Powder: -20°C for 3 years | In solvent: -80°C for 1 year
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 | Availability | Price/USD | Quantity |
---|---|---|---|
1 mg | In stock | $ 67.00 | |
5 mg | In stock | $ 163.00 | |
10 mg | In stock | $ 288.00 | |
25 mg | In stock | $ 491.00 | |
50 mg | In stock | $ 716.00 | |
1 mL * 10 mM (in DMSO) | In stock | $ 178.00 |
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) demonstrates therapeutic effects in a C4-2B CRPC xenograft tumor model in mice. Y06137 exhibited strong antitumor activities during the 25-day treatment period, with a tumor growth inhibition (TGI) of 51%[1]. |
Molecular Weight | 444.57 |
Formula | C27H32N4O2 |
CAS No. | 2226534-49-0 |
Powder: -20°C for 3 years | In solvent: -80°C for 1 year
DMSO: 60 mg/mL (134.96 mM), sonification is recommended.
You can also refer to dose conversion for different animals. More
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Y06137 2226534-49-0 Chromatin/Epigenetic Cytoskeletal Signaling PKC Epigenetic Reader Domain Y 06137 Y-06137 Inhibitor inhibit inhibitor