货号:A165763 同义名: LBH589;NVP-LBH589
Panobinostat (LBH589; NVP-LBH589) 是一种强效且口服活性的非选择性HDAC抑制剂,具有抗肿瘤活性。在低浓度(8-31 nM)下诱导HIV-1病毒的产生,并在潜伏感染的细胞中刺激HIV-1的表达。Panobinostat还诱导细胞凋亡和自噬,可用于研究难治性或复发性多发性骨髓瘤。
There will be a HazMat fee per item when shipping a dangerous goods. The HazMat fee will be charged to your UPS/DHL/FedEx collect account or added to the invoice unless the package is shipped via Ground service. Ship by air in Excepted Quantity (each bottle), which is up to 1g/1mL for class 6.1 packing group I or II, and up to 25g/25ml for all other HazMat items.
Type | HazMat fee for 500 gram (Estimated) |
Excepted Quantity | USD 0.00 |
Limited Quantity | USD 15-60 |
Inaccessible (Haz class 6.1), Domestic | USD 80+ |
Inaccessible (Haz class 6.1), International | USD 150+ |
Accessible (Haz class 3, 4, 5 or 8), Domestic | USD 100+ |
Accessible (Haz class 3, 4, 5 or 8), International | USD 200+ |
规格 | 价格 | 会员价 | 库存 | 数量 | |||
---|---|---|---|---|---|---|---|
{[ item.pr_size ]} |
{[ getRatePrice(item.pr_rmb, 1,1) ]} {[ getRatePrice(item.pr_rmb_sale, 1,1) ]} {[ suihuo_tips(item.pr_am, item.pr_size) ]} |
{[ getRatePrice(item.pr_rmb, 1,1) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,1) ]} {[ suihuo_tips(item.pr_am, item.pr_size) ]} |
{[ getRatePrice(item.pr_rmb, 1,1) ]}{[ suihuo_tips(item.pr_am, item.pr_size) ]} | {[ getRatePrice(item.pr_rmb_sale, 1,1) ]} {[ getRatePrice(item.pr_rmb,item.pr_rate,item.mem_rate) ]} {[ getRatePrice(item.pr_rmb,1,item.mem_rate) ]} | 现货 | 咨询 | - + |
快速发货 顺丰冷链运输,1-2 天到达
品质保证
技术支持
免费溶解
产品名称 | HD1 ↓ ↑ | HD2 ↓ ↑ | HDAC ↓ ↑ | HDAC1 ↓ ↑ | HDAC10 ↓ ↑ | HDAC11 ↓ ↑ | HDAC2 ↓ ↑ | HDAC3 ↓ ↑ | HDAC4 ↓ ↑ | HDAC5 ↓ ↑ | HDAC6 ↓ ↑ | HDAC7 ↓ ↑ | HDAC8 ↓ ↑ | HDAC9 ↓ ↑ | 其他靶点 | 纯度 | |||
---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|---|
Givinostat HCl monohydrate |
++++
HD1-A, IC50: 16 nM HD1-B, IC50: 7.5 nM |
+++
HD2, IC50: 10 nM |
99%+ | ||||||||||||||||
MC1568 |
++
HD1-A (Maize), IC50: 100 nM HD1-B (Maize), IC50: 3.4 μM |
96% | |||||||||||||||||
Trichostatin A |
++++
HDAC, IC50: ~1.8 nM |
99%+ | |||||||||||||||||
Scriptaid | ✔ | 99%+ | |||||||||||||||||
Valproic acid sodium | ✔ | Autophagy | 97% | ||||||||||||||||
AR-42 |
+++
HDAC, IC50: 30 nM |
99%+ | |||||||||||||||||
Dacinostat |
+++
HDAC, IC50: 32 nM |
98+% | |||||||||||||||||
CUDC-101 |
++++
HDAC, IC50: 4.4 nM |
++++
HDAC1, IC50: 4.5 nM |
+++
HDAC10, IC50: 26.1 nM |
+++
HDAC2, IC50: 12.6 nM |
++++
HDAC3, IC50: 9.1 nM |
+++
HDAC4, IC50: 13.2 nM |
+++
HDAC5, IC50: 11.4 nM |
++++
HDAC6, IC50: 5.1 nM |
+
HDAC7, IC50: 373 nM |
++
HDAC8, IC50: 79.8 nM |
++
HDAC9, IC50: 67.2 nM |
HER2,EGFR | 99%+ | ||||||
M344 |
++
HDAC, IC50: 100 nM |
99%+ | |||||||||||||||||
Splitomicin |
+
Sir2p, IC50: 60 μM |
95% | |||||||||||||||||
Panobinostat |
++++
HDAC (MOLT-4 cells), IC50: 5 nM HDAC (Reh cells), IC50: 20 nM |
98% | |||||||||||||||||
Sodium 4-Phenylbutyrate | ✔ | 98% | |||||||||||||||||
Vorinostat |
+++
HDAC, IC50: ~10 nM |
98% | |||||||||||||||||
Curcumin | ✔ | NF-κB,Nrf2 | 98% | ||||||||||||||||
Belinostat |
+++
HDAC, IC50: 27 nM |
98% | |||||||||||||||||
RG-2833 |
++
HDAC1, Ki: 32 nM |
++
HDAC3, Ki: 5 nM |
98% | ||||||||||||||||
Valproic acid |
+
HDAC1, IC50: 0.4 mM |
98% | |||||||||||||||||
BG45 |
+
HDAC1, IC50: 2 μM |
+
HDAC2, IC50: 2.2 μM |
+
HDAC3, IC50: 289 nM |
99%+ | |||||||||||||||
Entinostat |
+
HDAC1, IC50: 0.51 μM |
+
HDAC3, IC50: 1.7 μM |
98% | ||||||||||||||||
Resminostat |
+++
HDAC1, IC50: 42.5 nM |
++
HDAC3, IC50: 50.1 nM |
++
HDAC6, IC50: 71.8 nM |
98+% | |||||||||||||||
Romidepsin |
+++
HDAC1, IC50: 36 nM |
+++
HDAC2, IC50: 47 nM |
99%+ | ||||||||||||||||
Parthenolide | ✔ | NF-κB,p53 | 97% HPLC | ||||||||||||||||
Tacedinaline |
+
HDAC1, IC50: 0.9 μM |
+
HDAC2, IC50: 0.9 μM |
+
HDAC3, IC50: 1.2 μM |
98% | |||||||||||||||
Mocetinostat |
++
HDAC1, IC50: 0.15 μM |
+
HDAC11, IC50: 0.59 μM |
+
HDAC2, IC50: 0.29 μM |
+
HDAC3, IC50: 1.66 μM |
98% | ||||||||||||||
WT-161 |
++++
HDAC1, IC50: 8.35 nM |
+++
HDAC2, IC50: 15.4 nM |
++++
HDAC6, IC50: 0.4 nM |
99%+ | |||||||||||||||
Fimepinostat |
++++
HDAC1, IC50: 1.7 nM |
++++
HDAC10, IC50: 2.8 nM |
++++
HDAC11, IC50: 5.4 nM |
++++
HDAC2, IC50: 5.0 nM |
++++
HDAC3, IC50: 1.8 nM |
+++
HDAC6, IC50: 27 nM |
99%+ | ||||||||||||
Tucidinostat |
++
HDAC1, IC50: 95 nM |
++
HDAC10, IC50: 78 nM |
++
HDAC2, IC50: 160 nM |
++
HDAC3, IC50: 67 nM |
99%+ | ||||||||||||||
Santacruzamate A |
++++
HDAC2, IC50: 119 pM |
99%+ | |||||||||||||||||
(E,E)-RGFP966 |
++
HDAC3, IC50: 80 nM |
99%+ | |||||||||||||||||
LMK-235 |
+++
HDAC4, IC50: 11.9 nM |
++++
HDAC5, IC50: 4.2 nM |
99%+ | ||||||||||||||||
Tasquinimod | ✔ | 99%+ | |||||||||||||||||
CAY10603 |
++++
HDAC6, IC50: 2 pM |
98% | |||||||||||||||||
Tubastatin A |
+++
HDAC6, IC50: 15 nM |
98% | |||||||||||||||||
Tubacin |
++++
HDAC6, IC50: 4 nM |
99%+ | |||||||||||||||||
ACY-738 |
++++
HDAC6, IC50: 1.7 nM |
99%+ | |||||||||||||||||
Nexturastat A |
++++
HDAC6, IC50: 5 nM |
99%+ | |||||||||||||||||
BRD73954 |
+++
HDAC6, IC50: 36 nM |
++
HDAC8, IC50: 120 nM |
98% | ||||||||||||||||
Tubastatin A HCl |
+++
HDAC6, IC50: 15 nM |
+
HDAC8, IC50: 854 nM |
98% | ||||||||||||||||
PCI-34051 |
+++
HDAC8, IC50: 10 nM |
99%+ | |||||||||||||||||
Ricolinostat |
++
HDAC1, IC50: 58 nM |
++
HDAC2, IC50: 48 nM |
++
HDAC3, IC50: 51 nM |
++++
HDAC6, IC50: 4.7 nM |
++
HDAC8, IC50: 100 nM |
99%+ | |||||||||||||
Droxinostat |
+
HDAC3, IC50: 16.9 μM |
+
HDAC6, IC50: 2.47 μM |
+
HDAC8, IC50: 1.46 μM |
99%+ | |||||||||||||||
Abexinostat |
++++
HDAC1, Ki: 7 nM |
+++
HDAC10, IC50: 24 nM |
+++
HDAC2, Ki: 19 nM |
++++
HDAC3/SMRT, Ki: 8.2 nM |
+++
HDAC6, Ki: 17 nM |
+
HDAC8, IC50: 280 nM |
98%+ | ||||||||||||
Citarinostat |
+++
HDAC1, IC50: 35 nM |
+++
HDAC2, IC50: 45 nM |
+++
HDAC3, IC50: 46 nM |
++++
HDAC6, IC50: 2.6 nM |
++
HDAC8, IC50: 137 nM |
99%+ | |||||||||||||
HPOB |
+
HDAC1, IC50: 2.9 μM |
+
HDAC10, IC50: 3.0 μM |
+
HDAC2, IC50: 4.4 μM |
+
HDAC3, IC50: 1.7 μM |
++
HDAC6, IC50: 56 nM |
+
HDAC8, IC50: 2.8 μM |
97% | ||||||||||||
Quisinostat 2HCl |
++++
HDAC1, IC50: 0.11 nM |
++++
HDAC10, IC50: 0.46 nM |
++++
HDAC11, IC50: 0.37 nM |
++++
HDAC2, IC50: 0.33 nM |
++++
HDAC3, IC50: 4.86 nM |
++++
HDAC4, IC50: 0.64 nM |
++++
HDAC5, IC50: 3.69 nM |
++++
HDAC8, IC50: 4.26 nM |
99+% | ||||||||||
Domatinostat |
+
HDAC1, IC50: 1.20 μM |
+
HDAC10, IC50: 21 μM |
+
HDAC11, IC50: 9.7 μM |
+
HDAC2, IC50: 1.12 μM |
+
HDAC3, IC50: 0.57 μM |
+
HDAC5, IC50: 11.3 μM |
+
HDAC9, IC50: 50 μM |
99%+ | |||||||||||
TMP269 |
++
HDAC4, IC50: 157 nM |
++
HDAC5, IC50: 97 nM |
+++
HDAC7, IC50: 43 nM |
+++
HDAC9, IC50: 23 nM |
99%+ | ||||||||||||||
Pracinostat |
++
HDAC1, IC50: 49 nM |
+++
HDAC10, IC50: 40 nM |
++
HDAC11, IC50: 93 nM |
++
HDAC2, IC50: 96 nM |
+++
HDAC3, IC50: 43 nM |
++
HDAC4, IC50: 56 nM |
+++
HDAC5, IC50: 47 nM |
+
HDAC6, IC50: 1.008 μM |
++
HDAC7, IC50: 137 nM |
++
HDAC8, IC50: 140 nM |
++
HDAC9, IC50: 70 nM |
99%+ | |||||||
TMP195 |
++
HDAC4, Ki: 59 nM |
++
HDAC5, Ki: 60 nM |
+++
HDAC7, Ki: 26 nM |
+++
HDAC9, Ki: 15 nM |
99%+ | ||||||||||||||
1. 鼠标悬停在“+”上可以显示相关IC50的具体数值。"+"越多,抑制作用越强。2. "✔"表示该化合物对相应的亚型有抑制作用,但抑制强度暂时没有相关数据。 |
靶点 |
|
描述 | HDACs (Histone deacetylases) are a group of enzymes that remove acetyl groups and regulate the histone tail, protein-DNA interaction, chromatin conformation, and even transcription. There are 18 mammalian HDACs divided into four classes: class I (HDACs 1, 2, 3, 8), class II (HDACs 4, 5, 6, 7, 9, 10), class III (sirtuin family: sirt1-sirt7) and class IV (HDAC 11)[1]. Panobinostat, also called as LBH-589 or NVP-LBH589, is broad-spectrum HDAC inhibitor with hydroxamate-based structure (IC50 value measured by cell-free assay not tested). A maximum effect of 85% apoptosis with 20 nM panobinostat in MOLT-4 cells and 80% apoptosis with 50 nM panobinostat in Reh cells can observed at 72h. Panobinostat can inhibit proliferation and cell-cycle progression in the two ALL cells. IC50 of panobinostat in anti-proliferation of MOLT-4 cells is approximately 5 nM and for Reh cells is approximately 20 nM. Compared with the control cells, panobinostat treatment for 24h (up to 50 nM) caused a 2- to 3-fold increase in the number of cells in the G2/M phase. Like other HDAC pan inhibitors, the hyperacetylation of H3K9 and H4K8, which are the biomarkers for the inhibition of class 1 HDACs, can be observed in MOLT-4 cells treated with panobinostat (10 - 50 nM) for 24h in a dose-dependent manner. Accompanied by that, the induction of p21 and p27 expression, as well as a decrease of c-Myc expression can also be found in the same time with 10 - 20 nM panobinostat. Echoing to the cell-arrest and growth inhibition, the apoptosis and DNA damage response genes, like GADD45A, GADD45B, GADD45G, FANCG, and FOXO3A can be increased robustly in the ALL cells after treatment with 50 nM panobinostat for 24h. These suggest that the growth inhibition effect of panobinostat may due to the apoptosis and DNA damage response caused by HDACs inhibition[2]. Panobinostat in combination with bortezomiband dexamethasone is approved by FDA for the treatment for patients with multiple myeloma who receive prior treatment with bortezomib and an immunomodulatory (IMiD) agent[3]. |
作用机制 | Panobinostat has hydroxamate-based structure, which can chelate the Zn2+ ion of HDACs[2]. |
细胞系 | 浓度 | 检测类型 | 检测时间 | 活动说明 | 数据源 |
769-P | 10/25/50 nM | Growth Inhibition Assay | 48 h | inhibits cell growth in a dose dependent manner synergistically with ritonavir | 25279191 |
769-P | 50 nM | Apoptosis Assay | 48 h | induces cell apoptosis combined ritonavir | 25279191 |
769-P | 25/50 nM | Growth Inhibition Assay | 48 h | inhibits cell growth in a dose dependent manner synergistically with bortezomib | 25176354 |
769-P | 50 nM | Colony Formation Assay | 7-14 d | suppressed colony formation significantly combined with with bortezomib | 25176354 |
Dose | Mice[4] (i.p.): 5 mg/kg- 20 mg/kg |
Administration | i.p. |
Pharmacokinetics |
NCT号 | 适应症或疾病 | 临床期 | 招募状态 | 预计完成时间 | 地点 |
NCT02506959 | Plasma Cell Leukemia ... 展开 >> Plasmacytoma Recurrent Plasma Cell Myeloma Refractory Plasma Cell Myeloma 收起 << | Phase 2 | Recruiting | September 14, 2019 | United States, Texas ... 展开 >> M D Anderson Cancer Center Recruiting Houston, Texas, United States, 77030 Contact: Yago L. Nieto 713-792-8750 ynieto@mdanderson.org Principal Investigator: Yago L. Nieto 收起 << |
NCT00449761 | Leukemia, Myeloid, Chronic | Phase 2 Phase 3 | Completed | - | - |
NCT01055483 | Acute Myeloid Leukemia | Phase 1 | Completed | - | France ... 展开 >> Novartis Investigative Site Paris Cedex 4, France, 75181 Novartis Investigative Site Paris, France, 75475 Germany Novartis Investigative Site Dresden, Germany, 01307 Novartis Investigative Site Frankfurt, Germany, 60590 Novartis Investigative Site Hannover, Germany, 30625 Novartis Investigative Site Ulm, Germany, 89081 收起 << |
计算器 | ||||
存储液制备 | 1mg | 5mg | 10mg | |
1 mM 5 mM 10 mM |
2.86mL 0.57mL 0.29mL |
14.31mL 2.86mL 1.43mL |
28.62mL 5.72mL 2.86mL |
CAS号 | 404950-80-7 |
分子式 | C21H23N3O2 |
分子量 | 349.43 |
别名 | LBH589;NVP-LBH589 |
运输 | 蓝冰 |
存储条件 |
液体 -20°C:3-6个月-80°C:12个月 粉末 Keep in dark place,Inert atmosphere,Store in freezer, under -20°C |
溶解度 |
DMSO: 105 mg/mL(300.49 mM),注意:DMSO长时间开封后,会吸水并导致溶解能力下降,请避免使用长期开封的DMSO |
动物实验配方 |
IP 2% DMSO+2% Tween80+30% PEG300+water 9 mg/mL clear PO 0.5% CMC-Na 50 mg/mL suspension |