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| 1mg |
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| 5mg |
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| Targets |
SLMP53-1 targets the tumor suppressor protein p53, which is mutated in many cancers. The compound is a reactivator of both wild-type and mutant p53. By reactivating p53, SLMP53-1 induces p53-dependent anti-proliferative activity in tumor cells. The compound also mediates reprogramming of glucose metabolism in cancer cells and reduces angiogenesis. These multiple mechanisms contribute to its antitumor activity.
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| ln Vitro |
In vitro, SLMP53-1 shows p53-dependent anti-proliferative activity in human wt and mut p53R280K-expressing tumor cells. It mediates reprogramming of glucose metabolism in cancer cells. The compound reduces angiogenesis, decreases endothelial cell tube formation, and reduces VEGF expression levels. SLMP53-1 inhibits tumor cell growth.
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| ln Vivo |
Specific in vivo data for SLMP53-1 are limited. The compound has promising antitumor activity and can be used to study human rectal cancer. However, detailed in vivo efficacy studies in animal models have not been extensively reported. The compound is primarily used as a research tool for studying p53 reactivation in cancer.
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| Enzyme Assay |
In vitro binding assays for SLMP53-1 measure its interaction with p53. Surface plasmon resonance (SPR) or other biophysical methods can be used to characterize the compound's binding to p53. Cell-based assays measure p53-dependent transcriptional activity and anti-proliferative effects.
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| Cell Assay |
Cell-based assays for SLMP53-1 are conducted in cancer cell lines expressing wild-type or mutant p53. Cells are treated with the compound at various concentrations, and cell viability is assessed using MTT or similar assays. p53 activity is assessed by measuring the expression of p53 target genes. Glucose metabolism is assessed by measuring glucose uptake and lactate production. Angiogenesis is assessed in endothelial cell tube formation assays.
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| Animal Protocol |
In vivo animal experiments with SLMP53-1 have not been extensively documented. Typical study designs would involve administration of the compound in xenograft models to evaluate antitumor efficacy. Dosing regimens and routes of administration would need to be optimized. The compound is for research use only.
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| ADME/Pharmacokinetics |
Pharmacokinetic properties of SLMP53-1 are not extensively characterized. The compound has a molecular formula of C20H18N2O2 and a molecular weight of 318.37. Solubility: DMSO: 100 mg/mL (314.10 mM; Need ultrasonic). Storage: powder at -20°C for 3 years; in solvent at -80°C for 1 year.
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| Toxicity/Toxicokinetics |
Safety and toxicology data for SLMP53-1 are limited. The compound is for research use only and is not approved for human therapeutic use. Standard laboratory safety precautions should be followed when handling the compound. No specific toxicity data are available.
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| References |
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| Additional Infomation |
SLMP53-1 has CAS number 1643469-17-3, molecular formula C20H18N2O2, and molecular weight 318.37. It is a reactivator of wild-type and mutant p53 with antitumor activity. It mediates reprogramming of glucose metabolism and reduces angiogenesis. Not for human use; for research purposes only.
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| Molecular Formula |
C20H18N2O2
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|---|---|
| Molecular Weight |
318.369124889374
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| Exact Mass |
318.136
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| CAS # |
1643469-17-3
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| PubChem CID |
86346168
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| Appearance |
White to off-white solid powder
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| LogP |
3.1
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
2
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| Rotatable Bond Count |
2
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| Heavy Atom Count |
24
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| Complexity |
524
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| Defined Atom Stereocenter Count |
2
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| SMILES |
O1C[C@H](CC2=CNC3C=CC=CC2=3)N2C(C3C=CC=CC=3[C@@]12C)=O
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| InChi Key |
RSAFMLBHKXOCJG-VBKZILBWSA-N
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| InChi Code |
InChI=1S/C20H18N2O2/c1-20-17-8-4-2-7-16(17)19(23)22(20)14(12-24-20)10-13-11-21-18-9-5-3-6-15(13)18/h2-9,11,14,21H,10,12H2,1H3/t14-,20+/m0/s1
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| Chemical Name |
(3S,9bR)-3-(1H-indol-3-ylmethyl)-9b-methyl-2,3-dihydro-[1,3]oxazolo[2,3-a]isoindol-5-one
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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 : ~250 mg/mL (~785.25 mM)
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| Solubility (In Vivo) |
Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.
Injection Formulations
Injection Formulation 1: DMSO : Tween 80： Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution → 50 μL Tween 80 → 850 μL Saline)(e.g. IP/IV/IM/SC) *Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution. Injection Formulation 2: DMSO : PEG300 ：Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO → 400 μLPEG300 → 50 μL Tween 80 → 450 μL Saline) Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO → 900 μL Corn oil) Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals). View More
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO → 900 μL (20% SBE-β-CD in saline)] Oral Formulations
Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium) Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals). View More
Oral Formulation 3: Dissolved in PEG400 (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 3.1410 mL | 15.7050 mL | 31.4100 mL | |
| 5 mM | 0.6282 mL | 3.1410 mL | 6.2820 mL | |
| 10 mM | 0.3141 mL | 1.5705 mL | 3.1410 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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