CCT018159 |
| Catalog No.GC10223 |
3,4-디아릴 피라졸레조르시놀인 CCT018159는 인간 Hsp90β 및 효모 Hsp90에 대해 IC50이 각각 3.2 및 6.6μM인 ATP 경쟁적 HSP90 ATPase 활성 억제제입니다. CCT018159는 G1 정지와 관련된 세포 세포 정지를 일으키고 세포 사멸을 유도합니다. CCT018159는 침습 및 혈관신생과 관련된 주요 내피 및 종양 세포 기능을 억제합니다.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: 171009-07-7
Sample solution is provided at 25 µL, 10mM.
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IC50: 3.2 and 6.6 μM for human Hsp90β and yeast Hsp90, respectively
CCT018159 is an inhibitor of Hsp90.
The molecular chaperone heat shock protein 90 (HSP90) regulates the activation, stability, and biological function of various oncogenic client proteins, such as steroid hormone receptors, kinases, and other proteins.
In vitro: CCT018159 was identified by high-throughput screening inhibiting human HSP90beta with comparable potency to 17-AAG and with similar ATP-competitive kinetics. X-ray crystallographic structures of the yeast Hsp90 complexed with CCT018159 showed binding properties similar to radicicol. The mean cellular GI50 of CCT018159 across a panel of human cancer cell lines, including melanoma, was 5.3 μM. Unlike 17-AAG, the in-vitro antitumor activity of CCT018159 was independent of NQO1/DT-diaphorase and P-glycoprotein expression. The signature of HSP90 inhibition, comprising increased expression of HSP72 protein and depletion of ERBB2, CDK4, C-RAF, and mutant B-RAF, was indicated in human cancer cell lines treated with CCT018159 [1].
In vivo: In human tumor xenografts including SKMEL 28 melanoma cells, CCT018159 was found to induce the expression of Hsp72 as well as ERBB2, Cdk4 and dc-Raf [1].
Clinical trial: Up to now, CCT018159 is still in the preclinical development stage.
Reference:
[1] S. Y. Sharp, K. Boxall, M. Rowlands, et al. In vitro biological characterization of a novel, synthetic diaryl pyrazole resorcinol class of heat shock protein 90 inhibitors. Cancer Research 67(5), 2206-2216 (2007).
| Cas No. | 171009-07-7 | SDF | |
| Chemical Name | 4-[4-(2,3-dihydo-1,4-benzodioxin-6-yl)-5-methyl-1H-pyrazol-3-yl]-6-ethyl-1,3-benzenediol | ||
| Canonical SMILES | CCc1cc(c(O)cc1O)c1n[nH]c(C)c1c1ccc2OCCOc2c1 | ||
| Formula | C20H20N2O4 | M.Wt | 352.4 |
| Solubility | ≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide | Storage | Store at -20°C |
| General tips | Please select the appropriate solvent to prepare the stock solution according to the
solubility of the product in different solvents; once the solution is prepared, please store it in
separate packages to avoid product failure caused by repeated freezing and thawing.Storage method
and period of the stock solution: When stored at -80°C, please use it within 6 months; when stored
at -20°C, please use it within 1 month. To increase solubility, heat the tube to 37°C and then oscillate in an ultrasonic bath for some time. |
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| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
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1 mg | 5 mg | 10 mg |
| 1 mM | 2.8377 mL | 14.1884 mL | 28.3768 mL |
| 5 mM | 0.5675 mL | 2.8377 mL | 5.6754 mL |
| 10 mM | 0.2838 mL | 1.4188 mL | 2.8377 mL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
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Method for preparing DMSO master liquid: mg drug pre-dissolved in μL DMSO ( Master liquid concentration mg/mL, Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug. )
Method for preparing in vivo formulation: Take μL DMSO master liquid, next addμL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O, mix and clarify.
Method for preparing in vivo formulation: Take μL DMSO master liquid, next add μL Corn oil, mix and clarify.
Note: 1. Please make sure the liquid is clear before adding the next solvent.
2. Be sure to add the solvent(s) in order. You must ensure that the solution obtained, in the previous addition, is a clear solution before proceeding to add the next solvent. Physical methods such as vortex, ultrasound or hot water bath can be used to aid dissolving.
3. All of the above co-solvents are available for purchase on the GlpBio website.
Quality Control & SDS
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- Purity: >98.50%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 20 reference(s) in Google Scholar.)
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