ReACp53 |
| Catalog No.GC15946 |
ReACp53 pourrait inhiber la formation d'amyloÏde p53 et sauver la fonction p53 dans les lignées cellulaires cancéreuses.
Products are for research use only. Not for human use. We do not sell to patients.
Cas No.: N/A
Sample solution is provided at 25 µL, 10mM.
ReACp53 is an inhibitor of p53 amyloid formation.
Nearly half of all human cancers lose p53 function by missense mutations, with an unknown fraction of these containing p53 in a self-aggregated amyloid-like state.
In vitro: Previous study found that ReACp53 could penetrates into HGSOC primary cancer cells and convert mutant p53 from a punctate state into soluble wild-type-like p53. ReACp53 could also induce cell-dycle arrest, cancer cell death, resulting in p53 Degradation. Moreover, ReACp53 induced quich cell death in human primary uterine fibroblasts transfected with a R175H p53 mutant. In addition, ReACp53 was found to be able to specifically reduce the cell viability and proliferation of cancer cells with mutant but not wild-type p53 [1].
In vivo: Animal study showed that i.p. administered ReACp53 could rapidly enter the systemic circulation and could be detected in the mouse serum at the 1-hr time point. In addition, ReACp53 could be detected in tumor tissue. In efficacy models, tumor volumes monitored daily suggested that only ReACp53-treated OVCAR3 xenografts shrank whereas vehicle-treated tumors grew more than doubled in size. Moreover, mutant p53-bearing tumors in the ReACp53-treated mice were 80%–90% smaller in weight than the control cohort, further confirming the ability of ReACp53 to inhibit tumor proliferation in vivo [1].
Clinical trial: Up to now, ReACp53 is still in the preclinical development stage.
Reference:
[1] Soragni A et al. A Designed Inhibitor of p53 Aggregation Rescues p53 Tumor Suppression in Ovarian Carcinomas. Cancer Cell. 2016 Jan 11;29(1):90-103.
Animal experiment: | Mice[1]In the minimal residual disease model, three cohorts of mice (n=3) are injected with a matrigel/OVCAR3 (p53 mutant) suspension on one flank and with a matrigel/MCF7 (WT p53) suspension on the other flank. Treatment is started the same day. In both models, the treatment phase consist of three weeks of daily IP injections with 15 mg/kg of ReACp53, sequence-scrambled control peptide or vehicle alone[1]. |
References: [1]. Soragni A et al. A Designed Inhibitor of p53 Aggregation Rescues p53 Tumor Suppression in Ovarian Carcinomas.Cancer Cell. 2016 Jan 11;29(1):90-103. | |
| Cas No. | N/A | SDF | |
| Chemical Name | (S)-2-((Z)-((1Z,3S,4Z,6S,7Z,9S,10Z,12S,13Z,15S,16Z,18S,19Z,21S)-3,15-di((S)-sec-butyl)-1-((S)-1-((6S,7Z,9S,10Z,12S,13Z,15S,16Z,18S,19Z,21S,22Z,24S,25Z,27S,28Z,30S,31Z,33S)-1,6-diamino-9,12,15,18,21,24,27,30,33-nonakis(3-guanidinopropyl)-7,10,13,16,19,22,2 | ||
| Canonical SMILES | CC[C@]([C@@](/N=C(O)/[C@]1([H])CCCN1C([C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](/N=C(O)/[C@](N)([H])CCCNC(N)=N)([H])CCCNC(N)=N)([H])CCCNC(N)=N)([H])CCCNC(N)=N)([H])CCCNC(N)=N)([H])CCCNC(N) | ||
| Formula | C108H206N52O24 | M.Wt | 2617.13 |
| Solubility | Soluble in DMSO | 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. |
||
| Shipping Condition | Evaluation sample solution: shipped with blue ice. All other sizes available: with RT, or with Blue Ice upon request. | ||
| Prepare stock solution | |||
|
1 mg | 5 mg | 10 mg |
| 1 mM | 382.1 μL | 1.9105 mL | 3.821 mL |
| 5 mM | 76.4 μL | 382.1 μL | 764.2 μL |
| 10 mM | 38.2 μL | 191 μL | 382.1 μL |
Step 1: Enter information below (Recommended: An additional animal making an allowance for loss during the experiment)
Step 2: Enter the in vivo formulation (This is only the calculator, not formulation. Please contact us first if there is no in vivo formulation at the solubility Section.)
Calculation results:
Working concentration: mg/ml;
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
- View current batch:
- Purity: >99.00%
- COA (Certificate Of Analysis)
- SDS (Safety Data Sheet)
- Datasheet
Average Rating: 5 (Based on Reviews and 16 reference(s) in Google Scholar.)
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