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  3. JNJ-63576253 hydrochloride

JNJ-63576253 hydrochloride (Synonyms: TRC-253 hydrochloride)

Cat. No.: HY-115282A Purity: 99.22%
Handling Instructions

JNJ-63576253 (TRC-253) hydrochloride is a potent and orally active full antagonist of androgen receptor (AR), with IC50s of 37 and 54 nM for F877L mutant AR and wild-type AR in LNCaP cells. JNJ-63576253 hydrochloride can be used for the research of castration-resistant prostate cancer (CRPC).

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

JNJ-63576253 hydrochloride Chemical Structure

JNJ-63576253 hydrochloride Chemical Structure

CAS No. : 2110428-64-1

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Free Sample (0.5-1 mg)   Apply Now  
10 mM * 1 mL in DMSO USD 119 In-stock
Estimated Time of Arrival: December 31
5 mg USD 100 In-stock
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10 mg USD 170 In-stock
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25 mg USD 350 In-stock
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50 mg USD 550 In-stock
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100 mg USD 950 In-stock
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Based on 1 publication(s) in Google Scholar

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Description

JNJ-63576253 (TRC-253) hydrochloride is a potent and orally active full antagonist of androgen receptor (AR), with IC50s of 37 and 54 nM for F877L mutant AR and wild-type AR in LNCaP cells. JNJ-63576253 hydrochloride can be used for the research of castration-resistant prostate cancer (CRPC)[1].

IC50 & Target

IC50: 37 nM (F877L mutant AR in LNCaP cells); 54 nM (wild-type AR in LNCaP cells)[1]

In Vitro

JNJ-63576253 (0.0003-100 μM; 5 d) inhibits the growth of VCaP cells, with an IC50 of 265 nM[1].
JNJ-63576253 is stable in human liver microsomes, with an T1/2 of >180 min[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

In Vivo

JNJ-63576253 (30 mg/kg; p.o. once daily for 72 days) significantly inhibits the growth of prostate LNCaP SRα F877L tumor in mice[1].
JNJ-63576253 (30 mg/kg; p.o. once daily for 10 days) inhibits the five androgen sensitive organs (ASOs) under stimulation by testosterone propionate (TP) in mice[1].
JNJ-63576253 (10 mg/kg; p.o.) exhibits moderate oral bioavailability (45%), Cmax (0.66 μM) and AUClast (4.9 μg•h/mL) in mice[1].
JNJ-63576253 (2 mg/kg; i.v.) exhibits reasonable half-life (5.99 h), CL (15.0 mL/min/kg) and Vdss (6.11 L/kg) in mice[1].

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Castrated SHO mice with prostate LNCaP SRα F877L tumor[1]
Dosage: 30 mg/kg
Administration: P.o. once daily for 72 days
Result: Inhibited the tumor growth by 87%.
Animal Model: CD-1 male mice[1]
Dosage: 2 mg/kg for i.v.; 10 mg/kg for p.o. (Pharmacokinetic Analysis)
Administration: Intravenous administration and oral administration
Result: I.v.: T1/2=5.99 h; CL=15.0 mL/min/kg; Vdss=6.11 L/kg.
P.o.: F=45%; Cmax=0.66 μM; AUClast=4.9 μg•h/mL.
Molecular Weight

538.97

Formula

C₂₃H₂₂ClF₃N₆O₂S

CAS No.

2110428-64-1

SMILES

[H]Cl.O=C(N(C(N1C2=CC=C(N=C2)OC3CCNCC3)=S)C(C=C4C(F)(F)F)=CN=C4C#N)C51CCC5

Shipping

Room temperature in continental US; may vary elsewhere.

Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (463.85 mM; Need ultrasonic)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 1.8554 mL 9.2770 mL 18.5539 mL
5 mM 0.3711 mL 1.8554 mL 3.7108 mL
10 mM 0.1855 mL 0.9277 mL 1.8554 mL
*Please refer to the solubility information to select the appropriate solvent.
In Vivo:
  • 1.

    Add each solvent one by one:  10% DMSO    40% PEG300    5% Tween-80    45% saline

    Solubility: ≥ 2.08 mg/mL (3.86 mM); Clear solution

  • 2.

    Add each solvent one by one:  10% DMSO    90% (20% SBE-β-CD in saline)

    Solubility: ≥ 2.08 mg/mL (3.86 mM); Clear solution

  • 3.

    Add each solvent one by one:  10% DMSO    90% corn oil

    Solubility: ≥ 2.08 mg/mL (3.86 mM); Clear solution

*All of the co-solvents are provided by MCE.
References
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Keywords:

JNJ-63576253TRC-253JNJ63576253JNJ 63576253TRC253TRC 253Androgen ReceptorandrogenARmutantwild-typeLNCaPcastrationresistantprostatecancerCRPCInhibitorinhibitorinhibit

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JNJ-63576253 hydrochloride
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