I-BRD9
目录号 : GC12588
A BRD9 bromodomain inhibitor
Cas No.:1714146-59-4
Sample solution is provided at 25 µL, 10mM.
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pIC50: 7.3
I-BRD9 is a BRD9 inhibitor.
BRD9 is identified as a bromodomain containing protein forming a small sub-branch of the bromodomain family tree. Human BRD9 has a single bromodomain and contains five isoforms which are produced by alternative splicing.
In vitro: In previous study, the I-BRD9 development was driven by iterative medicinal chemistry, using structure based design to result in nanomolar potency at BRD9, over 700-fold selectivity against the BET family as well as more than 70-fold to a panel of 34 bromodomains. In Kasumi-1 cells, I-BRD9 could downregulate DUSP6, CLEC1, SAMSN1 and FES genes. Moreover, I-BRD9 was used to expore genes regulated by BRD9 in Kasumi-1 cells involved in immune response and oncology pathways. In addition, when BRD4 was used as a representative member of the BET family for initial selectivity screening, I-BRD9 was found to have a pIC50 of 5.3 against this protein. I-BRD9 thus represented the first available selective tool compound to investigate the cellular phenotype of the inhibition of BRD9 bromodomain [1].
In vivo: So far, there is no animal in vivo data reported for I-BRD9.
Clinical trial: Up to now, I-BRD9 is still in the preclinical development stage.
Reference:
[1] Theodoulou NH et al. Discovery of I-BRD9, a Selective Cell Active Chemical Probe for Bromodomain Containing Protein 9 Inhibition. J Med Chem. 2016 Feb 25;59(4):1425-39.
| Cas No. | 1714146-59-4 | SDF | |
| 化学名 | N-(1,1-dioxidotetrahydro-2H-thiopyran-4-yl)-5-ethyl-4-oxo-7-(3-(trifluoromethyl)phenyl)-4,5-dihydrothieno[3,2-c]pyridine-2-carboximidamide | ||
| Canonical SMILES | N=C(C(S1)=CC2=C1C(C3=CC=CC(C(F)(F)F)=C3)=CN(CC)C2=O)NC(CC4)CCS4(=O)=O | ||
| 分子式 | C22H22F3N3O3S2 | 分子量 | 497.55 |
| 溶解度 | DMF: 30 mg/mL,DMF:PBS(pH 7.2)(1:1): 0.5 mg/mL,DMSO: 25 mg/mL | 储存条件 | Store at -20°C |
| General tips | 请根据产品在不同溶剂中的溶解度选择合适的溶剂配制储备液；一旦配成溶液，请分装保存，避免反复冻融造成的产品失效。 储备液的保存方式和期限：-80°C 储存时，请在 6 个月内使用，-20°C 储存时，请在 1 个月内使用。 为了提高溶解度，请将管子加热至37℃，然后在超声波浴中震荡一段时间。 |
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| Shipping Condition | 评估样品解决方案：配备蓝冰进行发货。所有其他可用尺寸：配备RT，或根据请求配备蓝冰。 | ||
| 制备储备液 | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.0098 mL | 10.0492 mL | 20.0985 mL |
| 5 mM | 0.402 mL | 2.0098 mL | 4.0197 mL |
| 10 mM | 0.201 mL | 1.0049 mL | 2.0098 mL |
| 第一步：请输入基本实验信息（考虑到实验过程中的损耗，建议多配一只动物的药量） | ||||||||||
| 给药剂量 | mg/kg |  |
动物平均体重 | g | |
每只动物给药体积 | ul | |
动物数量 | 只 |
| 第二步：请输入动物体内配方组成（配方适用于不溶于水的药物；不同批次药物配方比例不同，请联系GLPBIO为您提供正确的澄清溶液配方） | ||||||||||
| % DMSO % % Tween 80 % saline | ||||||||||
| 计算重置 | ||||||||||
计算结果:
工作液浓度： mg/ml；
DMSO母液配制方法： mg 药物溶于 μL DMSO溶液（母液浓度 mg/mL，
体内配方配制方法：取 μL DMSO母液，加入 μL PEG300，混匀澄清后加入μL Tween 80，混匀澄清后加入 μL saline，混匀澄清。
1. 首先保证母液是澄清的；
2.
一定要按照顺序依次将溶剂加入，进行下一步操作之前必须保证上一步操作得到的是澄清的溶液，可采用涡旋、超声或水浴加热等物理方法助溶。
3. 以上所有助溶剂都可在 GlpBio 网站选购。
Quality Control & SDS
- View current batch:
- Purity: >99.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet