PrCP-7414
Based on 1 Customer Validation
PrCP-7414 is a prolyl carboxypeptidase (PRCP) inhibitor. PrCP-7414 blocks PRCP-mediated activation of the IGF1R/HER3 signaling pathway and subsequent AKT activation. PrCP-7414 exhibits pro-apoptotic, anti-tumor and synergistic cytotoxic activities, and inhibits the proliferation and survival of triple-negative breast cancer cells. PrCP-7414 can be used for the research of breast cancer.
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- Purity : 99.53%
- CAS No.: 1252037-41-4
- 화학식: C31H33Cl2N5O2
- 분자량:578.53
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보관:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 6 months , -20°C, 1 month
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- Protocol
- 순도&문서
- References
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Help & FAQs
Biological Activity
제품 설명
In Vitro
PRCP-7414 (5 μM; 72 h) inhibits the IGF1R/HER3-AKT signaling pathway in B6-9 breast cancer cells, enhances Endoxifen (HY-18719E)-induced cell death in both MCF7 and B6-9 breast cancer cells, and reduces their colony-forming ability[1].
PRCP-7414 (5 μM; 3 days) enhances the proliferation-inhibiting effect of Endoxifen on MCF7 and TRC breast cancer cells, as well as the cell death-inducing effect of Endoxifen on TRC breast cancer cells[1].
PrCP-7414 (1-10 μM; 3 days) reduces the viability of MCF7, BT549, MDA468, BT20, MDA231, Hs578T and SUM159PT breast cancer cells in a dose-dependent manner[2].
PrCP-7414 inhibits AKT activation downstream of EGFR, ErbB3, IGF1R and PDGFR in MDA468 and SUM159PT triple-negative breast cancer (TNBC) cells[2].
PrCP-7414 (5 μM-10 μM; 3 days) induces apoptosis in various triple-negative breast cancer (TNBC) cell lines[2].
PrCP-7414 (0-7.5 μM; 3 days) synergistically induces apoptosis of MDA468 and BT549 triple-negative breast cancer (TNBC) cells in combination with 2 μM Lapatinib (HY-50898)[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. Further protocols information, click here.
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Cell Line:MCF7, BT549, MDA468, BT20, MDA231, Hs578T, SUM159PT breast cancer cell lines
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Concentration:1 μM, 5 μM, 10 μM
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Incubation Time:3 days
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Result:Caused a dose-dependent reduction in relative MTT absorbance in all tested cell lines.
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Cell Line:BT549, MDA468, BT20, MDA231, Hs578T, SUM159PT TNBC cell lines
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Concentration:5 μM (BT549, MDA468, BT20, MDA231, Hs578T); 10 μM (SUM159PT)
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Incubation Time:3 days
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Result:Increased the percentage of Sub-G1 (apoptotic) cells in all tested cell lines.
In Vivo
PRCP-7414 (40 mg/kg; i.p.; 5 days per week; 51 days) inhibits the growth of triple-negative breast tumors in NOD SCID mice[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:NOD.Cg-PrkdcscidIl2rgtmlWjl/Sz (NSG) mice (6-8 weeks of age)[1]
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Dosage:20 mg/kg/day
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Administration:i.p.; 5 days/week; 5 weeks
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Result:Slowed PDX tumor growth with a significant reduction in tumor log-volume relative to vehicle-treated controls.
Reduced levels of phosphorylated (S473) AKT in tumor lysates compared to vehicle or endoxifen-only treated tumors.
Synergized with endoxifen to cause significant tumor regression.
Showed no obvious weight loss in treated mice.
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Animal Model:NOD.Cg-PrkdcscidIl2rgtmlWjl/Sz (NSG) mice (female, 6-8 weeks of age, estrogen receptor-positive breast cancer model)[2]
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Dosage:20 mg/kg/day; 40 mg/kg/day
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Administration:i.p.; 5 days/week; 51 days
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Result:Reduced MCF7 tumor volume relative to vehicle control at 20 mg/kg/day.
Resulted in a statistically significant reduction in MCF7 tumor volume relative to vehicle control at 40 mg/kg/day.
Chemical Information
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CAS No. 1252037-41-4
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Appearance Solid
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분자량 578.53
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화학식 C31H33Cl2N5O2
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Color White to off-white
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SMILES
C[C@@H](C1=CC=C(C2=CC=CC=C2)C=C1)[C@H](NC(C(C)(N)C)=O)C(N3[C@@H](CCC3)C(NC4=C5)=NC4=CC(Cl)=C5Cl)=O
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선적
Room temperature in continental US; may vary elsewhere.
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보관
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month
용액&용해도
In Vitro:
DMSO : 100 mg/mL (172.85 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (4.32 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (4.32 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Protocol
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Detection of Apoptosis
Apoptosis, also called programmed cell death, is generally characterized by distinct morphological characteristics.
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Apoptosis Solutions
Apoptosis is a regulated, generally non-lytic cell-death pathway that removes unwanted, damaged, infected, or abnormal cells through coordinated morphological changes, caspase activation, DNA fragmentation, and membrane remodeling. The intrinsic apoptosis pathway is controlled mainly by mitochondrial outer membrane permeabilization, BCL-2 family proteins, cytochrome c release, apoptosome formation, caspase-9 activation, and downstream executioner caspase-3/7 activation. The extrinsic apoptosis pathway is initiated by death receptors such as Fas, TNFR, and TRAIL receptors, which recruit adaptor proteins and activate caspase-8 before engaging executioner caspases or mitochondrial amplification through BID cleavage. Apoptosis is linked to many phenotypes, including cancer cell killing, tissue homeostasis, immune regulation, neurodegeneration, infection response, and treatment-induced cytotoxicity; unresolved questions include how apoptosis interacts with necroptosis, pyroptosis, ferroptos
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Breast Cancer Modeling
Breast cancer is a heterogeneous cancer, and it has been distinguished into four subtypes: luminal A, luminal B, HER2-positive and basal-like. Molecular mutations, epigenetic alterations, hormone exposure and immune microenvironment are related to the progression of breast cancer.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
순도&문서
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Data Sheet (280 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Duan L, et al. Prolylcarboxypeptidase promotes IGF1R/HER3 signaling and is a potential target to improve endocrine therapy response in estrogen receptor positive breast cancer. Cancer Biol Ther. 2022;23(1):1-10. [Content Brief]
[2]. Duan L, et al. Prolyl Carboxypeptidase Maintains Receptor Tyrosine Kinase Signaling and Is a Potential Therapeutic Target in Triple Negative Breast Cancer. Cancers (Basel). 2022;14(3):739. Published 2022 Jan 31. [Content Brief]
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
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| DMSO | 1 mM | 1.7285 mL | 8.6426 mL | 17.2852 mL | 43.2130 mL |
| 5 mM | 0.3457 mL | 1.7285 mL | 3.4570 mL | 8.6426 mL | |
| 10 mM | 0.1729 mL | 0.8643 mL | 1.7285 mL | 4.3213 mL | |
| 15 mM | 0.1152 mL | 0.5762 mL | 1.1523 mL | 2.8809 mL | |
| 20 mM | 0.0864 mL | 0.4321 mL | 0.8643 mL | 2.1606 mL | |
| 25 mM | 0.0691 mL | 0.3457 mL | 0.6914 mL | 1.7285 mL | |
| 30 mM | 0.0576 mL | 0.2881 mL | 0.5762 mL | 1.4404 mL | |
| 40 mM | 0.0432 mL | 0.2161 mL | 0.4321 mL | 1.0803 mL | |
| 50 mM | 0.0346 mL | 0.1729 mL | 0.3457 mL | 0.8643 mL | |
| 60 mM | 0.0288 mL | 0.1440 mL | 0.2881 mL | 0.7202 mL | |
| 80 mM | 0.0216 mL | 0.1080 mL | 0.2161 mL | 0.5402 mL | |
| 100 mM | 0.0173 mL | 0.0864 mL | 0.1729 mL | 0.4321 mL |
PrCP-7414 Related Classifications
HY-177760 Related Classifications
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