| Size | Price | Stock | Qty |
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| 5mg |
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| 10mg |
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| 25mg |
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| 50mg |
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| 100mg |
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| 250mg |
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| Targets |
YHO-13177 targets the breast cancer resistance protein (BCRP/ABCG2), an ATP-binding cassette (ABC) transporter involved in multidrug resistance. By blocking BCRP activity, YHO-13177 reverses BCRP-mediated drug resistance and potentiates the cytotoxicity of chemotherapeutic agents such as SN-38 in cancer cells.
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| ln Vitro |
YHO-13177 is a potent and specific inhibitor of BCRP/ABCG2. It potentiates the cytotoxicity of SN-38 in cancer cells. The compound has no effect on P-glycoprotein-mediated paclitaxel resistance in MDR1-transduced human leukemia K562 cells, indicating its specificity for BCRP. YHO-13177 can specifically reverse BCRP/ABCG2-mediated drug resistance in vitro.
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| ln Vivo |
YHO-13177 can specifically reverse BCRP/ABCG2-mediated drug resistance in vivo. As a potent and specific inhibitor of BCRP, it is expected to enhance the efficacy of chemotherapeutic agents that are substrates of BCRP in animal models. Further studies are needed to fully characterize its in vivo pharmacokinetic and pharmacodynamic profiles.
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| Enzyme Assay |
The in vitro assay for YHO-13177 typically involves measuring its inhibitory activity against BCRP/ABCG2 using standard transporter assays. The compound is tested for its ability to inhibit the efflux of BCRP substrates (e.g., mitoxantrone, Hoechst 33342) in cells expressing BCRP. The IC50 value is determined from the dose-response curve.
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| Cell Assay |
The in vitro cellular assay for YHO-13177 typically involves culturing cancer cell lines that express BCRP (e.g., cancer cells with acquired drug resistance) in appropriate growth media. Cells are treated with varying concentrations of the compound in combination with chemotherapeutic agents such as SN-38, and cell viability is assessed using standard assays such as MTT or CellTiter-Glo. The reversal of drug resistance is quantified by determining the fold change in IC50.
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| Animal Protocol |
In vivo animal studies for YHO-13177 would typically involve the use of mouse xenograft models bearing BCRP-expressing tumors. Tumor-bearing mice would be administered the compound via appropriate routes (e.g., oral gavage or intraperitoneal injection) in combination with chemotherapeutic agents. Tumor growth inhibition would be monitored over several weeks, and endpoints would include tumor volume measurements and assessment of drug accumulation in tumors.
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| ADME/Pharmacokinetics |
YHO-13177 has a molecular weight of 370.5 g/mol and a molecular formula of C20H22N2O3S. It is soluble in DMSO (70 mg/mL). The IUPAC name is (Z)-2-(3,4-dimethoxyphenyl)-3-(5-(4-hydroxypiperidin-1-yl)thiophen-2-yl)acrylonitrile. The compound should be stored under recommended conditions. Further detailed PK parameters are available from the manufacturer's data sheets.
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| Toxicity/Toxicokinetics |
Specific toxicology data for YHO-13177 are not available in the public domain. The compound is intended for research use only and should be handled with appropriate laboratory safety precautions. Standard safety assessments would be required before any clinical application. Researchers should consult the safety data sheet for detailed handling and disposal information.
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| References |
: Zhang L, Zhao J, Liang C, Liu M, Xu F, Wang X. A novel biosensor based on intestinal 3D organoids for detecting the function of BCRP. Drug Deliv. 2017 Nov;24(1):1453-1459. doi: 10.1080/10717544.2017.1381199. PubMed PMID: 28949254.
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| Additional Infomation |
YHO-13177 is a potent and specific inhibitor of breast cancer resistance protein (BCRP/ABCG2). It is an acrylonitrile derivative and the active form of YHO-13351 that can specifically reverse BCRP/ABCG2-mediated drug resistance in vitro and in vivo. The compound is used in research to study multidrug resistance in cancer. It has not yet entered clinical trials and is strictly for preclinical research purposes.
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| Molecular Formula |
C20H22N2O3S
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|---|---|
| Molecular Weight |
370.46
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| Exact Mass |
370.135
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| Elemental Analysis |
C, 64.84; H, 5.99; N, 7.56; O, 12.96; S, 8.65
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| CAS # |
912287-56-0
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| Related CAS # |
912287-56-0;
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| PubChem CID |
16757522
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| Appearance |
Light yellow to yellow solid powder
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| LogP |
3.855
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| Hydrogen Bond Donor Count |
1
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| Hydrogen Bond Acceptor Count |
6
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| Rotatable Bond Count |
5
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| Heavy Atom Count |
26
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| Complexity |
538
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C(/C1C=CC(OC)=C(OC)C=1)(\C#N)=C\C1=CC=C(N2CCC(O)CC2)S1
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| InChi Key |
NOGGBVNCVONHHC-RVDMUPIBSA-N
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| InChi Code |
InChI=1S/C20H22N2O3S/c1-24-18-5-3-14(12-19(18)25-2)15(13-21)11-17-4-6-20(26-17)22-9-7-16(23)8-10-22/h3-6,11-12,16,23H,7-10H2,1-2H3/b15-11+
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| Chemical Name |
(Z)-2-(3,4-Dimethoxyphenyl)-3-(5-(4-hydroxypiperidin-1-yl)thiophen-2-yl)acrylonitrile
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| Synonyms |
YHO-13177 YHO 13177 YHO13177
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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 : ~33.33 mg/mL (~89.97 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 2.5 mg/mL (6.75 mM) (saturation unknown) in 10% DMSO + 40% PEG300 +5% Tween-80 + 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 25.0 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. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 2.6993 mL | 13.4967 mL | 26.9935 mL | |
| 5 mM | 0.5399 mL | 2.6993 mL | 5.3987 mL | |
| 10 mM | 0.2699 mL | 1.3497 mL | 2.6993 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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