Stafib-2
目录号 : GC63204
Stafib-2 是一种有效和选择性的转录因子 STAT5b 抑制剂，抑制 STAT5b 和 STAT5a 的 IC50 值分别为 82 nM 和 1.7 μM。Stafib-2 的细胞通透性较差。
Cas No.:2097938-74-2
Sample solution is provided at 25 µL, 10mM.
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Quality Control & SDS
- View current batch:
- Purity: >95.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Stafib-2 is a potent and selctive inhibitor of the transcription factor STAT5b, with an IC50 of 82 nM and 1.7 μM for STAT5b and STAT5a, respectively. Stafib-2 exhibits poor cell permeability[1].
Stafib-2 has an extremely high affinity for STAT5b (Ki=8.8 nM)[1].Stafib-2 (3-10 μM; 4-48 h) does not show significant activity in K562 and MDA-MB-231 cells[1].
[1]. Elumalai N, et, al. Rational development of Stafib-2: a selective, nanomolar inhibitor of the transcription factor STAT5b. Sci Rep. 2017 Apr 11;7(1):819.
| Cas No. | 2097938-74-2 | SDF | |
| 分子式 | C28H26N2O12P2 | 分子量 | 644.46 |
| 溶解度 | DMSO : 50 mg/mL (77.58 mM; Need ultrasonic) | 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 | 1.5517 mL | 7.7584 mL | 15.5169 mL |
| 5 mM | 0.3103 mL | 1.5517 mL | 3.1034 mL |
| 10 mM | 0.1552 mL | 0.7758 mL | 1.5517 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。
Rational development of Stafib-2: a selective, nanomolar inhibitor of the transcription factor STAT5b
Sci Rep 2017 Apr 11;7(1):819.PMID:28400581DOI:10.1038/s41598-017-00920-3.
The transcription factor STAT5b is a target for tumour therapy. We recently reported catechol bisphosphate and derivatives such as Stafib-1 as the first selective inhibitors of the STAT5b SH2 domain. Here, we demonstrate STAT5b binding of catechol bisphosphate by solid-state nuclear magnetic resonance, and report on rational optimization of Stafib-1 (Ki = 44 nM) to Stafib-2 (Ki = 9 nM). The binding site of Stafib-2 was validated using combined isothermal titration calorimetry (ITC) and protein point mutant analysis, representing the first time that functional comparison of wild-type versus mutant protein by ITC has been used to characterize the binding site of a small-molecule ligand of a STAT protein with amino acid resolution. The prodrug Pomstafib-2 selectively inhibits tyrosine phosphorylation of STAT5b in human leukaemia cells and induces apoptosis in a STAT5-dependent manner. We propose Pomstafib-2, which currently represents the most active, selective inhibitor of STAT5b activation available, as a chemical tool for addressing the fundamental question of which roles the different STAT5 proteins play in various cell processes.
Halogen-substituted catechol bisphosphates are potent and selective inhibitors of the transcription factor STAT5b
Bioorg Med Chem 2017 Jul 15;25(14):3871-3882.PMID:28559059DOI:10.1016/j.bmc.2017.05.039.
The transcription factor STAT5b is an antitumor target. Recently, we presented the small molecules Stafib-1 and Stafib-2 as potent, selective inhibitors of the STAT5b SH2 domain. Here we report that halogen substitutions on the terminal phenyl ring of Stafib-1 and a close derivative are tolerated and specificity over the STAT5a SH2 domain is maintained, albeit with a slight reduction in activity. Our data demonstrate that the synthetic methodology used for generating Stafib-1 and Stafib-2 can be utilized to synthesize a small library of halogen-substituted derivatives, and extend the panel of catechol bisphosphate-based submicromolar and selective STAT5b inhibitors.