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JNJ-63576253 free base

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Purity:98.32%

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COA HNMR HPLC

JNJ-63576253 free base

Catalog No. T8933Cas No. 2110426-27-0

JNJ-63576253 free base (TRC253) 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 can be used for the research of castration-resistant prostate cancer (CRPC).

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Pack Size	Price	Availability
1 mg	$41	In Stock
2 mg	$56	In Stock
5 mg	$81	In Stock
10 mg	$137	In Stock
25 mg	$283	In Stock
50 mg	$452	In Stock
100 mg	$665	In Stock
1 mL x 10 mM (in DMSO)	$138	In Stock

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Product Introduction

Bioactivity

Description	JNJ-63576253 free base (TRC253) 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 can be used for the research of castration-resistant prostate cancer (CRPC).
In vitro	JNJ-63576253 is stable in human liver microsomes, with an T1/2 of >180 min. It(0.0003-100 μM; 5 d) inhibits the growth of VCaP cells, with an IC50 of 265 nM.
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.?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.?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.?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.
Alias	TRC253, JNJ-63576253

Chemical Properties

Molecular Weight	502.51
Formula	C23H21F3N6O2S
Cas No.	2110426-27-0

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year

Solubility Information

DMSO: 45 mg/mL (89.55 mM)

Solution Preparation Table

DMSO

	1mg	5mg	10mg	50mg
1 mM	1.9900 mL	9.9501 mL	19.9001 mL	99.5005 mL
5 mM	0.3980 mL	1.9900 mL	3.9800 mL	19.9001 mL
10 mM	0.1990 mL	0.9950 mL	1.9900 mL	9.9501 mL
20 mM	0.0995 mL	0.4975 mL	0.9950 mL	4.9750 mL
50 mM	0.0398 mL	0.1990 mL	0.3980 mL	1.9900 mL

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