| ACY-241Selective and orally active HDAC6 inhibitor |
Sample solution is provided at 25 µL, 10mM.
Nature.2017 Jan 19;541(7637):417-420.
Nature.2018 Nov;563(7731):407-411.Nature.2018 Jun 13.Nature.2018 Jun 27.Nature.2018 Mar 29;555(7698):673-677.Nature.2017 Sep 7;549(7670):96-100.Nature.2016 Apr 21;532(7599):398-401.
Science.2016 Aug 5;353(6299)594-8Nat Nanotechnol.2017 Dec;12(12):1190-1198.Nature Biotechnology.2017 Jun;35(6):569-576Nat Med.2018 Sep 17.Cell.2018 Dec 21. pii: S0092-8674(18)31561-7.Cell.Available online 25 October 2018.Cell.2018 Sep 27. pii: S0092-8674(18)31183-8.Cell.2018 Jun 28;174(1):172-186.e21.Cell.2018 Feb 22;172(5):1007-1021.e17.Cell.2017 Nov 30;171(6):1284-1300.e21.Cell.2017 Aug 17. pii: S0092-8674(17)30869-3.Cell.2017 Jul 13;170(2):312-323Nat Med.2018 Jan 29.Nat Med.2017 Nov;23(11):1342-1351.Cell.2017 Apr 6;169(2):286-300.Cell.2015 Aug 27;162(5):987-1002.Cell.2015 Feb 12;160(4):729-44.Nature Medicine.2017 Apr;23(4):493-500.Cancer Cell.2018 May 14;33(5):905-921.e5.Cancer Cell.2018 Apr 9;33(4):752-769.e8.Cancer Cell.2018 Mar 12;33(3):401-416.e8.Cancer Cell.2017 Aug 14;32(2):253-267.e5.Nat Methods.2018 Jul;15(7):523-526.Cell Stem Cell.2018 May 3;22(5):769-778.e4.Cell Stem Cell.2017 Nov 20. pii: S1934-5909(17)30375-2.Quality Control & MSDS
- View current batch:
- Purity = 98.72%
- COA (Certificate Of Analysis)
- HPLC
- NMR (Nuclear Magnetic Resonance)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
| Cell experiment [1]: | |
Cell lines | A2780 ovarian cancer cells |
Preparation method | The solubility of this compound in DMSO is >23.4mg/mL. General tips for obtaining a higher concentration: Please warm the tube at 37℃ for 10 minutes and/or shake it in the ultrasonic bath for a while. Stock solution can be stored below -20℃ for several months. |
Reacting condition | 0.1, 0.3, 0.5, 1. 3 μM; dissolved in DMSO; 24 h |
Applications | In A2780 ovarian cancer cells, ACY-241 (0.3 μM) increased hyperacetylation of α-tubulin, consistent with inhibition of the tubulin deacetylase HDAC6. Hyperacetylation of histone H3, a target of Class I HDACs, was only observed at doses above 1 μM. ACY-241 preferentially induced hyperacetylation of α-tubulin relative to H3K56. |
| Animal experiment [1]: | |
Animal models | female athymic nude mice bearing MiaPaCa-2 pancreatic cancer xenografts |
Dosage form | ACY-241: 50 mg/kg once daily for five days, followed by two days off, for three consecutive weeks; intraperitoneal injectionPaclitaxel: 10 mg/kg once daily for five consecutive days; intraperitoneal injection |
Application | In female athymic nude mice bearing MiaPaCa-2 pancreatic cancer xenografts, ACY-241 (50 mg/kg) plus paclitaxel (10 mg/kg) inhibited tumor growth and did not result in body weight loss. ACY-241 was well tolerated in mice when dosed as a single agent and in combination with paclitaxel. |
Other notes | Please test the solubility of all compounds indoor, and the actual solubility may slightly differ with the theoretical value. This is caused by an experimental system error and it is normal. |
References: [1]. Huang P, Almeciga-Pinto I, Jordan M, et al. Selective HDAC inhibition by ACY-241 enhances the activity of paclitaxel in solid tumor models. In: Proceedings of the 2015 AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics; 2015 Nov 5-9; Boston, Massachusetts. Philadelphia (PA): AACR | |
ACY-241 Dilution Calculator
calculate
ACY-241 Molarity Calculator
calculate
| Cas No. | 1316215-12-9 | SDF | Download SDF |
| Chemical Name | (Z)-2-((2-chlorophenyl)(phenyl)amino)-N-((Z)-7-hydroxy-7-(hydroxyimino)heptyl)pyrimidine-5-carbimidic acid | ||
| Canonical SMILES | ClC1=CC=CC=C1N(C2=NC=C(/C(O)=N/CCCCCC/C(O)=N/O)C=N2)C3=CC=CC=C3 | ||
| Formula | C24H26ClN5O3 | M.Wt | 467.95 |
| Solubility | ≥23.4mg/mL in DMSO | Storage | Store at -20°C |
| Physical Appearance | A solid | Shipping Condition | Evaluation sample solution : ship with blue ice.All other available size:ship with RT , or blue ice upon request |
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. | ||
ACY-241 is a new, selective and orally available inhibitor of HDAC6 [1][2].
Histone deacetylase 6 (HDAC6) is an enzyme that removes acetyl groups from an ε-N-acetyl lysine on a histone, allowing the histones to wrap the DNA more tightly. HDAC6 plays an important role in transcriptional regulation and cell cycle progression.
ACY-241 is a new, selective and orally available HDAC6 inhibitor. In MM and MCL cells, the addition of ACY-241 to either lenalidomide (len) or pomalidomide (pom) resulted in synergistic increases in apoptosis and further reduced the expression of transcription factors MYC and IRF4 [1]. In multiple solid tumor cell lines, combination treatment with ACY-241 and paclitaxel resulted in enhanced inhibition of cell proliferation and increased cell death, compared with either single agent alone [2].
In MM xenograft model, combination treatment with ACY-241 and pomalidomide was well tolerated with no overt toxicity and significantly extended survival [1]. In xenograft models of pancreatic and ovarian cancer, combination treatment with ACY-241 and paclitaxel significantly increased mitotic cells with multipolar spindles. ACY-241 dose-dependently increased α-tubulin hyperacetylation [2].
References:[1]. Quayle SN, Almeciga-Pinto I, Tamang D, et al. Selective HDAC inhibition by ricolinostat (ACY-1215) or ACY-241 synergizes with IMiD® immunomodulatory drugs in Multiple Myeloma (MM) and Mantle Cell Lymphoma (MCL) cells. In: Proceedings of the 106th Annual Meeting of the American Association for Cancer Research, 2015, Philadelphia, PA. Philadelphia (PA): AACR; Cancer Res 2015;75(15 Suppl):Abstract nr 5380. [2]. Huang P, Almeciga-Pinto I, Jordan M, et al. Selective HDAC inhibition by ACY-241 enhances the activity of paclitaxel in solid tumor models. In: Proceedings of the 2015 AACR-NCI-EORTC International Conference on Molecular Targets and Cancer Therapeutics; 2015 Nov 5-9; Boston, Massachusetts. Philadelphia (PA): AACR
ebiomall.com
>
>
>
>
>
>
>
>
>
>
>
>
（1）确定抗体的名字，注意中英文名字、别名、亚型等信息。
（2）确定您的实验类型，Elisa，WB，IHC，ICC，或者是FACS。每种抗体说明书都会列出抗体经验证过适用的实验类型，如果抗体说明书没有提及的应用类型，并不意味着该抗体不适用于此种分析应用类型，而仅是说明尚未经过此种实验验证。
（3）确定实验样本的种属，Human，Mouse，Rat等。我们的抗体说明书都列出该抗体验证过的适用物种，可根据说明书列出已验证的种属来选择适合你实验的抗体。
（4）样本抗原蛋白的结构性质。了解样本抗原蛋白的结构性质有助于选择最合适的抗体，待测样本蛋白的结构域和样本在提取和处理过程中是否会变性，蛋白空间构象的改变，会影响抗体的免疫亲和反应。
（5）单多克隆抗体的选择。一般单克隆抗体特异性强，但亲和力相对小，检测抗原灵敏度相对就低；而多克隆抗体特异性稍弱，但抗体的亲和力强，灵敏度高，但易出现非特异性染色（可以通过封闭等避免）。
2. 二抗选择
（1）种属来源。主要根据一抗种属来源而决定二抗来源，如一抗是小鼠来源，那二抗就买抗小鼠的即可（羊、兔等均可）。
（2）标记物的选择。有HRP、Biotin、荧光素等标记物。免疫组化，WB二抗主要选择HRP，Biotin标记的二抗，而免疫荧光染色可按实验需要选择不同荧光素标记的二抗，如FITC、Cy3、PE等。
确定了需要检测样品的种属，就可以选择对应的一抗
而二抗是根据一抗来选择的，比如一抗是小鼠来源的，二抗就要是抗小鼠的
羊抗兔IgG抗体同理。
不过现在的技术发达了，为了大批量生产抗体，大多数都是通过单克隆技术完成的。
PS：你的IGg的写法有误，应为IgG或者IgM。。。
