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Y06137

Y06137
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.
Catalog No. T13363Cas No. 2226534-49-0
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Purity:97.27%
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Y06137

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.
With extensive experience in compound synthesis, we can provide rapid custom synthesis services for this product according to your research needs.
Pack SizePriceAvailabilityQuantity
1 mg$55In Stock
2 mg$79In Stock
5 mg$129In Stock
10 mg$213In Stock
25 mg$396In Stock
1 mL x 10 mM (in DMSO)$143In Stock
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Product Introduction

Bioactivity
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].
Chemical Properties
Molecular Weight444.57
FormulaC27H32N4O2
Cas No.2226534-49-0
Storage & Solubility Information
StoragePowder: -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
1mg5mg10mg50mg
1 mM2.2494 mL11.2468 mL22.4936 mL112.4682 mL
5 mM0.4499 mL2.2494 mL4.4987 mL22.4936 mL
10 mM0.2249 mL1.1247 mL2.2494 mL11.2468 mL
20 mM0.1125 mL0.5623 mL1.1247 mL5.6234 mL
50 mM0.0450 mL0.2249 mL0.4499 mL2.2494 mL
100 mM0.0225 mL0.1125 mL0.2249 mL1.1247 mL

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