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製品番号: HY-18343

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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.

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CAS 番号: 259199-65-0
分子式: C₂₂H₂₆N₄O
分子量:362.47

保管条件:

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

Data Sheet (269 KB)

CP-31398 構造式

CAS 番号: 259199-65-0

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生物活性
- 製品説明
- Cellular Effect
- 体外実験
- 体内実験
化学情報
純度とドキュメンテーション
参考文献
Calculators
Help & FAQs
関連分類
Bioz

生物活性

製品説明

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]

体外実験

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.

体内実験

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%.

化学情報

CAS 番号 259199-65-0
分子量 362.47
分子式 C₂₂H₂₆N₄O
SMILES

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

Room temperature in continental US; may vary elsewhere.
保管条件

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

純度とドキュメンテーション

バッチを選択:

純度: 99.98%

Assay: 99.98%

ee.: 99.98%

データシート (269 KB)
COA (2659 KB)
元素分析報告書 (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
取扱説明書 (2659 KB)

参考文献

[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

モル濃度計算機

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

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分子量分子量

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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