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Panobinostat

(CAS No:404950-80-7)
Panobinostat (LBH589) is a novel broad-spectrum HDAC inhibitor with IC50 of 5 nM in a cell-free assay. Phase 3.
CAS No:404950-80-7
Molecular Weight(MW):349.43
Purity:99.00%
Specification:500MG;1G;5G;10G;50G;100G
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QC Documents
　COA 　MSDS 　HPLC 　NMR
ChemicalInfomation
CAS No: 404950-80-7
Molecular formula(MF) C21H23N3O2
Molecular Weight(MW): 349.43
Alias
Solubility
In vitro DMSO 69 mg/mL (197.46 mM)
Water <1 mg/mL
Ethanol <1 mg/mL
In vivo 2% DMSO+48% PEG 300+2% Tween 80+ddH2O 5mg/mL
Biological Activity
Description Panobinostat (LBH589) is a novel broad-spectrum HDAC inhibitor with IC50 of 5 nM in a cell-free assay. Phase 3.
Targets
HDAC (MOLT-4 cells) [1] HDAC (Reh cells) [1]
5 nM 20 nM
In vitro

LBH589 induces apoptosis among MOLT-4 and Reh cells in a time- and dose-dependent manner. Moreover, LBH589 is more potent in MOLT-4 than in Reh cells. LBH589 markedly prevents the growth of both MOLT-4 and Reh cells in a dose-dependent manner at 48 hours. LBH589 treatment causes a 2- to 3-fold increase in the number of cells in the G2/M phase of the cell cycle compared with the control cells. LBH589 is associated with induction of histone H3K9 and histone H4K8 acetylation as well as decreasing levels of c-Myc expression in a dose-dependent manner. LBH589 treatment also increases the levels of p21 expression. LBH589 treatment also decreases the levels of c-Myc after an initial increase at the lowest dose (10 nM) in Reh cells. In addition, LBH589 gives rise to substantial increases in mRNA levels of proapoptosis and DNA repair genes. LBH589 induces increased levels of acetylated histone H3 and H4 at the GADD45G promoter. [1] Besides, LBH589 inhibits growth of non small cell lung cancer cell lines (such as human H1299, L55 and A549 with IC50 of 5 nM, 11 nM and 30 nM, respectively), mesothelioma (such as human OK-6 and Ok-5 with IC50 of 5 nM and 7 nM, respectively) and small cell lung cancer cell lines (such as human RG-1 and LD-T with IC50 of 4 nM and 5 nM, respectively). [2]
Cell Data
Cell Lines Assay Type Concentration Incubation Time Formulation Activity Description PMID
HT29 Growth Inhibition Assay 0-10 μM 0-4 d inhibits cell growth in both time- and dose-dependent manner 26702784
HepG2 Growth Inhibition Assay 0-10 μM 0-4 d inhibits cell growth in both time- and dose-dependent manner 26702784
HT29 Function Assay 50 nM 24-72 h induced activation of caspase 3 after 48 h  26702784
HepG2 Function Assay 50 nM 24-72 h induced activation of caspase 3 after 24 h  26702784
HCC827 Growth Inhibition Assay 5/7.5/10 nM 72 h DMSO enhances the antiproliferative effect of erlotinib 26675484
A549  Growth Inhibition Assay 10/15/20 nM 72 h DMSO enhances the antiproliferative effect of erlotinib 26675484
NCI-H460  Growth Inhibition Assay 10/20/30 nM 72 h DMSO enhances the antiproliferative effect of erlotinib 26675484
J89GFP Growth Inhibition Assay DMSO  EC50=49.85 ± 12.65 nM 26563568
THP89GFP Growth Inhibition Assay DMSO  EC50=19.34 ± 6.43 nM 26563568
SK-NEP-1 Growth Inhibition Assay 0.01–10.0 μM 24 h DMSO  IC50=76.34 nM 26176219
G401 Growth Inhibition Assay 0.01–10.0 μM 24 h DMSO  IC50=143.02 nM 26176219
SK-NEP-1 Cell Viability Assay 50 nM 1–4 d DMSO  reduces cell survival in a time dependent manner 26176219
G401 Cell Viability Assay 50 nM 1–4 d DMSO  reduces cell survival in a time dependent manner 26176219
SK-NEP-1 Apoptosis Assay 50/100 nM 24 h DMSO  induces cell apoptosis in a dose-dependent manner 26176219
G401 Apoptosis Assay 50/100 nM 24 h DMSO  induces cell apoptosis in a dose-dependent manner 26176219
SK-NEP-1 Function Assay 50/100 nM 24 h DMSO  shows the induction of DNA fragmentation 26176219
G401 Function Assay 50/100 nM 24 h DMSO  shows the induction of DNA fragmentation 26176219
SK-NEP-1 Function Assay 50/100 nM 24 h DMSO  induces cell cycle disorder  26176219
G401 Function Assay 50/100 nM 24 h DMSO  induces cell cycle disorder  26176219
RPMI 8226 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
U266 Cell Survival Assay 2/4/6 nM 48 h induces a significant decrease in the cell growth 26000292
H929 Cell Survival Assay 2/4/6 nM 48 h induces a significant decrease in the cell growth 26000292
RPMI 8226  Apoptosis Assay 4 nM 24/48 h induces cell apoptosis in a time-dependent manner 26000292
HCC827 Growth Inhibition Assay 10 nM 48 h DMSO enhances cisplatin sensitivity  25944617
NCI-H23 Growth Inhibition Assay 10 nM 48 h DMSO enhances cisplatin sensitivity  25944617
AML3 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
RPMI-8226vr10  Function Assay 0-1 μM 24 h induces DNA fragmentation in a dose-dependent manner 25612941
ML-1 Function Assay 1 μM 24 h increases caspase-3 activity 4-fold 25612941
RPMI-8226vr10  Function Assay 1 μM 24 h increases caspase-3 activity 2.5-fold 25612941
SK-N-BE (2) Growth Inhibition Assay 24 h IC50=104.0 ± 7.8 nM 25308916
SK-N-BE (2), PAN  MK Growth Inhibition Assay 24 h IC50=104.0 ± 7.8 nM 25308916
SK-N-BE (2), MK  PAN Growth Inhibition Assay 24 h IC50=382.0 ± 43.2 nM 25308916
SK-N-AS Growth Inhibition Assay 24 h IC50=37.1 ± 2.4 nM 25308916
SK-N-DZ Growth Inhibition Assay 24 h IC50=17.1 ± 0.4 nM 25308916
Caki-1 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
769-P Growth Inhibition Assay 10/25/50 nM 48 h inhibits cell growth in a dose dependent manner synergistically with 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
Caki-1 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
769-P Apoptosis Assay 50 nM 48 h induces cell apoptosis combined ritonavir 25279191
786-O  Apoptosis Assay 50 nM 48 h induces cell apoptosis combined ritonavir 25279191
Caki-1 Growth Inhibition Assay 25/50 nM 48 h DMSO inhibits cell growth in a dose dependent manner synergistically with bortezomib 25176354
ACHN Growth Inhibition Assay 25/50 nM 48 h DMSO inhibits cell growth in a dose dependent manner synergistically with bortezomib 25176354
769-P Growth Inhibition Assay 25/50 nM 48 h DMSO inhibits cell growth in a dose dependent manner synergistically with bortezomib 25176354
Caki-1 Colony Formation Assay 50 nM 7-14 d DMSO suppressed colony formation significantly combined with with bortezomib   25176354
ACHN Colony Formation Assay 50 nM 7-14 d DMSO suppressed colony formation significantly combined with with bortezomib   25176354
769-P Colony Formation Assay 50 nM 7-14 d DMSO suppressed colony formation significantly combined with with bortezomib   25176354
Caki-1 Apoptosis Assay 50 nM 48 h DMSO induces cell apoptosis 25176354
ACHN Apoptosis Assay 50 nM 48 h DMSO induces cell apoptosis 25176354
769-P Apoptosis Assay 50 nM 48 h DMSO induces cell apoptosis 25176354
MDA-MB-231 Morphological Crystal Violet (CV) Assay 10 nM 3 d DMSO alters cell morphology  24810497
BT-549 Morphological Crystal Violet (CV) Assay 10 nM 3 d DMSO alters cell morphology  24810497
MCF-7  Morphological Crystal Violet (CV) Assay 10 nM 3 d DMSO alters cell morphology  24810497
MCF-7 Function Assay 5-50 nM 24 h DMSO reduced the level of expression of ERα, PR and FoxA1  24366407
CTS 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
U937 Apoptosis Assay 0–40 nM  48 h induces apoptosis in a dose-dependent manner 24244429
PC3 Apoptosis Assay 0-100 nM 24/48 h induces apoptosis in a dose-dependent manner 24163230
PC3-AR Apoptosis Assay 0-100 nM 24/48 h induces apoptosis in both time- and dose-dependent manner 24163230
PC3 Growth Inhibition Assay 0-100 nM 24/48 h induces accumulation of subG1 population 24163230
PC3-AR Growth Inhibition Assay 0-100 nM 24/48 h induces cell cycle arrest in the G2M phase 24163230
PC3 Function Assay 0-100 nM 24 h suppresses expression of activated ATM, Akt and Erk1/2 protein 24163230
PC3-AR Function Assay 0-100 nM 24 h suppresses expression of activated ATM, Akt and Erk1/2 protein 24163230
OS-RC-2 Cell Viability Assay 0-1000 nM 24/48/72 h DMSO decreases cell viability in both time- and dose-dependent manner 24144737
OS-RC-2 Growth Inhibition Assay 50 nM 48 h DMSO induces G2/M arrest 24144737
OS-RC-2 Apoptosis Assay 50 nM 48 h DMSO induces cell apoptosis 24144737
SK-N-AS Growth Inhibition Assay 0–80 nM 48 h IC50=27.4 nM 24098799
SK-N-DZ Growth Inhibition Assay 0–80 nM 48 h IC50=21.9 nM 24098799
SK-N-SH Growth Inhibition Assay 0–80 nM 48 h IC50=72.3 nM 24098799
SK-N-BE Growth Inhibition Assay 0–80 nM 48 h IC50=75.4 nM 24098799
SK-N-AS Apoptosis Assay 0–80 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-SH Apoptosis Assay 0–40 nM 48 h potently induced apoptosis in a dose-dependent fashion 24098799
SK-N-BE Apoptosis Assay 0–40 nM 48 h potently induced apoptosis in a dose-dependent fashion 24098799
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 DMSO inhibits cell growth in both time- and dose-dependent manner 24093956
HepG2 Growth Inhibition Assay 1-1000 nM 24/48/72 h DMSO inhibits cell growth in both time- and dose-dependent manner 24093956
SMMC-7721 Growth Inhibition Assay 1-1000 nM 24/48/72 h DMSO inhibits cell growth in both time- and dose-dependent manner 24093956
HCC-LM3 Apoptosis Assay 50 nM 48 h DMSO 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 DMSO 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 DMSO 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 DMSO decreases the levels of p-STAT3 and p-Akt  24093956
HepG2 Function Assay 50/100 nM 24 h DMSO decreases the levels of p-STAT3 and p-Akt  24093956
SMMC-7721 Function Assay 50/100 nM 24 h DMSO decreases the levels of p-STAT3 and p-Akt  24093956
HCC-LM3 Function Assay 50/100 nM 24 h DMSO downregulates Bcl-xL expression 24093956
HepG2 Function Assay 50/100 nM 24 h DMSO downregulates Bcl-xL expression 24093956
SMMC-7721 Function Assay 50/100 nM 24 h DMSO 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 DMSO downregulated Ron mRNA and protein expression and downstream signaling 23922886
L3.6pl Function Assay 25/50/100 nM 8/24/48 h DMSO downregulated Ron mRNA and protein expression and downstream signaling 23922886
CFPAC-1  Function Assay 25/50/100 nM 8/24/48 h DMSO downregulated Ron mRNA and protein expression and downstream signaling 23922886
Capan-1 Growth Inhibition Assay 25/50/100 nM 48 h DMSO reduces cell growth in a dose-dependent manner 23922886
L3.6pl Growth Inhibition Assay 25/50/100 nM 48 h DMSO reduces cell growth in a dose-dependent manner 23922886
CFPAC-1  Growth Inhibition Assay 25/50/100 nM 48 h DMSO reduces cell growth in a dose-dependent manner 23922886
Capan-1 Apoptosis Assay 25/50/100 nM 48 h DMSO induces cell growth in a dose-dependent manner 23922886
L3.6pl Apoptosis Assay 25/50/100 nM 48 h DMSO induces cell growth in a dose-dependent manner 23922886
CFPAC-1  Apoptosis Assay 25/50/100 nM 48 h DMSO induces cell growth in a dose-dependent manner 23922886
HN22 Growth Inhibition Assay 0-20 nM 24/48 h DMSO inhibits cell viability in both time- and dose- dependent manner 23877235
HSC4  Growth Inhibition Assay 0-20 nM 24/48 h DMSO inhibits cell viability in both time- and dose- dependent manner 23877235
HN22 Apoptosis Assay 0-20 nM 48 h DMSO induces cell apoptosis 23877235
HSC4  Apoptosis Assay 0-20 nM 48 h DMSO induces cell apoptosis 23877235
HN22 Growth Inhibition Assay 0-20 nM 48 h DMSO induces G1 phase cell cycle arrest  23877235
HSC4  Growth Inhibition Assay 0-20 nM 48 h DMSO induces G1 phase cell cycle arrest  23877235
HN22 Function Assay 0-20 nM 48 h DMSO suppresses Sp1 expression  23877235
HSC4  Function Assay 0-20 nM 48 h DMSO suppresses Sp1 expression  23877235
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
HCT8 Growth Inhibition Assay 72 h DMSO IC50=12.9 ± 1.9 nM 23299388
H630 Growth Inhibition Assay 72 h DMSO IC50=12.4 ± 3.1 nM 23299388
cH630 5-FU-res Growth Inhibition Assay 72 h DMSO IC50=15.5 ± 1.2 nM 23299388
HCT116 Growth Inhibition Assay 72 h DMSO IC50=10.7 ± 2.2 nM 23299388
HCT116 p53−/− Growth Inhibition Assay 72 h DMSO IC50=8.6 ± 1.7 nM 23299388
dHCT116 p21−/− Growth Inhibition Assay 72 h DMSO IC50=5.9 ± 1.3 nM 23299388
HT29 Growth Inhibition Assay 72 h DMSO IC50=16.3 ± 2.3 nM 23299388
LoVo Growth Inhibition Assay 72 h DMSO IC50=5.1 ± 0.6 nM 23299388
RKO Growth Inhibition Assay 72 h DMSO IC50=7.9 ± 2.2 nM 23299388
SW480 Growth Inhibition Assay 72 h DMSO IC50=17.5 ± 0.8 nM 23299388
eSW620 Growth Inhibition Assay 72 h DMSO IC50=9.1 ± 2.1 nM 23299388

... Click to View More Cell Line Experimental Data
In vivo In lung cancer and mesothelioma animal models, LBH589 markedly decreases tumor growth by 62%. LBH589 is equally effective in immunocompetent and severe combined immunodeficien-cymice, suggesting that the inhibition of tumor growth by LBH589 is not due to direct immunologic effects. Daily LBH589, given i.p. at 20 mg/kg for 5 days per week, leading to an average decrease in growth of 70%. Compared with the corresponding control tumors, LBH589 leads to a 53% decrease for H526-derived tumors, an 81% decrease for BK-T-derived tumors, a 76% decrease for RG-1- derived tumors, and a 70% decrease for H69-derived tumors. In contrast to the lack of tumor regression notes in NSCLC and Meso-derived xenografted tumors that are treated under identical conditions and doses, LBH589 results in dramatic tumor regression in SCLC-derived tumors and RG-1-derived tumor. [2]
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