切换导航

UM 729

现货
Catalog No.
A8952
AhR拮抗剂的增强剂
组合的产品项目
规格价格库存 数量
10mM (in 1mL DMSO)
¥ 1,600.00
现货
5mg
¥ 1,380.00
现货
25mg
¥ 3,480.00
现货
100mg
¥ 6,980.00
现货

电话: 021-55669583

邮箱: sales@apexbio.cn

全球经销商

Background

UM729 is a small molecule enhancer of AhR antagonists [1].

UM729 has been found to be a new pyrimidoindole and have an additive efficacy with AhR antagonists in preventing differentiation in most AML specimen. In addition, UM729 has been reported to expand mormal HSPCs in a AhR-independent fashion. Moreover, UM729 has shown an additive effect with AhR inhibitors(SR1) on the ex vivo culture of primary human AML cells(05H163 cells) and progenitor cells [1]. Besides, UM729 has been revealed to expand HSCs and synergize with SR1 to enhance human HSC expansion, result in successful long-term engraftment of SCID repopulating cells (SRCs) in immunodeficient mice [2].

References:
[1] Pabst C1, Krosl J1, Fares I1, Boucher G1, Ruel R1, Marinier A2, Lemieux S3, Hébert J4, Sauvageau G4.Identification of small molecules that support human leukemia stem cell activity ex vivo. Nat Methods. 2014 Apr;11(4):436-42.
[2] Watts K L, Chandrasekaran D, Sauvageau G, et al. Effective Expansion and Engraftment Of Nonhuman Primate CD34+ Hematopoietic Stem Cells After Co-Culture With The Small Molecule UM171[J]. Blood, 2013, 122(21): 1656-1656.

Chemical Properties

Physical AppearanceA solid
StorageStore at -20°C
M.Wt367.44
Cas No.1448723-60-1
FormulaC20H25N5O2
Solubility≥36.7mg/mL in DMSO
Chemical Namemethyl 4-((3-(piperidin-1-yl)propyl)amino)-9H-pyrimido[4,5-b]indole-7-carboxylate
SDFDownload SDF
Canonical SMILESO=C(OC)C1=CC=C(C2=C(NCCCN3CCCCC3)N=CN=C2N4)C4=C1
运输条件试用装:蓝冰运输。 其他可选规格:常温运输或根据您的要求用蓝冰运输。
一般建议为了使其更好的溶解,请用37℃加热试管并在超声波水浴中震动片刻。不同厂家不同批次产品溶解度各有差异,仅做参考。若实验所需浓度过大至产品溶解极限,请添加助溶剂助溶或自行调整浓度。

试验操作

细胞实验 [1]:

细胞系

人类AML细胞

制备方法

可溶于DMSO。若配制更高浓度的溶液,一般步骤如下:请将试管置于37 °C加热10分钟和/或将其置于超声波浴中震荡一段时间。原液于-20 °C可放置数月。

反应条件

1 μM;4 天

实验结果

UM 729抑制AML细胞分化。在05H163细胞中,AhR抑制剂(类黄酮、苯并噻吩和β-咔啉)与UM 729联合用药增加CD34+CD15-细胞数量。在大多数AML样本中,UM 729增强AhR拮抗剂的细胞分化抑制作用。

动物实验 [1]:

动物模型

NSG小鼠

给药剂量

1 μM;静脉注射

实验结果

在NSG小鼠中,单独给予UM 729或同时给予UM 729和SR1促进AML细胞植入,但不提高白血病干细胞频率。

其它注意事项

请于室内测试所有化合物的溶解度。虽然化合物的实际溶解度可能与其理论值略有不同,但仍处于实验系统误差的允许范围内。

References:

[1]. Pabst C1, Krosl J1, Fares I1, Boucher G1, Ruel R1, Marinier A2, Lemieux S3, Hébert J4, Sauvageau G4.Identification of small molecules that support human leukemia stem cell activity ex vivo. Nat Methods. 2014 Apr;11(4):436-42.

质量控制

化学结构

UM 729