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Panobinostat lactate

(Synonyms: LBH589 lactate; NVP-LBH589 lactate) 目录号 : GC74758

Panobinostat lactate 是一种有效的口服非选择性 HDAC 抑制剂,具有抗肿瘤活性。Panobinostat lactate 可有效干扰HIV潜伏期。Panobinostat lactate 诱导细胞凋亡 (apoptosis) 和自噬 (autophagy)。Panobinostat lactate 可用于难治性或复发性多发性骨髓瘤的研究。

Panobinostat lactate Chemical Structure

Cas No.:960055-56-5

规格 价格 库存 购买数量
10mM (in 1mL DMSO)
¥2,663.00
现货
1 mg
¥1,251.00
现货
5 mg
¥2,754.00
现货
10 mg
¥4,689.00
现货

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Sample solution is provided at 25 µL, 10mM.

Description

Panobinostat lactate is a potent and orally active non-selective HDAC inhibitor. Panobinostat lactate has antineoplastic activities. Panobinostat lactate effectively disrupts HIV latency. Panobinostat lactate induces cell apoptosis and autophagy. Panobinostat lactate can be used for the study of refractory or relapsed multiple myeloma[1][2][3][4][5].

Panobinostat lactate induces apoptosis of both MOLT-4 and Reh cells in a time- and dose-dependent manner. Panobinosta lactate results in histone (H3K9 and H4K8) hyperacetylation and regulation of cell-cycle control genes in Reh cells[1]. Panobinostat lactate exhibites potent antiproliferative activity in human NSCLC cell lines with the IC50 ranging from 5 to 100 nM[2].

Panobinosta lactate (10, 20 mg/kg, i.p.) significantly slows tumor growth derived from Meso and NSCLC cells in vivo models. Panobinosta lactate markedly increases acetylation of histone H3 and H4 of H69 human SCLC cells harvest from SCID mice[2]. Panobinostat lactate (5, 10 and 20 mg/kg i.p.) demonstrates a clear benefit of decreased tumor burden, significantly improves TTE and reduces bone density loss in a disseminated multiple myeloma mouse model[3].

References:
[1]. Scuto A, et al. The novel histone deacetylase inhibitor, LBH589, induces expression of DNA damage response genes and apoptosis in Ph- acute lymphoblastic leukemia cells. Blood. 2008 May 15;111(10):5093-100.
[2]. Crisanti MC, et al. The HDAC inhibitor panobinostat (LBH589) inhibits mesothelioma and lung cancer cells in vitro and in vivo with particular efficacy for small cell lung cancer. Mol Cancer Ther. 2009 Aug;8(8):2221-31.
[3]. Ocio EM, et al. In vitro and in vivo rationale for the triple combination of panobinostat (LBH589) and dexamethasone with either bortezomib or lenalidomide in multiple myeloma. Haematologica. 2010 May;95(5):794-803.
[4]. Banerjee NS, et al. Vorinostat, a pan-HDAC inhibitor, abrogates productive HPV-18 DNA amplification. Proc Natl Acad Sci U S A. 2018 Nov 20;115(47):E11138-E11147.
[5]. Barton K, et al. Broad activation of latent HIV-1 in vivo. Nat Commun. 2016;7:12731. Published 2016 Sep 8.

化学性质

Cas No. 960055-56-5 SDF
别名 LBH589 lactate; NVP-LBH589 lactate
分子式 C24H29N3O5 分子量 439.5
溶解度 DMSO: 100 mg/mL (227.53 mM; Need ultrasonic) 储存条件 4°C, sealed storage, away from moisture
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溶解性数据

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1 mg 5 mg 10 mg
1 mM 2.2753 mL 11.3766 mL 22.7531 mL
5 mM 0.4551 mL 2.2753 mL 4.5506 mL
10 mM 0.2275 mL 1.1377 mL 2.2753 mL
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