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PhiKan-083, a carbazole analog, is a novel and potent stabilizer of p53 mutant Y220C that can stabilize Y220C (a p53 mutant) with a Kd of 167 μM. Has anticancer activity.
| ln Vitro |
PhiKan 083, a derivative of carbazole, has a Kd of 167 μM[1] and a relative binding affinity (Kd) of 150 μM for p53Y220C in Ln229 cells[3]. It binds to surface cavities and stabilizes Y220C (p53 mutant). Its thermal denaturation rate is slowed down by PhiKan 083 [2]. Engineered Ln229 cell variations' cell viability is decreased by PhiKan 083 (125 μM, 48 hours) [3]. In Ln229 cells, combining PhiKan 083 (100 μM) with NSC 123127 (1 μM) increases the pro-apoptotic activity of all variants (p53wt, p53Y220C, p53G245S, and p53R282W) [3].
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| Cell Assay |
Cell Viability Assay [1]
Cell Types: Ln229, Ln229-p53-wt, Ln229-p53-Y220C, Ln229-p53-G245S, Ln229-p53-R282W Cell Tested Concentrations: 125 μM Incubation Duration: 48 hrs (hours) Experimental Results: Caused ∼70 ± The Ln229 cell variant had a 5% reduction in cell viability. |
| References |
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| Molecular Formula |
C16H19CLN2
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|---|---|
| Molecular Weight |
274.79
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| Exact Mass |
274.123
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| CAS # |
1050480-30-2
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| Related CAS # |
PhiKan 083;880813-36-5
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| PubChem CID |
16255105
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| Appearance |
White to off-white solid powder
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
19
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| Complexity |
278
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| Defined Atom Stereocenter Count |
0
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| SMILES |
Cl.N1(CC)C2C=CC=CC=2C2C=C(CNC)C=CC1=2
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| InChi Key |
IXWVUPURFWFRNE-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H18N2.ClH/c1-3-18-15-7-5-4-6-13(15)14-10-12(11-17-2)8-9-16(14)18;/h4-10,17H,3,11H2,1-2H3;1H
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| Chemical Name |
1-(9-ethylcarbazol-3-yl)-N-methylmethanamine;hydrochloride
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| Synonyms |
PhiKan 083; PhiKan083; PhiKan-083;
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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, avoid exposure to moisture. |
| 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 : ~62.5 mg/mL (~227.45 mM)
H2O : ~2 mg/mL (~7.28 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 | 3.6391 mL | 18.1957 mL | 36.3914 mL | |
| 5 mM | 0.7278 mL | 3.6391 mL | 7.2783 mL | |
| 10 mM | 0.3639 mL | 1.8196 mL | 3.6391 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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