膜联蛋白V-阳性和PI-阳性及膜联蛋白V/PI-阳性细胞计算细胞活力丢失百分比。
实验图片 检测方法 检测指标 实验图片 PMID
Western blot DNMT1 / EZH2 caspase-8 / cleaved caspase-8 / Sp1 c-Myc / IRF4 Ac-H3 / cleaved caspase-3 / CCND1 / ID1 / ID2 / ID3 / ID4 / Synaptophysin / NeuroD1 RAD51 / BRCA1 / CHK1 / RPL13a H3K9AC / H3K18AC / H3K56AC / H3 / H4K8AC / H4K16AC / H4 / p21 / p27 / cleaved PARP 19279403
Immunofluorescence Synaptophysin / NACM α-tubulin / Acetyl-α-tubulin BiP ATF4 IRE1α / S724-IRE1α 28915627
Growth inhibition assay Cell viability 27738323
体内研究(In Vivo)
体内研究活性 LBH589作用于患肺癌和间皮瘤动物模型,明显降低肿瘤生长,与对照组相比平均降低62%。LBH589作用于免疫活性鼠和严重联合免疫缺陷鼠效果差不多,说明LBH589抑制肿瘤生长与免疫学无关。LBH589按20 mg/kg剂量腹腔注射,每周持续5天,导致在实验最后肿瘤生长平均下降70%。与相应的对照组肿瘤相比,LBH589作用于H526衍生的肿瘤下降53%,作用于BK-T衍生的肿瘤下降81%, 作用于RG-1衍生的肿瘤下降76%,作用于H69衍生的肿瘤下降 70%。在相同条件和剂量的情况下,LBH589 作用于NSCLC和Meso衍生的移植瘤,导致SCLC衍生的肿瘤中有两种衰退,伴随着BK-T衍生的平均肿瘤尺寸从实验开始时的296 mm3降低到实验结束时的116 mm3,RG-1衍生的平均肿瘤尺寸从实验开始时的185mm3降低到实验结束时的86 mm3[2]
动物实验 Animal Models 携带10×106个M30细胞或5×106个A549细胞的SCID鼠
Dosages 10 mg/kg, 20 mg/kg
Administration 腹腔注射
NCT Number Recruitment Conditions Sponsor/Collaborators Start Date Phases
NCT04341311 Active not recruiting
Diffuse Intrinsic Pontine Glioma|Pediatric Brainstem Glioma|Pediatric Brainstem Gliosarcoma Recurrent|Pediatric Cancer|Pediatric Brain Tumor|Diffuse Glioma
Dana-Farber Cancer Institute|Celgene|Secura Bio Inc.
August 10 2020 Phase 1
NCT03632317 Withdrawn
Glioma|Diffuse Intrinsic Pontine Glioma
University of Michigan Rogel Cancer Center
October 2019 Phase 2
NCT03982134 Withdrawn
Melanoma|Non Small Cell Lung Cancer
Muhammad Furqan|Novartis Pharmaceuticals|University of Iowa
September 2019 Phase 1
NCT04326764 Terminated
Acute Myeloid Leukaemia (AML)|Myelodysplastic Syndromes (MDS)
Goethe University|Stichting Hemato-Oncologie voor Volwassenen Nederland|Polish Adult Leukemia Group|Schweizerische Arbeitsgemeinschaft für klinische Krebsforschung
July 24 2018 Phase 3
NCT03515915 Unknown status
Patients With Recurrent or Refractory Multiple Myeloma
University Hospital Montpellier|Poitiers University Hospital
April 23 2018 --

化学信息&溶解度

分子量 349.43 分子式

C21H23N3O2

CAS号 404950-80-7 SDF Download Panobinostat (LBH589) SDF
Smiles CC1=C(C2=CC=CC=C2N1)CCNCC3=CC=C(C=C3)C=CC(=O)NO
储存条件(自收到货起)

体外溶解度
批次:

DMSO : 70 mg/mL ( 200.32 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

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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常见问题及建议解决方法

问题 1:
How to reconstitute the compound for in vivo mice study?

回答:
We recommend the vehicle is 2 % DMSO, 2 % Tween 80, 48%PEG300, 48% water. The compound is first dissolved in DMSO, then add Tween, PEG300, water in sequence.

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