| Size | Price | Stock | Qty |
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| 1mg |
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| 5mg |
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| 10mg |
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| 50mg |
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| Other Sizes |
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| 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 |
C16H18N2.HCL
|
|---|---|
| Molecular Weight |
274.78846
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| Exact Mass |
238.146
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| CAS # |
880813-36-5
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| Related CAS # |
PhiKan 083 hydrochloride;1050480-30-2
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| PubChem CID |
4722579
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| Appearance |
Colorless to light yellow solid powder
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| LogP |
4.726
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
1
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| Rotatable Bond Count |
3
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| Heavy Atom Count |
18
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| Complexity |
278
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| Defined Atom Stereocenter Count |
0
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| InChi Key |
LBPNOEAFWYTTEB-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H18N2/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
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| Chemical Name |
1-(9-ethylcarbazol-3-yl)-N-methylmethanamine
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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 : ~100 mg/mL (~419.59 mM)
Ethanol : ~100 mg/mL (~419.59 mM) |
|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (10.49 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 25.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. Solubility in Formulation 2: ≥ 2.17 mg/mL (9.11 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 21.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL 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. View More
Solubility in Formulation 3: 2.17 mg/mL (9.11 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. |
| 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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