| Size | Price | Stock | Qty |
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| 1mg |
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| Other Sizes |
| Targets |
CCTA-1523 targets the ATP-binding cassette (ABC) transporter ABCG2, which is responsible for the efflux of chemotherapeutic agents from cancer cells, reducing their intracellular accumulation and therapeutic efficacy. By inhibiting ABCG2, CCTA-1523 reverses ABCG2-mediated multidrug resistance (MDR) in cancer cells. It selectively and reversibly inhibits the efflux function of ABCG2.
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| ln Vitro |
Against H460, H460/MX20, HEK293/pcDNA3.1, HEK/R482, HEK/R482G, and HEK/R482T, CCTA-1523 (0-1000 µM; 72 hours) exhibits cytotoxicity [1].
CCTA-1523 exhibits cytotoxicity and anticancer activity in vitro. It selectively reverses ABCG2-mediated MDR in cancer cells. At a concentration of 5 μM, it restores drug sensitivity in ABCG2-overexpressing cells. The compound demonstrates high specificity for ABCG2 and does not significantly affect other ABC transporters. Its inhibitory effect is fully reversible. |
| ln Vivo |
CCTA-1523 (75 mg/kg; chamber; q3d x 6) suppresses tumor growth and increases the length of survival in mice when coupled with doxorubicin (1.8 mg/kg, i.p., q3d x 6) [1].
CCTA-1523 has demonstrated in vivo anticancer activity. When used in combination with doxorubicin, it restores the in vivo antitumor activity of doxorubicin in ABCG2-overexpressing tumor xenograft models. It enhances the efficacy of doxorubicin in xenograft models, demonstrating its potential to overcome ABCG2-mediated drug resistance in vivo. |
| Enzyme Assay |
CCTA-1523's activity as an ABCG2 inhibitor is assessed using in vitro transporter assays. These assays measure the compound's ability to inhibit the efflux of ABCG2 substrates, such as chemotherapeutic agents or fluorescent dyes. The compound's selectivity for ABCG2 over other ABC transporters is evaluated to confirm its specificity. The reversibility of its inhibition is also characterized.
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| Cell Assay |
Cellular assays for CCTA-1523 involve treating ABCG2-overexpressing cancer cells with the compound and measuring its ability to reverse drug resistance. Cells are co-treated with CCTA-1523 and a chemotherapeutic agent (e.g., doxorubicin), and cell viability is assessed to determine the restoration of drug sensitivity. The compound's effect on ABCG2 protein expression is also evaluated.
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| Animal Protocol |
Animal/Disease Models: NCR nude mice (H460/MX20 xenograft) [1]
Doses: 75 mg/kg (DOX; 1.8 mg/kg, ip, q3d x 6) Route of Administration: Po; q3d x 6 Experimental Results: Significant inhibition Growth of H460/MX20 tumor xenografts when combined with doxorubicin compared to vehicle controls. In vivo animal model protocols for CCTA-1523 involve its administration to tumor-bearing mice with ABCG2-overexpressing xenografts. The compound is typically administered orally or in combination with a chemotherapeutic agent. Tumor growth inhibition and drug accumulation in tumor tissues are measured to assess the compound's efficacy in reversing MDR in vivo. |
| ADME/Pharmacokinetics |
CCTA-1523 is an orally active compound. It has a molecular weight of 340.2 and a molecular formula of C16H15Cl2NO3. The compound is soluble in DMSO and is supplied as a solid powder. Its pharmacokinetic properties support oral administration and in vivo efficacy.
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| Toxicity/Toxicokinetics |
CCTA-1523 is intended for research use only and not for human consumption. As a research compound, its comprehensive toxicological profile may not be fully characterized. However, its use in xenograft models suggests it is well-tolerated at efficacious doses. Standard safety assessments would be required for clinical development.
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| References | |
| Additional Infomation |
CCTA-1523 (CAS# 1616271-41-0) is a research compound used to study ABCG2-mediated multidrug resistance in cancer. It is not approved for clinical use. The compound is a potent, selective, reversible, and orally active ABCG2 inhibitor with demonstrated efficacy in reversing drug resistance in vitro and in vivo. It is a valuable tool for developing strategies to overcome MDR.
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| Molecular Formula |
C16H15CL2NO3
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|---|---|
| Molecular Weight |
340.20
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| Exact Mass |
339.042
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| CAS # |
1616271-41-0
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| PubChem CID |
73438576
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| Appearance |
Typically exists as solid at room temperature
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| LogP |
4
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
3
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
22
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| Complexity |
367
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| Defined Atom Stereocenter Count |
0
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| SMILES |
COC1=C(C=C(C=C1)C2=CC(=CC=C2)NC(=O)C(Cl)Cl)OC
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| InChi Key |
KVFQJGFFQSVTND-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C16H15Cl2NO3/c1-21-13-7-6-11(9-14(13)22-2)10-4-3-5-12(8-10)19-16(20)15(17)18/h3-9,15H,1-2H3,(H,19,20)
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| Chemical Name |
2,2-dichloro-N-[3-(3,4-dimethoxyphenyl)phenyl]acetamide
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| Synonyms |
CCTA 1523; CCTA1523; CCTA-1523
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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) |
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
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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 | 2.9394 mL | 14.6972 mL | 29.3945 mL | |
| 5 mM | 0.5879 mL | 2.9394 mL | 5.8789 mL | |
| 10 mM | 0.2939 mL | 1.4697 mL | 2.9394 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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