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Y06137
🥰Excellent
Catalog No. T13363Cas No. 2226534-49-0
Y06137 is an effective and selective BET inhibitor with a Kd of 81 nM for BRD4(1) bromodomain. Y06137 can be used for research on the treatment of castration-resistant prostate cancer.
Y06137
🥰Excellent
Purity: 97.27%
Catalog No. T13363Cas No. 2226534-49-0
Y06137 is an effective and selective BET inhibitor with a Kd of 81 nM for BRD4(1) bromodomain. Y06137 can be used for research on the treatment of castration-resistant prostate cancer.
| Pack Size | Price | Availability | Quantity |
|---|---|---|---|
| 1 mg | $55 | In Stock | |
| 2 mg | $79 | In Stock | |
| 5 mg | $129 | In Stock | |
| 10 mg | $213 | In Stock | |
| 25 mg | $396 | In Stock | |
| 1 mL x 10 mM (in DMSO) | $143 | In Stock |
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CitedSelect Batch
Purity:97.27%
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With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.Product Introduction
Bioactivity
Chemical Properties
| Description | Y06137 is an effective and selective BET inhibitor with a Kd of 81 nM for BRD4(1) bromodomain. Y06137 can be used for research on the treatment of castration-resistant prostate cancer. |
| Targets&IC50 | BRD4(1):81 nM (kd) |
| In vitro | Treatment of AR-positive prostate cancer cell lines 22Rv1 cells with Y06137 (1, 2, 4, 8, and 16 μM, 48 hours) results in significant down-regulation of both full-length (AR-fl) and AR variants levels. Y06137 (0.001-100 nM) exhibits low micromolar or nanomolar potencies in the four androgen receptor (AR)-positive prostate cancer cell lines LNCaP, C4-2B, 22Rv1, and VCaP cells with IC50s of 0.47, 0.84, 0.70, 0.29 μM, respectively[1]. |
| In vivo | Y06137 (50 mg/kg, i.p., 100 μL) exhibited potent antitumor activity in a C4-2B CRPC xenograft tumor model in mice, achieving a tumor growth inhibition (TGI) of 51% during a 25-day treatment period[1]. |
| Molecular Weight | 444.57 |
| Formula | C27H32N4O2 |
| Cas No. | 2226534-49-0 |
| Smiles | C[C@H]1COCCN1c1ccc2nc(-c3ccc4onc(C)c4c3)n(CC3CCCCC3)c2c1 |
| Relative Density. | 1.31 g/cm3 (Predicted) |
Storage & Solubility Information
| Storage | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice. | |||||||||||||||||||||||||||||||||||
| Solubility Information | DMSO: 65 mg/mL (146.21 mM), Sonication is recommended.  | |||||||||||||||||||||||||||||||||||
Solution Preparation Table | ||||||||||||||||||||||||||||||||||||
DMSO
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In Vivo Formulation Calculator (Clear solution)
Please enter your animal experiment information in the following box and click Calculate to obtain the mother liquor preparation method and in vivo formula preparation method:
For example, your dosage is 10 mg/kg Each animal weighs 20 g, and the dosage volume is 100 μL . A total of 10 animals were administered, and the formula you used is 5% 
DMSO+30% PEG300+5% Tween 80+60% ddH2O. So your working solution concentration is 2 mg/mL。Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO (mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.
(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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