PrCP-7414
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.
For research use only. We do not sell to patients.
- CAS No.: 1252037-41-4
- Formula: C31H33Cl2N5O2
- Molecular Weight:578.53
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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.
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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.
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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Molecular Weight 578.53
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Formula C31H33Cl2N5O2
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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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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
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]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
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