2. Metabolic Enzyme/Protease Apoptosis PI3K/Akt/mTOR
  3. Carboxypeptidase Apoptosis Akt
  4. 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.

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PrCP-7414

PrCP-7414 Chemical Structure

CAS No. : 1252037-41-4

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Based on 1 publication(s) in Google Scholar

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Description

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[1][2].

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.

PrCP-7414 Related Antibodies

Cell Viability Assay[2]

Cell Line: MCF7, BT549, MDA468, BT20, MDA231, Hs578T, SUM159PT breast cancer cell lines
Concentration: 1 μM, 5 μM, 10 μM
Incubation Time: 3 days
Result: Caused a dose-dependent reduction in relative MTT absorbance in all tested cell lines.

Apoptosis Analysis[2]

Cell Line: BT549, MDA468, BT20, MDA231, Hs578T, SUM159PT TNBC cell lines
Concentration: 5 μM (BT549, MDA468, BT20, MDA231, Hs578T); 10 μM (SUM159PT)
Incubation Time: 3 days
Result: Increased the percentage of Sub-G1 (apoptotic) cells in all tested cell lines.
In Vivo

PRCP-7414 (20 mg/kg, i.p., 5 days per week for 5 consecutive weeks) slows tumor growth in ER+ breast cancer PDX models in NSG mice, reduces the activation level of intratumoral AKT, and exerts a synergistic effect with Endoxifen to induce significant tumor regression[1].
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.

Animal Model: NOD.Cg-PrkdcscidIl2rgtmlWjl/Sz (NSG) mice (6-8 weeks of age)[1]
Dosage: 20 mg/kg/day
Administration: i.p.; 5 days/week; 5 weeks
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.
Animal Model: NOD.Cg-PrkdcscidIl2rgtmlWjl/Sz (NSG) mice (female, 6-8 weeks of age, estrogen receptor-positive breast cancer model)[2]
Dosage: 20 mg/kg/day; 40 mg/kg/day
Administration: i.p.; 5 days/week; 51 days
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.
Molecular Weight

578.53

Formula

C31H33Cl2N5O2
CAS No.
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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Please store the product under the recommended conditions in the Certificate of Analysis.
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References
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PrCP-7414 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

PrCP-74141252037-41-4PrCP7414PrCP 7414CarboxypeptidaseApoptosisAktPKBProtein kinase BCaMKIIPRCPIGF1R/HER3 signalingtriple negative breast cancer cellsestrogen receptor positive breast cancerMCF7 breast cancer cellsAKTB6-9 breast cancer cellsNOD scid miceInhibitorinhibitorinhibit

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