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Y06137 

Cat. No.: HY-111503
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Y06137 is a potent and selective BET inhibitor, which binds to the BRD4(1) bromodomain with a Kd of 81 nM. Antitumor activity.

For research use only. We do not sell to patients.

Y06137 Chemical Structure

Y06137 Chemical Structure

CAS No. : 2226534-49-0

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  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

Y06137 is a potent and selective BET inhibitor, which binds to the BRD4(1) bromodomain with a Kd of 81 nM[1]. Antitumor activity[1].

IC50 & Target[1]

BRD4(1)

81 nM (Kd)

In Vitro

Y06137 (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 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[1].

Cell Viability Assay[1]

Cell Line: LNCaP, C4-2B, 22Rv1, and VCaP prostate cancer cells
Concentration: 0.001-100 μM
Incubation Time: 96 hours for LNCaP, C4-2B, and 22Rv1; 144 hours for VCaP
Result: Inhibited LNCaP, C4-2B, 22Rv1, and VCaP cells with IC50s of 0.47, 0.84, 0.70, 0.29 μM, respectively.

Western Blot Analysis[1]

Cell Line: 22Rv1 cells
Concentration: 1, 2, 4, 8, and 16 μM
Incubation Time: 48 hours
Result: Resulted in significant down-regulation of both AR-fl and AR variants levels.
In Vivo

Y06137 (50 mg/kg, i.p. injection, 5 times per week, 25 days) demonstrates therapeutic effects in a C4-2B CRPC xenograft tumor model in mice. Y06137 is well tolerated in the treated mice, based on the weight of the animal body and their general behavior[1].

Animal Model: Four-week-old male mice (strain: C.B-17/IcrHsd-Prkdcscid for C4-2B) with C4-2B mouse xenograft model[1]
Dosage: 50 mg/kg, 100 μL
Administration: Intraperitoneal (i.p.) injection, 5 times per week, 25 days
Result: Exhibited strong antitumor activities during the 25-day treatment period, with a tumor growth inhibition (TGI) of 51%.
Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.2494 mL 11.2468 mL 22.4936 mL
5 mM 0.4499 mL 2.2494 mL 4.4987 mL
10 mM 0.2249 mL 1.1247 mL 2.2494 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

444.57

Formula

C₂₇H₃₂N₄O₂

CAS No.

2226534-49-0

SMILES

CC1=NOC(C1=C2)=CC=C2C3=NC(C=C4)=C(N3CC5CCCCC5)C=C4N6CCOC[[email protected]@H]6C

Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Y06137
Cat. No.:
HY-111503
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Y06137

Cat. No.: HY-111503