GSK6853
目录号 : GC13025
A selective chemical probe for the bromodomain of BRPF1
Cas No.:1910124-24-1
Sample solution is provided at 25 µL, 10mM.
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pIC50: 8.1
GSK6853 is a BRPF1 inhibitor.
The BRPF (Bromodomain and PHD Fingercontaining) protein family are key scaffolding proteins for assembly of MYST histone acetyltransferase complexes.
In vitro: In previous study, GSK6853 was tested in the BROMOscan panel of bromodomain binding assays and the results showed that consistent with the previous findings, it showed excellent BRPF1 potency (pKd 9.5) and greater than 1600-fold selectivity over all other bromodomains tested. In addition, screening GSK6853 against a panel of 48 unrelated assays revealed only off-target activities that were relatively weak compared to its high BRPF1 potency [1].
In vivo: To assess the suitability of GSK6853 for in vivo studies, its DMPK characteristics were studied in male CD1 mice by i.v., po, and i.p. administration. The results indicated that the i.p. route of administration would be suitable for dosing this molecule in further PK/PD models. Moreover, in order to be able to compare biochemical potency measurements to free blood concentrations, the fraction unbound in the CD1 mouse was also tested with a resulting value of 7.9% [1].
Clinical trial: So far, no clinical study has been conducted.
Reference:
[1] Bamborough, P. ,Barnett, H.A.,Becher, I., et al. GSK6853, a chemical probe for inhibition of the BRPF1 bromodomain. ACS Med. Chem. Lett. 7(6), 552-557 (2016).
| Cas No. | 1910124-24-1 | SDF | |
| 化学名 | N-[2,3-dihydro-1,3-dimethyl-6-[(2R)-2-methyl-1-piperazinyl]-2-oxo-1H-benzimidazol-5-yl]-2-methoxy-benzamide | ||
| Canonical SMILES | C[C@H](CNCC1)N1C2=C(NC(C3=CC=CC=C3OC)=O)C=C4C(N(C)C(N4C)=O)=C2 | ||
| 分子式 | C22H27N5O3 | 分子量 | 409.5 |
| 溶解度 | ≤30mg/ml in ethanol;25mg/ml in DMSO;30mg/ml in dimethyl formamide | 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 | 2.442 mL | 12.21 mL | 24.42 mL |
| 5 mM | 0.4884 mL | 2.442 mL | 4.884 mL |
| 10 mM | 0.2442 mL | 1.221 mL | 2.442 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: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet