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Art. -Nr.: HY-115282

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JNJ-63576253 free base

Name: JNJ-63576253 free base
Brand: MedChemExpress
SKU: HY-115282
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(Synonyms: TRC-253 free base)

1 Cited Publications

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Based on 1 publication(s) in Google Scholar

JNJ-63576253 (TRC-253) free base 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 free base can be used for the research of castration-resistant prostate cancer (CRPC).

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

CAS. Nr.: 2110426-27-0
Formel: C₂₃H₂₁F₃N₆O₂S
Molecular Weight:502.51

Speicherung:

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

Data Sheet (277 KB)

JNJ-63576253 free base Chemical Structure

CAS. Nr.: 2110426-27-0

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- Cellular Effect
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target

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

Cellular Effect

Cell Line	Type	Value	Description	References
VCaP	IC₅₀	265 nM Compound: 5; JNJ-63576253	Antiproliferative activity against human VCaP cells expressing wild-type androgen receptor assessed as reduction in cell viability incubated for 5 days in presence of R1881 by CellTiter-glo assay Antiproliferative activity against human VCaP cells expressing wild-type androgen receptor assessed as reduction in cell viability incubated for 5 days in presence of R1881 by CellTiter-glo assay	[PMID: 33470111]
VCaP	IC₅₀	290 nM Compound: 110; JNJ-63576253	Antiproliferative activity against human VCaP cells Antiproliferative activity against human VCaP cells	[PMID: 35786895]

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 T_1/2 of >180 min^[1].

MedChemExpress (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%), C_max (0.66 μM) and AUC_last (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].

MedChemExpress (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.: T_1/2=5.99 h; CL=15.0 mL/min/kg; Vdss=6.11 L/kg.
P.o.: F=45%; C_max=0.66 μM; AUC_last=4.9 μg•h/mL.

Related Protocols :

Research Protocol for Endocrine Diseases

Chemical Information

CAS. Nr. 2110426-27-0
Molecular Weight 502.51
Formel C₂₃H₂₁F₃N₆O₂S
SMILES

O=C(N(C(N1C2=CC=C(N=C2)OC3CCNCC3)=S)C(C=C4C(F)(F)F)=CN=C4C#N)C51CCC5
Synonyms

TRC-253 free base
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

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

Publications (1)

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Journal Impact Factor

Eur J Med Chem

Elevated labile iron in castration-resistant prostate cancer is targetable with ferrous iron-activatable antiandrogen therapy. [Abstract]

2023 Mar 5:249:115110. PMID: 36708680

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (277 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[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. [Content Brief]

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Bioz

JNJ-63576253 free base

1 Cited Publications

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Publications (1)
Reinheit & Dokumentation
Verweise

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JNJ-63576253 free base

Publications Citing Use of MedChemExpress (MCE) JNJ-63576253 free base