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Carbonic anhydrase inhibitor 12 2883451-38-3

Carbonic anhydrase inhibitor 12 2883451-38-3

CAS No.: 2883451-38-3

Carbonic anhydrase inhibitor 12 is a potent inhibitor of CA II and also exhibits inhibitory effect against CA I (Kis of
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Carbonic anhydrase inhibitor 12 is a potent inhibitor of CA II and also exhibits inhibitory effect against CA I (Kis of CA II and CA I are 1.72 nM and 271 nM, respectively). Carbonic anhydrase inhibitor 12 has strong anti-cancer activity against different tumor cell lines.

Physicochemical Properties


CAS # 2883451-38-3
Appearance Typically exists as solid at room temperature
HS Tariff Code 2934.99.9001
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)

Biological Activity


Targets CA Ⅱ
ln Vitro Carbonic anhydrase inhibitor 12 (Compound 14h) (10 μM; 48 hours; single) has a significant impact on the inhibitory potency and specificity against several cancer cell lines[1]. Carbonic anhydrase inhibitor 12 (2.5 μM in MDA-MB-231 and 2.4 μM in MCF-7; 48 hours) can stop MCF-7 and MDA-MB-231 cells in their G2/M phase of the cell cycle[1]. When compared to the untreated control cells, carbonic anhydrase inhibitor 12 (2.4 μM in MCF-7 and 2.5 μM in MDA-MB-231; 48 hours) increases the early and late apoptotic phases[1].
Cell Assay Cell Proliferation Assay
Cell Types: MCF-7, T47D, MDA-MB-231, COLO 205, HCT-116, HT29, SW-620, A549, SK-OV-3 and NCI-ADR-RES[1] Tested
Tested Concentrations: 10 μM
Incubation Duration: 48 hrs (hours)
Experimental Results: demonstrated a mean growth inhibitory activity of 55.12% and a broad range of antiproliferative activity against most of the tested cancer cell lines.

Cell Cycle Analysis
Cell Types: MCF-7 and MDA-MB-231[1] Tested
Tested Concentrations: 2.4 μM in MCF-7, 2.5 μM MDA-MB-231
Incubation Time: 48 hrs (hours)
Experimental Results: Arrested the cell cycle of MCF-7 and MDA-MB-231 cells at the G2/M phase.

Apoptosis Analysis
Cell Types: MCF-7 and MDA-MB-231[1] Tested
Tested Concentrations: 2.4 μM in MCF -7, 2.5 μM MDA-MB-231
Incubation Duration: 48 hrs (hours)
Experimental Results: Demonstrated an increase in the early apoptotic and late apoptotic phase in comparison to the control untreated cells.
References

[1]. Application of the dual-tail approach for the design and synthesis of novel Thiopyrimidine-Benzenesulfonamide hybrids as selective carbonic anhydrase inhibitors. Eur J Med Chem. 2022;228:114004.


Solubility Data


Solubility (In Vitro) May dissolve in DMSO (in most cases), if not, try other solvents such as H2O, Ethanol, or DMF with a minute amount of products to avoid loss of samples
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
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*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).
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)]
*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.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300:Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL 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).
Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)