CP-31398
CP-31398 can stabilize the active conformation of p53 and promote p53 activity in cancer cells with either mutant or wild-type p53. In addition, CP-31398 can upregulate p53 target genes, such as p21WAF1/Cip1 and KILLER/DR5. CP-31398 exerts an inhibitory effect on tumor growth.
For research use only. We do not sell to patients.
- CAS No.: 259199-65-0
- Formula: C22H26N4O
- Molecular Weight:362.47
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biological Activity
Description
Cellular Effect
|
Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| A549 | IC50 |
>25 μM
Compound: CP-31398
|
Antiproliferative activity against human A549 cells after 72 hrs by CellTiter 96 aqueous one solution assay
Antiproliferative activity against human A549 cells after 72 hrs by CellTiter 96 aqueous one solution assay
|
[PMID: 30562697] |
| A549 | IC50 |
24.78 μM
Compound: CP-31398
|
Cytotoxicity against human A549 cells expressing wild type p53 assessed as reduction in cell viability preincubated for 48 hrs and measured after 4 hrs by MTT assay
Cytotoxicity against human A549 cells expressing wild type p53 assessed as reduction in cell viability preincubated for 48 hrs and measured after 4 hrs by MTT assay
|
[PMID: 31761381] |
| DU-145 | IC50 |
15.34 μM
Compound: CP-31398
|
Cytotoxicity against human DU145 cells expressing mutant type p53 assessed as reduction in cell viability preincubated for 48 hrs and measured after 4 hrs by MTT assay
Cytotoxicity against human DU145 cells expressing mutant type p53 assessed as reduction in cell viability preincubated for 48 hrs and measured after 4 hrs by MTT assay
|
[PMID: 31761381] |
| HCT-116 | IC50 |
18.63 μM
Compound: CP-31398
|
Antiproliferative activity against p53+/+ human HCT116 cells after 72 hrs by CellTiter 96 aqueous one solution assay
Antiproliferative activity against p53+/+ human HCT116 cells after 72 hrs by CellTiter 96 aqueous one solution assay
|
[PMID: 30562697] |
| HCT-116 | IC50 |
18.63 μM
Compound: CP-31398
|
Anticancer activity against human HCT116 cells assessed as inhibition of cell proliferation
Anticancer activity against human HCT116 cells assessed as inhibition of cell proliferation
|
[PMID: 31158748] |
| HCT-116 | IC50 |
18.63 μM
Compound: CP-31398
|
Cytotoxicity against human HCT116 cells expressing wild type p53 incubated for 72 hrs by MTS assay
Cytotoxicity against human HCT116 cells expressing wild type p53 incubated for 72 hrs by MTS assay
|
[PMID: 31158748] |
| HCT-116 | IC50 |
26.28 μM
Compound: CP-31398
|
Antiproliferative activity against p53-/- human HCT116 cells after 72 hrs by CellTiter 96 aqueous one solution assay
Antiproliferative activity against p53-/- human HCT116 cells after 72 hrs by CellTiter 96 aqueous one solution assay
|
[PMID: 30562697] |
| HCT-116 | IC50 |
26.28 μM
Compound: CP-31398
|
Cytotoxicity against human HCT116 cells deficient in p53 incubated for 72 hrs by MTS assay
Cytotoxicity against human HCT116 cells deficient in p53 incubated for 72 hrs by MTS assay
|
[PMID: 31158748] |
| L02 | IC50 |
25.34 μM
Compound: CP-31398
|
Cytotoxicity against human HL-7702 cells expressing wild type p53 assessed as reduction in cell viability preincubated for 48 hrs and measured after 4 hrs by MTT assay
Cytotoxicity against human HL-7702 cells expressing wild type p53 assessed as reduction in cell viability preincubated for 48 hrs and measured after 4 hrs by MTT assay
|
[PMID: 31761381] |
| MCF7 | IC50 |
26.96 μM
Compound: CP-31398
|
Antiproliferative activity against human MCF7 cells after 72 hrs by CellTiter 96 aqueous one solution assay
Antiproliferative activity against human MCF7 cells after 72 hrs by CellTiter 96 aqueous one solution assay
|
[PMID: 30562697] |
| MGC-803 | IC50 |
18.27 μM
Compound: CP-31398
|
Cytotoxicity against human MGC-803 cells expressing mutant type p53 assessed as reduction in cell viability preincubated for 48 hrs and measured after 4 hrs by MTT assay
Cytotoxicity against human MGC-803 cells expressing mutant type p53 assessed as reduction in cell viability preincubated for 48 hrs and measured after 4 hrs by MTT assay
|
[PMID: 31761381] |
| NHDF | IC50 |
12.26 μM
Compound: CP-31398
|
Antiproliferative activity against human NHDF cells after 72 hrs by CellTiter 96 aqueous one solution assay
Antiproliferative activity against human NHDF cells after 72 hrs by CellTiter 96 aqueous one solution assay
|
[PMID: 30562697] |
| NHDF | IC50 |
12.26 μM
Compound: CP-31398
|
Cytotoxicity against human NHDF cells incubated for 72 hrs by MTS assay
Cytotoxicity against human NHDF cells incubated for 72 hrs by MTS assay
|
[PMID: 31158748] |
| PANC-1 | IC50 |
>25 μM
Compound: CP-31398
|
Cytotoxicity against human PANC1 cells harboring mutant TP53 gene incubated for 72 hrs by MTS assay
Cytotoxicity against human PANC1 cells harboring mutant TP53 gene incubated for 72 hrs by MTS assay
|
[PMID: 31158748] |
| PC-3 | IC50 |
16.34 μM
Compound: CP-31398
|
Cytotoxicity against human PC-3 cells assessed as reduction in cell viability preincubated for 48 hrs and measured after 4 hrs by MTT assay
Cytotoxicity against human PC-3 cells assessed as reduction in cell viability preincubated for 48 hrs and measured after 4 hrs by MTT assay
|
[PMID: 31761381] |
| T-24 | IC50 |
20.34 μM
Compound: CP-31398
|
Cytotoxicity against human T-24 cells expressing wild type p53 assessed as reduction in cell viability preincubated for 48 hrs and measured after 4 hrs by MTT assay
Cytotoxicity against human T-24 cells expressing wild type p53 assessed as reduction in cell viability preincubated for 48 hrs and measured after 4 hrs by MTT assay
|
[PMID: 31761381] |
| U-251 | IC50 |
18.77 μM
Compound: CP-31398
|
Cytotoxicity against human U251 cells harboring mutant TP53 gene incubated for 72 hrs by MTS assay
Cytotoxicity against human U251 cells harboring mutant TP53 gene incubated for 72 hrs by MTS assay
|
[PMID: 31158748] |
In Vitro
CP-31398 (36.75 μM, 16 h) induces p21 in p53-mutant cells[1]. CP-31398 (15 μg/mL, 20 hours) could induce apoptosis and cell cycle arrest in SW480 cells[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:Saos-2 cells expressing transfected mutant p53
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Concentration:36.75 μM
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Incubation Time:16 h
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Result:Induction of p21 in cells expressing only mutant p53.
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Cell Line:LN-18 and U87MG cells
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Concentration:36 μM
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Incubation Time:16 h
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Result:Decreased the levels of procaspase 3 and induced cleavage of caspase 7.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Small human tumor xenografts in mice[1]
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Dosage:100 mg/kg
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Administration:Orally twice daily for 7 days
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Result:Suppressed A375.S2 tumor growth by -50%.
Chemical Information
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CAS No. 259199-65-0
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Molecular Weight 362.47
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Formula C22H26N4O
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SMILES
CN(C)CCCNC1=C2C=CC=CC2=NC(/C=C/C3=CC=C(OC)C=C3)=N1
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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.
Protocols
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Patient-Derived Xenograft (PDX)
Patient-derived xenograft (PDX) models are generated by engrafting primary human tumor tissue directly into immunodeficient mice, allowing in vivo propagation of patient tumor biology without initial in vitro adaptation. These models are used to preserve key histopathological and molecular characteristics of the original tumor and enable assessment of tumor growth dynamics and therapeutic response in a living organism. The biological readout is tumor engraftment and subsequent growth in the murine host, which reflects the ability of human tumor cells to survive, vascularize, and expand in an immunocompromised microenvironment.
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Patient-Derived Orthotopic Xenograft (PDOX)
Patient-derived orthotopic xenograft (PDOX) modeling implants fresh patient tumor tissue or patient-derived tumor cells into the anatomically corresponding organ or tissue site of immunodeficient mice, usually by surgical orthotopic implantation, to preserve patient tumor histology, local microenvironmental context, invasion, metastatic behavior, and treatment-response features better than subcutaneous implantation. PDOX readouts include tumor engraftment, orthotopic tumor growth, local invasion, metastasis, recurrence after resection, histologic similarity to the donor tumor, biomarker retention, molecular concordance, survival, and response or resistance to therapy. PDOX models are used for preclinical drug testing and individualized therapy evaluation, but engraftment success varies by tumor type and specimen quality.
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Subcutaneous Cell-Line-Derived Xenograft
Subcutaneous cell-line-derived xenograft (CDX) models are established by implanting cultured human cancer cell lines into immunodeficient mice, where the injected cells form localized tumors that can be monitored in vivo as a measure of tumorigenic potential, growth kinetics, and treatment response. These models are widely used in oncology research because they allow reproducible tumor formation and enable comparative assessment of tumor growth between different cell lines or genetic manipulations in a controlled in vivo microenvironment. Subcutaneous implantation of cancer cells in immunodeficient mice is a standard approach for evaluating tumor growth behavior and therapeutic response across multiple cancer types, including prostate, esophageal, pancreatic, and colon cancer models.
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Orthotopic Cell-Line Xenograft
Orthotopic cell-line xenograft models involve implantation of human cancer cell lines into the anatomically corresponding organ of immunodeficient mice to reproduce tumor growth within a native microenvironment, enabling more clinically relevant tumor behavior compared with subcutaneous models. These models are widely used because orthotopic placement better recapitulates tumor progression, including invasion and metastatic spread, which are often underrepresented in heterotopic implantation systems. Compared with conventional xenografts, orthotopic implantation is described as more technically complex but provides improved simulation of tumor-microenvironment interactions and metastatic behavior, making it particularly valuable for translational oncology research. Surgical orthotopic implantation approaches have been emphasized as enabling faithful reproduction of clinical cancer features, including metastasis and disease progression patterns that align with the tumor’s organ of origi
Purity & Documentation
References
[1]. B A Foster, et al. Pharmacological rescue of mutant p53 conformation and function. Science. 1999 Dec 24;286(5449):2507-10. [Content Brief]
[2]. Rishu Takimoto, et al. The Mutant p53-Conformation Modifying Drug, CP-31398, Can Induce Apoptosis of Human Cancer Cells and Can Stabilize Wild-Type p53 Protein. Cancer Biol Ther. Jan-Feb 2002;1(1):47-55. [Content Brief]
[3]. J Wischhusen, et al. CP-31398, a novel p53-stabilizing agent, induces p53-dependent and p53-independent glioma cell death. Oncogene. 2003 Nov 13;22(51):8233-45. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)