Y06036
Based on 1 publication(s) in Google Scholar
Y06036 is a potent and selective BET inhibitor, which binds to the BRD4(1) bromodomain with Kd value of 82 nM. Antitumor activity.
Para uso exclusivo en investigación. No vendemos a pacientes.
- Pureza: 98.57%
- No. CAS: 1832671-96-1
- Fòrmula: C16H15BrN2O5S
- Peso molecular:427.27
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Almacenamiento:Powder -20°C, 3 years , 4°C, 2 years ; In solvent -80°C, 2 years , -20°C, 1 year
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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
Publications Citing Use of MedChemExpress (MCE) Y06036
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Actividad biológica
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BRD4(1) 82 nM (Kd) |
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Cell Line
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Type | Value | Description | References |
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| A549 | IC50 |
>5 μM
Compound: 6i
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Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer glo assay
Antiproliferative activity against human A549 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer glo assay
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[PMID: 29566488] |
| CWR22R | IC50 |
1.5 μM
Compound: 6i
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Antiproliferative activity against AR-positive human 22Rv1 cells assessed as reduction in cell viability incubated for 96 hrs by cell-titer glo assay
Antiproliferative activity against AR-positive human 22Rv1 cells assessed as reduction in cell viability incubated for 96 hrs by cell-titer glo assay
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[PMID: 29566488] |
| DU-145 | IC50 |
>6 μM
Compound: 6i
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Antiproliferative activity against AR-negative human DU-145 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer glo assay
Antiproliferative activity against AR-negative human DU-145 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer glo assay
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[PMID: 29566488] |
| HeLa | IC50 |
>5 μM
Compound: 6i
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Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer glo assay
Antiproliferative activity against human HeLa cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer glo assay
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[PMID: 29566488] |
| HFL1 | IC50 |
18.2 μM
Compound: 6i
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Cytotoxicity against human HFL1 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer glo assay
Cytotoxicity against human HFL1 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer glo assay
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[PMID: 29566488] |
| Hs-578T | IC50 |
1 μM
Compound: 6i
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Antiproliferative activity against human Hs-578T cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer glo assay
Antiproliferative activity against human Hs-578T cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer glo assay
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[PMID: 29566488] |
| HT-29 | IC50 |
0.4 μM
Compound: 6i
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Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability incubated for 120 hrs by cell-titer glo assay
Antiproliferative activity against human HT-29 cells assessed as reduction in cell viability incubated for 120 hrs by cell-titer glo assay
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[PMID: 29566488] |
| LNCaP | IC50 |
1.06 μM
Compound: 6i
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Antiproliferative activity against AR-positive human LNCAP cells assessed as reduction in cell viability incubated for 96 hrs by cell-titer glo assay
Antiproliferative activity against AR-positive human LNCAP cells assessed as reduction in cell viability incubated for 96 hrs by cell-titer glo assay
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[PMID: 29566488] |
| LNCaP C4-2B | IC50 |
2.62 μM
Compound: 6i
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Antiproliferative activity against AR-positive human C4-2B cells assessed as reduction in cell viability incubated for 96 hrs by cell-titer glo assay
Antiproliferative activity against AR-positive human C4-2B cells assessed as reduction in cell viability incubated for 96 hrs by cell-titer glo assay
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[PMID: 29566488] |
| MCF7 | IC50 |
1 μM
Compound: 6i
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Antiproliferative activity against human MCF-7 cells assessed as reduction in cell viability incubated for 96 hrs by cell-titer glo assay
Antiproliferative activity against human MCF-7 cells assessed as reduction in cell viability incubated for 96 hrs by cell-titer glo assay
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[PMID: 29566488] |
| MV4-11 | IC50 |
0.4 μM
Compound: 6i
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Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 120 hrs by cell-titer glo assay
Antiproliferative activity against human MV4-11 cells assessed as reduction in cell viability incubated for 120 hrs by cell-titer glo assay
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[PMID: 29566488] |
| NCI-H1975 | IC50 |
2.5 μM
Compound: 6i
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Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer glo assay
Antiproliferative activity against human NCI-H1975 cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer glo assay
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[PMID: 29566488] |
| PC-3 | IC50 |
>3 μM
Compound: 6i
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Antiproliferative activity against AR-negative human PC-3 cells assessed as reduction in cell viability incubated for 96 hrs by cell-titer glo assay
Antiproliferative activity against AR-negative human PC-3 cells assessed as reduction in cell viability incubated for 96 hrs by cell-titer glo assay
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[PMID: 29566488] |
| U2OS | IC50 |
>5 μM
Compound: 6i
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Antiproliferative activity against human U2OS cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer glo assay
Antiproliferative activity against human U2OS cells assessed as reduction in cell viability incubated for 72 hrs by cell-titer glo assay
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[PMID: 29566488] |
| VCaP | IC50 |
0.63 μM
Compound: 6i
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Antiproliferative activity against AR-positive human VCaP cells assessed as reduction in cell viability incubated for 144 hrs by cell-titer glo assay
Antiproliferative activity against AR-positive human VCaP cells assessed as reduction in cell viability incubated for 144 hrs by cell-titer glo assay
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[PMID: 29566488] |
Y06036 (0.001-100 nM, 96 hours for LNCaP, C4-2B, and 22Rv1 cells; 144 hours for VCaP cells) exhibits low micromolar or nanomolar potencies (IC50: 0.29-2.6 μΜ) in the four androgen receptor (AR)-positive prostate cancer cell lines LNCaP, C4-2B, 22Rv1, and VCaP. Treatment of 22Rv1 cells with Y06036 (1, 2, 4, 8, and 16 μM, 48 hours) results in significant down-regulation of both full-length (AR-fl) and AR variants levels[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:LNCaP, C4-2B, 22Rv1, and VCaP prostate cancer cells
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Concentration:0.001-100 μM
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Incubation Time:96 hours for LNCaP, C4-2B, and 22Rv1; 144 hours for VCaP
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Result:Inhibited LNCaP, C4-2B, 22Rv1, and VCaP cells with IC50s of 1.06, 2.62, 1.50, 0.63 μM, respectively.
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Cell Line:22Rv1 cells
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Concentration:1,2,4,8, and 16 μM
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Incubation Time:48 hours
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Result:Resulted in significant down-regulation of both AR-fl and AR variants levels
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Four-week-old male mice (strain: C.B-17/IcrHsd-Prkdcscid for C4-2B) with C4-2B mouse xenograft model[1]
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Dosage:50 mg/kg, 100 μL
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Administration:Intraperitoneal (i.p.) injection, 5 times per week, 25 days
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Result:Exhibited strong antitumor activities during the 25-day treatment period, with a tumor growth inhibition (TGI) of 70%.
Chemical Information
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No. CAS 1832671-96-1
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Appearance Solid
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Peso molecular 427.27
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Fòrmula C16H15BrN2O5S
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Color Light yellow to yellow
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SMILES
BrC1=CC(S(=O)(NC2=C(OC)C=C(ON=C3C)C3=C2)=O)=C(OC)C=C1
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Powder -20°C 3 years 4°C 2 years In solvent -80°C 2 years -20°C 1 year
Publications (1)
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Journal Impact Factor
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Most Recent
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ACS Nano
Nanopore Discrimination of Protein-Small-Molecule Drug Complexes at Near-Atomic Resolution. [Abstract]2026 May 12;20(18):13624-13635. PMID: 42046448
Solvente y solubilidad
DMSO : 130 mg/mL (304.26 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.17 mg/mL (5.08 mM); Clear solution
This protocol yields a clear solution of ≥ 2.17 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (21.7 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Please enter the basic information of animal experiments:
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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL.
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
Pureza y Documentación
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Ficha de datos (279 KB)
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SDS (393 KB)
- English - EN (393 KB)
- Français - FR (393 KB)
- Deutsch - DE (393 KB)
- Norwegian - NO (393 KB)
- Español - ES (393 KB)
- Swedish - SV (393 KB)
- Italian - IT (393 KB)
- Korean - KR (393 KB)
- Portuguese - PT (393 KB)
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Instrucciones de manejo (2659 KB)
Referencias
Complete Stock Solution Preparation Table
Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 2 years; -20°C, 1 year. When stored at -80°C, please use it within 2 years. When stored at -20°C, please use it within 1 year.
| Optional Solvent | Concentration Solvent Mass | 1 mg | 5 mg | 10 mg | 25 mg |
|---|---|---|---|---|---|
| DMSO | 1 mM | 2.3404 mL | 11.7022 mL | 23.4044 mL | 58.5110 mL |
| 5 mM | 0.4681 mL | 2.3404 mL | 4.6809 mL | 11.7022 mL | |
| 10 mM | 0.2340 mL | 1.1702 mL | 2.3404 mL | 5.8511 mL | |
| 15 mM | 0.1560 mL | 0.7801 mL | 1.5603 mL | 3.9007 mL | |
| 20 mM | 0.1170 mL | 0.5851 mL | 1.1702 mL | 2.9256 mL | |
| 25 mM | 0.0936 mL | 0.4681 mL | 0.9362 mL | 2.3404 mL | |
| 30 mM | 0.0780 mL | 0.3901 mL | 0.7801 mL | 1.9504 mL | |
| 40 mM | 0.0585 mL | 0.2926 mL | 0.5851 mL | 1.4628 mL | |
| 50 mM | 0.0468 mL | 0.2340 mL | 0.4681 mL | 1.1702 mL | |
| 60 mM | 0.0390 mL | 0.1950 mL | 0.3901 mL | 0.9752 mL | |
| 80 mM | 0.0293 mL | 0.1463 mL | 0.2926 mL | 0.7314 mL | |
| 100 mM | 0.0234 mL | 0.1170 mL | 0.2340 mL | 0.5851 mL |
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