| BET bromodomain inhibitorPotent and selective inhibitor for BRD4 |
Sample solution is provided at 25 µL, 10mM.
Quality Control & MSDS
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- Purity = 98.00%
- COA (Certificate Of Analysis)
- NMR (Nuclear Magnetic Resonance)
- MSDS (Material Safety Data Sheet)
- Datasheet
Chemical structure
Related Biological Data
| Cell experiment [1]: | |
Cell lines | Primary Multiple Myeloma cell lines |
Preparation method | The solubility of this compound in DMSO is >18.3mg/mL. 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. |
Reacting condition | 2 μM at 72 h |
Applications | CPI-0610 treatment resulted in 40% decrease in viability in primary cells isolated from a newly diagnosed patient and caused 50% cell death in primary cells isolated from a relapsed disease patient. |
| Animal experiment [1]: | |
Animal models | Multiple Myeloma xenograft CB17-SCID mouse model |
Dosage form | subcutaneous injections, 10 mg/kg, twice a day for 38 days |
Application | Mice treated with CPI-0610 showed a significant delay in tumor growth, and the median overall survival of CPI-0610 treated animals was significantly prolonged. |
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] Siu KT, Ramachandran J, Yee AJ, et al. Preclinical activity of CPI-0610, a novel small-molecule bromodomain and extra-terminal protein inhibitor in the therapy of multiple myeloma. Leukemia. 2017 Jan 3. | |
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| Cas No. | 1380087-89-7 | SDF | Download SDF |
| Synonyms | CPI-0610; CPI0610; CPI 0610 | ||
| Chemical Name | 2-(6-(4-chlorophenyl)-1-methyl-4H-benzo[c]isoxazolo[4,5-e]azepin-4-yl)acetamide | ||
| Canonical SMILES | CC1=NOC2=C1C3=CC=CC=C3C(C4=CC=C(C=C4)Cl)=NC2CC(N)=O | ||
| Formula | C20H16ClN3O2 | M.Wt | 365.81 |
| Solubility | ≥18.3mg/mL in DMSO | Storage | Store at -20°C |
| Physical Appearance | A 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. | ||
IC50: < 500 nM for BRD4
BET (bromodomain and extra-terminal) proteins regulate gene expression through their ability to bind to acetylated chromatin and subsequently activate RNA PolII-driven transcriptional elongation. The bromodomain (BRD) and extra-C terminal domain (BET) protein family consists of four members (BRD2, BRD3, BRD4 and BRDT).Small molecule BET inhibitors prevent binding of BET proteins to acetylated histones and inhibit transcriptional activation of BET target genes. BET inhibitors attenuate cell growth and survival in several hematologic cancer models, partially through the down-regulation of the critical oncogene, MYC. BET bromodomain inhibitor is a potent and selective inhibitor for BRD4.
In vitro: The most potent systhsized ompound presented is BET bromodomain inhibitor, which shows activity with IC50 < 500 nM against BRD4 [1].
In vivo: BET bromodomain inhibitor shows activity in vivo at < 10 mg/kg against BRD4 in rat [1].
Clinical trial: Up to now, BET bromodomain inhibitor is still in the preclinical development stage.
Reference:[1] Garnier JM, Sharp PP, Burns CJ. BET bromodomain inhibitors: a patent review. Expert Opin Ther Pat. 2014 Feb;24(2):185-99.
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可以用移液器将细胞吸出来并高速离心，沉淀重悬于PBS中洗涤，接着就可以裂解提取蛋白了。可以用超声，酶解等等，裂解后离心收集上清。
做的比较好的，一般都是上海地区的，你可以看下基尔顿生物。
我刚开始做转染，悬浮细胞，分别做过表达和敲减，看了很多文献，大都没有提及转染后是用转染的这同一批细胞同时做pcr，wb，cck8，凋亡，细胞周期；还是说这次转染只做pcr或wb，再转染一次做cck8或细胞周期。剩下的功能试验均同前，转染一次做一次？我养的是悬浮细胞，转染后做cck8这些功能试验前需要离心换液吗？跪谢解答！
细胞状态与密度；转染试剂的类型、用量；DNA的品质、用量；转染复合物的品质、作用细胞的时间长度。
