| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Targets |
CP-31398 targets the tumor suppressor protein p53, stabilizing its active conformation. In p53 mutant cells, it restores the wild-type conformation of mutant p53 in vitro. This promotes p53-mediated transcriptional activity, leading to cell cycle arrest and apoptosis in cancer cells.
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| ln Vitro |
In p53 mutant cells, CP-31398 (36.75 μM, 16 hours) activates p21[1]. In SW480 cells, CP-31398 (15 μg/mL, 20 hours) causes apoptosis and cell cycle arrest [2].
In p53 mutant cells, CP-31398 (36.75 μM, 16 hours) activates p21 expression. It promotes p53 activity in cancer cell lines with mutant or wild-type p53. The compound induces cell cycle arrest and apoptosis in cancer cells. These activities confirm p53 pathway activation in vitro. |
| ln Vivo |
In mice models, CP-31398 (100 mg/kg, orally) has strong anti-tumor efficacy [1].
CP-31398 inhibits growth of small human tumor xenografts in vivo. It has shown promise in preclinical studies for treating cancers with p53 mutations, including breast, lung, and colon cancers. The compound has a maximum tolerated dose of 400 ppm and is regarded as a promising agent for combination with chemotherapy drugs. |
| Enzyme Assay |
Non-cell-based assays for CP-31398 involve p53-DNA binding studies using purified p53 protein and DNA containing p53 response elements. The compound is incubated with p53 protein and DNA, and binding is assessed by electrophoretic mobility shift assay (EMSA) or fluorescence polarization. Stabilization of the active conformation is confirmed by antibody recognition of conformation-specific epitopes.
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| Cell Assay |
Western Blot Analysis[1]
Cell Types: Saos-2 cells expressing transfected mutant p53. Tested Concentrations: 36.75 μM. Incubation Duration: 16 hrs (hours). Experimental Results: p21 was induced in cells expressing only mutant p53. Western Blot Analysis[3] Cell Types: LN-18 and U87MG cells. Tested Concentrations: 36μM. Incubation Duration: 16 hrs (hours). Experimental Results: diminished caspase 3 levels and induced caspase 7 cleavage. Cellular assays for CP-31398 utilize cancer cell lines with mutant or wild-type p53 (e.g., SW480). Cells are treated with the compound at various concentrations (e.g., 36.75 μM) for specified durations. p53 target gene expression (e.g., p21, PUMA, BAX) is measured by quantitative PCR or Western blotting. Cell cycle analysis and apoptosis assays (e.g., Annexin V staining) are performed to confirm functional activity. |
| Animal Protocol |
Animal/Disease Models: Small human tumor xenografts in mice [1].
Doses: 100 mg/kg. Route of Administration: Orally, twice (two times) daily for 7 days. Experimental Results: A375.S2 tumor growth inhibition -50%. In vivo animal models for CP-31398 involve xenograft studies in immunodeficient mice bearing human tumor cell lines with p53 mutations. The compound is administered orally or via other routes at various doses. Tumor growth inhibition is monitored over time. Pharmacodynamic markers such as p53 target gene expression in tumor tissues are assessed. Maximum tolerated dose is 400 ppm. |
| ADME/Pharmacokinetics |
Pharmacokinetic properties of CP-31398 dihydrochloride include molecular weight of 435.4 g/mol and purity >98%. The compound is a small molecule p53 stabilizer. Detailed PK parameters such as half-life and bioavailability are not extensively reported. The compound is administered orally in preclinical studies.
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| Toxicity/Toxicokinetics |
CP-31398 has a maximum tolerated dose of 400 ppm. No specific LD50 values or detailed toxicity profiles are provided. The compound is a research chemical for laboratory use only. Standard preclinical toxicity assessments would be required for therapeutic development. It is regarded as a promising agent for combination with chemotherapy.
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| References |
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| Additional Infomation |
CP-31398 dihydrochloride is a p53 stabilizer. It has CAS number 1217195-61-3. The compound stabilizes the active conformation of p53 and promotes p53 activity in cancer cells. It induces cell cycle arrest and apoptosis and has shown preclinical efficacy in p53-mutant cancers. It is a research tool for p53 biology and cancer therapy.
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| Molecular Formula |
C22H28CL2N4O
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|---|---|
| Molecular Weight |
435.39
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| Exact Mass |
434.164
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| CAS # |
1217195-61-3
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| Related CAS # |
259199-65-0;1217195-61-3 (2HCl);
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| PubChem CID |
56972205
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
5.198
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| Hydrogen Bond Donor Count |
3
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| Hydrogen Bond Acceptor Count |
5
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| Rotatable Bond Count |
8
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| Heavy Atom Count |
29
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| Complexity |
448
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| Defined Atom Stereocenter Count |
0
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| SMILES |
CN(C)CCCNC1=NC(=NC2=CC=CC=C21)/C=C/C3=CC=C(C=C3)OC.Cl.Cl
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| InChi Key |
WWIFDJIOGCGSBS-IVKCLRODSA-N
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| InChi Code |
InChI=1S/C22H26N4O.2ClH/c1-26(2)16-6-15-23-22-19-7-4-5-8-20(19)24-21(25-22)14-11-17-9-12-18(27-3)13-10-17;;/h4-5,7-14H,6,15-16H2,1-3H3,(H,23,24,25);2*1H/b14-11+;;
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| Chemical Name |
N-[2-[(E)-2-(4-methoxyphenyl)ethenyl]quinazolin-4-yl]-N',N'-dimethylpropane-1,3-diamine;dihydrochloride
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| Synonyms |
CP-31398 dihydrochloride; CP 31398 dihydrochloride; CP31398 dihydrochloride
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment (e.g. under nitrogen), avoid exposure to moisture and light. |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~200 mg/mL (~459.36 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 0.83 mg/mL (1.91 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 8.3 mg/mL clear DMSO stock solution to 400 μL of PEG300 and mix evenly; then add 50 μL of Tween-80 to the above solution and mix evenly; then add 450 μL of normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: 0.83 mg/mL (1.91 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with ultrasonication. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 8.3 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C，1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.2968 mL | 11.4840 mL | 22.9679 mL | |
| 5 mM | 0.4594 mL | 2.2968 mL | 4.5936 mL | |
| 10 mM | 0.2297 mL | 1.1484 mL | 2.2968 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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