- OTS514
- HI TOPK 032
- XRP44X
- PF-3644022
| OTS964TOPK inhibitor,potent and selective |
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 = 98.00%
- COA (Certificate Of Analysis)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
| Cell experiment [2]: | |
Cell lines | AML-CD34+, MV4-11 and MOLM13 cell lines |
Preparation method | Soluble in DMSO > 10 mM. 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. |
Reaction Conditions | ~ 48 hours |
Applications | There is a significant decrease in the number of colonies per well in AML-CD34+ cells treated with 10 nM of OTS514 compared to untreated cells (41 vs 73, P = 0.01). OTS514 exhibits cytotoxic activity in AML cells but not in normal CD34+ cells. OTS514 also leads to 80% and 70% increase in apoptotic cell population in MV4-11 and MOLM13 cells that carried FLT3 mutations. |
| Animal experiment [1]: | |
Animal models | LU-99 xenografts (female BALB/cSLC-nu/nu Mice) |
Dosage form | Intravenously treated with liposomal OTS964 (40 mg/kg) |
Applications | OTS514 induces irregular cell morphology with cytokinesis defects and significantly increases the number of LU-99 cells with the “intercellular bridge” which is one of the markers indicating impaired cell division. |
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. Matsuo Y, Park JH2, Miyamoto T, et al. TOPK inhibitor induces complete tumor regression in xenograft models of human cancer through inhibition of cytokinesis. ci Transl Med. 2014 Oct 22;6(259):259ra145. 2. Alachkar H, Mutonga M, Malnassy G et al. T-LAK cell-originated protein kinase presents a novel therapeutic target in FLT3-ITD mutated acute myeloid leukemia. Oncotarget. 2015 Oct 20;6(32):33410-25. | |
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| Cas No. | 1338545-07-5 | SDF | Download SDF |
| Chemical Name | (R)-9-(4-(1-(dimethylamino)propan-2-yl)phenyl)-8-hydroxythieno[2,3-c]quinolin-4(5H)-one | ||
| Canonical SMILES | C[C@@H](CN(C)C)C1=CC=C(C2=C(O)C=CC3=C2C(C=CS4)=C4C(N3)=O)C=C1 | ||
| Formula | C22H22N2O2S | M.Wt | 378.49 |
| Solubility | Soluble in DMSO | Storage | Store at -20°C |
| Physical Appearance | A crystalline 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. | ||
OTS964{(R)-9-(4-(1-(dimethylamino)propan-2-yl)phenyl)-8-hydroxy-6-methylthieno[2,3-c] quinolin-4(5H)-one} is a potent TOPK inhibitor with an IC50 value of 28 nM. It is a dimethylated derivative of OTS514. OTS964 can inhibit TOPK kinase activity with high affinity and selectivity. TOPK (T-lymphokine-activated killer cell-originated protein kinase) is a protein that is found in a wide range of human cancers and is believed to work as an oncogene, promoting tumor growth.
It has been reported that OTS964 inhibited the growth of TOPK-positive cells with low IC50 values [A549 (31 nM), LU-99 (7.6 nM), DU4475 (53 nM), MDA-MB-231 (73 nM), T47D (72 nM), Daudi (25 nM), UM-UC-3 (32 nM), HCT-116(33nM), MKN1(38nM), MKN45(39nM), HepG2(19nM), MIAPaca-2 (30 nM), and 22Rv1 (50 nM)]. However, its growth inhibitory effect against TOPK-negative HT29 cancer cells was significantly weaker, with IC50 value of 290 nM. Intravenous administration of OTS964 at 40 mg/kg on days 1, 4, 8, 11, 15, and 18 to mice bearing LU-99 lung cancer cells, a TGI of 44% was observed on day 22 without any body weight loss. The differentiation of HSCs to amega-karyocyte population was also enhanced by OTS964 treatment 1.
References:1.Matsuo Y, Park JH2, Miyamoto T, et al. TOPK inhibitor induces complete tumor regression in xenograft models of human cancer through inhibition of cytokinesis. ci Transl Med. 2014 Oct 22;6(259):259ra145.
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(1)、分子内含有发射荧光的基团，如羰基、氮氮双键、碳氮双键等。
(2)、分子内含有助色基团。助色基团使光谱红移并增大荧光效率，如伯胺基、仲胺基、羟基、醚键、酰胺基等。
(3)、分子内含有刚性平面结构的共轭π键。分子内共轭体系愈大平面性愈强其荧光强度愈高。一些能提高共轭度的因素能提高荧光效率，并使荧光波长向长波方向移动。 就是荧光染料的附着物，主要作用有帮助荧光染料展色、提高荧光染料与下游树酯的相溶性、保护荧光染料的性能。通常载体树脂是强极性树脂，分子中含有胺基、羟基、醚键、酰胺基等强极性基团，一方面有助色作用，增大荧光效率;另一方面与荧光染料有很好的相溶性，有助于染料的均匀分散。
荧光颜料常用的载体树脂有胺基树脂、苯代三聚氰胺一甲醛树脂、聚丙烯酸酯树脂、聚酰胺树酯、聚酯树脂、聚氨酯树脂等。 （1）、热塑性荧光颜料：线型
（2）、热固性荧光颜料： 体型
（3）、可溶解色精荧光颜料
（4）、水乳型荧光颜料 （1）、胺基树酯
（2）、聚酰胺树酯
（3）、聚酯树酯
（4）、丙烯酸乳液 （1）、塑胶类
低温型
中温型
高温型
（2）、涂料类
水性涂料
油性涂料
粉末涂料 （1）、含甲醛
（2）、不含甲醛
颜料是用着色的物质通常与被着色的物质混合在一起主要以无机化合物为主；染料是一种用来直接或经媒染剂作用而能附着在各种纤维和其他材料上的有色物质有的可以跟被染物质化合，多以有机化合物为主。 颜料不能上色,而染料能上色. 颜料和染料的区别 颜料是一种微细粉末状的有色物质,一般不溶于水、油和溶剂,但能均匀的分散在其中。颜料是色漆的次要成膜物质,在木材装饰过程中调制底漆、腻子以及木才着色,也经常使用颜料.
然后是碱性荧光染料，造纸厂用来增加纸的亮度。
直接和分散的荧光黄，印染厂用来增加棉质和化纤面料的艳度
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我想用共聚焦观察间期染色体，用涂染探针，有一个问题很困扰我，我想涂染完染色后用DAPI复染细胞核，但是目前哈尔滨的共聚焦都没有紫外激发光，不能激发DAPI，我怎么才能实现，用红色涂一条染色体，用绿色涂另一条，用DAPI蓝色染核，同时成像呢，所说的双光子显微镜可以么？我实在很迷惑，求求版主别再删我的帖子，尽管我现在只是一个索取者，还不能给大家提供有用的信息，但是相信有一天会为大家做贡献的，谢谢了
