| Size | Price | Stock | Qty |
|---|---|---|---|
| 5mg |
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| 10mg |
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| Other Sizes |
| Targets |
ABCG2 (BCRP)
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|---|---|
| ln Vitro |
Ac32Az19 is a potent BCRP inhibitor with an EC₅0 of 13 nM in BCRP‑overexpressing HEK293/R2 cells. It is highly selective for BCRP over other ABC transporters. By inhibiting BCRP‑mediated drug efflux, it enhances the intracellular accumulation of BCRP substrate drugs, including chemotherapeutic agents (e.g., mitoxantrone, topotecan, SN-38) and fluorescent probes (e.g., pheophorbide A, Hoechst 33342).
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| ln Vivo |
No detailed in vivo activity data for Ac32Az19 has been reported. As a potent and non‑toxic BCRP inhibitor, it is expected to enhance the oral bioavailability and brain penetration of BCRP substrate drugs in animal models. It may also reverse BCRP‑mediated multidrug resistance in mouse xenograft models when co‑administered with chemotherapeutic agents.
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| Enzyme Assay |
For BCRP efflux activity assays, membrane vesicles from BCRP‑overexpressing cells are incubated with a fluorescent BCRP substrate (e.g., Hoechst 33342 or pheophorbide A) and various concentrations of Ac32Az19 (0.1‑1000 nM). Substrate accumulation in vesicles is measured by fluorescence. EC₅0 values are calculated from dose‑response curves.
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| Cell Assay |
Ac32Az19 is dissolved in DMSO (up to 60 mg/mL) and diluted in cell culture media (final DMSO ≤0.1%). BCRP‑overexpressing HEK293/R2 cells are treated with Ac32Az19 (1‑1000 nM) in the presence of a fluorescent BCRP substrate (e.g., pheophorbide A). Intracellular substrate accumulation is measured by flow cytometry or fluorescence microscopy. Cell viability is assessed by MTT assays to confirm non‑toxicity.
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| Animal Protocol |
No detailed in vivo protocol for Ac32Az19 has been reported. For BCRP inhibition studies, the compound would be formulated in a suitable vehicle (e.g., 10% DMSO, 40% PEG400, 5% Tween 80) and administered orally or intraperitoneally to mice, either alone or in combination with a BCRP substrate drug. Plasma and tissue levels of the substrate drug would be measured by LC‑MS/MS.
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| ADME/Pharmacokinetics |
No PK data for Ac32Az19 has been reported. As a potent BCRP inhibitor, it is expected to have sufficient systemic exposure to inhibit BCRP in target tissues (e.g., intestine, liver, blood‑brain barrier). Detailed parameters such as half‑life, Cmax, and clearance are not publicly available. Solubility in DMSO is 60 mg/mL.
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| Toxicity/Toxicokinetics |
Ac32Az19 is reported to be non‑toxic in cell‑based assays, with no significant reduction in cell viability at concentrations up to 10 uM in HEK293/R2 cells. No in vivo toxicity data has been reported. The non‑toxic profile makes it attractive for combination therapy and for studying BCRP biology without confounding cytotoxic effects.
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| References | |
| Additional Infomation |
Ac32Az19 (CAS: 2760674-72-2; formula: C3₇H33N3O₆; MW: 615.67) is a potent, non‑toxic, and highly selective BCRP inhibitor based on a synthetic triazole‑containing flavonoid scaffold. It inhibits BCRP with an EC₅0 of 13 nM in BCRP‑overexpressing cells. The compound is for research use only; no clinical trials or regulatory approvals have been reported. It is stored at 4degC, away from moisture and light.
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| Molecular Formula |
C37H33N3O6
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|---|---|
| Molecular Weight |
615.674429655075
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| Exact Mass |
615.236
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| CAS # |
2760674-72-2
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| PubChem CID |
162640934
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| Appearance |
Off-white to light yellow solid powder
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| LogP |
6.7
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| Hydrogen Bond Donor Count |
0
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| Hydrogen Bond Acceptor Count |
8
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| Rotatable Bond Count |
14
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| Heavy Atom Count |
46
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| Complexity |
1020
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(OC)(=O)C1=CC=CC(COC2C(=O)C3=CC=CC=C3OC=2C2=CC=C(OCCCCC3=CN(CC4=CC=CC=C4)N=N3)C=C2)=C1
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| InChi Key |
BECCUKCZBHNIBT-UHFFFAOYSA-N
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| InChi Code |
InChI=1S/C37H33N3O6/c1-43-37(42)29-13-9-12-27(22-29)25-45-36-34(41)32-15-5-6-16-33(32)46-35(36)28-17-19-31(20-18-28)44-21-8-7-14-30-24-40(39-38-30)23-26-10-3-2-4-11-26/h2-6,9-13,15-20,22,24H,7-8,14,21,23,25H2,1H3
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| Chemical Name |
methyl 3-[[2-[4-[4-(1-benzyltriazol-4-yl)butoxy]phenyl]-4-oxochromen-3-yl]oxymethyl]benzoate
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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 (e.g. under nitrogen), avoid exposure to moisture and light. |
| 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: 60 mg/mL (97.45 mM)
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|---|---|
| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 3 mg/mL (4.87 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 30.0 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.6242 mL | 8.1212 mL | 16.2425 mL | |
| 5 mM | 0.3248 mL | 1.6242 mL | 3.2485 mL | |
| 10 mM | 0.1624 mL | 0.8121 mL | 1.6242 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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