CP-31398

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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.

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CP-31398 Chemical Structure

CAS No. : 259199-65-0

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Other In-stock Forms of CP-31398:

CP-31398 dihydrochloride

Other Forms of CP-31398:

CP-31398 dihydrochloride In-stock

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Biological Activity
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Description

Cellular Effect

Cell Line	Type	Value	Description	References
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]
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]
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.

Western Blot Analysis^[1]

Cell Line:	Saos-2 cells expressing transfected mutant p53
Concentration:	36.75 μM
Incubation Time:	16 h
Result:	Induction of p21 in cells expressing only mutant p53.

Western Blot Analysis^[3]

Cell Line:	LN-18 and U87MG cells
Concentration:	36 μM
Incubation Time:	16 h
Result:	Decreased the levels of procaspase 3 and induced cleavage of caspase 7.

In Vivo

CP-31398 (100 mg/kg, orally, twice daily for 7 days) exhibits significant anti-tumor activity in mice models^[1]

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:	Small human tumor xenografts in mice^[1]
Dosage:	100 mg/kg
Administration:	Orally twice daily for 7 days
Result:	Suppressed A375.S2 tumor growth by -50%.

Molecular Weight

362.47

Formula

C₂₂H₂₆N₄O

CAS No.

259199-65-0

SMILES

CN(C)CCCNC1=C2C=CC=CC2=NC(/C=C/C3=CC=C(OC)C=C3)=N1

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

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]

CP-31398 Related Classifications

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The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass		Concentration		Volume		Molecular Weight *
	=		×		×

The dilution calculator equation

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

Concentration _(start)	×	Volume _(start)	=	Concentration _(final)	×	Volume _(final)
	×		=		×
C1		V1		C2		V2

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:

CP-31398259199-65-0CP31398CP 31398MDM-2/p53ApoptosisSmall human tumor xenograftsSaos-2 cellsLN-18 and U87MG cellsAnti-tumorInhibitorinhibitorinhibit

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