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JNJ-63576253 free base

Catalog No. T8933 CAS 2110426-27-0

Synonyms: TRC253, JNJ-63576253

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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JNJ-63576253 free base Chemical Structure

JNJ-63576253 free base, CAS 2110426-27-0

Pack Size	Availability	Price/USD
1 mg	In stock	$ 41.00
2 mg	In stock	$ 56.00
5 mg	In stock	$ 81.00
10 mg	In stock	$ 137.00
25 mg	In stock	$ 283.00
50 mg	In stock	$ 452.00
100 mg	In stock	$ 665.00
1 mL * 10 mM (in DMSO)	In stock	$ 138.00

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Purity: 98.32%

Biological Description

Chemical Properties

Storage & Solubility Information

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).
Targets&IC50	Androgen receptor:37 nM(F877L mutant AR in LNCaP cells), Androgen receptor:54 nM(wild-type AR in LNCaP cells)
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.

Synonyms	TRC253, JNJ-63576253
Molecular Weight	502.51
Formula	C23H21F3N6O2S
CAS No.	2110426-27-0

Storage

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

Solubility Information

DMSO: 45 mg/mL (89.55 mM)

References and Literature

1. Zhang Z, et, al. Discovery of JNJ-63576253: A Clinical Stage Androgen Receptor Antagonist for F877L Mutant and Wild-Type Castration-Resistant Prostate Cancer (mCRPC). J Med Chem. 2021 Jan 28;64(2):909-924.

Related compound libraries

This product is contained In the following compound libraries：

Anti-Cancer Clinical Compound Library Anti-Cancer Active Compound Library Anti-Cancer Drug Library Drug Repurposing Compound Library Inhibitor Library Anti-Prostate Cancer Compound Library Anti-Cancer Compound Library Endocrinology-Hormone Compound Library Clinical Compound Library Bioactive Compounds Library Max

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Keywords

JNJ-63576253 free base 2110426-27-0 Endocrinology/Hormones Androgen Receptor JNJ63576253 JNJ 63576253 free base resistant CRPC JNJ63576253 free base wild-type TRC253 prostate JNJ 63576253 cancer TRC-253 JNJ-63576253 TRC 253 castration androgen LNCaP Inhibitor inhibit mutant inhibitor

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