| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Targets |
p53 DBD (Ki = 1-2 μM)
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| ln Vitro |
In p53 mutant cells (H157, H1975, and H322), SCH529074 (2-4 μM; 24 hours) significantly reduced cell viability, to 20–25%, and in the p53 WT cell line A549, to 68 % 4 μM. In NSCLC cells (H157, A549, HCT116, and HCT116 p53-/-), SCH 529074 (2 and 4 μM) induces G0/G1 phase when compared to control cells treated with low concentration (2 μM) (59). 72%, 66%, 57%, and 57%[1]. H1975 cells are exposed to SCH 529074 (2-4 μM) for 24 hours, which causes both early and late fluorescence. Similar to how SCH 529074 at 2 and 4 μM greatly boosted early and late cells in A549 cells, it also considerably enhanced H157 cells. This is supported by the fact that SCH 529074 at 4 μM significantly promoted early and late cells in HCT116 cells in arc cells, as well as early cells in HCT116 p53-/- cells [1]. SCH 529074 (2–6 μM; 24 hours) raises p21 and PUMA protein levels in wireline
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| ln Vivo |
At dosages of 50 and 30 mg/kg, respectively, of the lung cancer medication SCH529074, tumor development was reduced by 79% and 43% over the course of four weeks, beginning on day three and ending on day thirty-one. In human DLD-1 colorectal cancer xenografts, the degree of inhibition corresponds with the compound's switch sensitivity (0.26-0.55 μM at 30 mg/kg, 0.39-0.79 μM at 50 mg/kg, final 2 post-
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| Cell Assay |
cell viability assay [1]
Cell Types: p53 mutant cells (H157, H1975, and H322) and p53 WT cell line A549 Tested Concentrations: 4 or 6 μM, regardless of their p53 status [1]. 2μM; 4 μM Incubation Duration: 24 hrs (hours) Experimental Results: Inhibition of cancer WT and mutant cell viability. Cell cycle analysis[1] Cell Types: H1975, H157, A549, HCT116, HCT116 p53-/- Cell Tested Concentrations: 2 µM, 4 µM, 6 µM Incubation Duration: 24 hrs (hours) Experimental Results: Induced cells in all NSCLC cell lines evaluated apoptotic, regardless of their p53 mutation status. Western Blot Analysis[1] Cell Types: H1975, H322, H157, A549, HCT116, HCT116 p53-/- Tested Concentrations: 2 µM, 4 µM, 6 µM Incubation Duration: 24 hrs (hours) Experimental Results: Increased PUMA and p21 protein expression. |
| Animal Protocol |
Animal/Disease Models: Female nude mice, 5-7 weeks old, were inoculated subcutaneously (sc) (sc) with DLD-1 human colorectal cancer cells [2].
Doses: 30 or 50 mg/kg. Route of Administration: oral; -12 hrs (hrs (hours))) [2]. twice (two times) daily; 4 weeks; starting on day 3 through day 31 Experimental Results: Inhibition of tumor growth |
| References |
[1]. Miljana Nenkov, et al. Growth Inhibitory Role of the p53 Activator SCH 529074 in non‑small Cell Lung Cancer Cells Expressing Mutant p53. Oncol Rep. 2020 Jun;43(6):2073-2082.
[2]. Mark Demma, et al. SCH529074, a Small Molecule Activator of Mutant p53, Which Binds p53 DNA Binding Domain (DBD), Restores Growth-Suppressive Function to Mutant p53 and Interrupts HDM2-mediated Ubiquitination of Wild Type p53. J Biol Chem. 2010 Apr 2;285(14):10198-212. |
| Molecular Formula |
C31H36CL2N6
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|---|---|
| Molecular Weight |
563.571
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| Exact Mass |
562.2379
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| Elemental Analysis |
C, 66.07; H, 6.44; Cl, 12.58; N, 14.91
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| CAS # |
922150-11-6
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| Related CAS # |
922150-11-6
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| Appearance |
Solid powder
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| SMILES |
CN(C)CCCNC1=NC(=NC2=CC=CC=C21)CN3CCN(CC3)C(C4=CC=C(C=C4)Cl)C5=CC=C(C=C5)Cl
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| InChi Key |
NCAJLQDPTZBGJV-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C31H36Cl2N6/c1-37(2)17-5-16-34-31-27-6-3-4-7-28(27)35-29(36-31)22-38-18-20-39(21-19-38)30(23-8-12-25(32)13-9-23)24-10-14-26(33)15-11-24/h3-4,6-15,30H,5,16-22H2,1-2H3,(H,34,35,36)
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| Chemical Name |
N-[2-[[4-[bis(4-chlorophenyl)methyl]piperazin-1-yl]methyl]quinazolin-4-yl]-N',N'-dimethylpropane-1,3-diamine
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| Synonyms |
SCH-529074; SCH529074; SCH 529074
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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 |
| 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: ~20 mg/mL (~35.5 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1 mg/mL (1.77 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 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: ≥ 1 mg/mL (1.77 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 10.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.7744 mL | 8.8720 mL | 17.7440 mL | |
| 5 mM | 0.3549 mL | 1.7744 mL | 3.5488 mL | |
| 10 mM | 0.1774 mL | 0.8872 mL | 1.7744 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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