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JNJ-63576253 free base

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Catalog No. T8933Cas No. 2110426-27-0
Alias 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).

JNJ-63576253 free base

JNJ-63576253 free base

🥰Excellent
Purity: 98.32%
Catalog No. T8933Alias TRC253, JNJ-63576253Cas 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).
Pack SizePriceAvailabilityQuantity
2 mg$34In Stock
5 mg$48In Stock
10 mg$82In Stock
25 mg$170In Stock
50 mg$271In Stock
100 mg$398In Stock
200 mg$568In Stock
1 mL x 10 mM (in DMSO)$83In Stock
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Purity:98.32%
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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).
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.
AliasTRC253, JNJ-63576253
Chemical Properties
Molecular Weight502.51
FormulaC23H21F3N6O2S
Cas No.2110426-27-0
SmilesFC(F)(F)c1cc(cnc1C#N)N1C(=S)N(c2ccc(OC3CCNCC3)nc2)C2(CCC2)C1=O
Relative Density.1.53 g/cm3 (Predicted)
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 45 mg/mL (89.55 mM)
Solution Preparation Table
DMSO
1mg5mg10mg50mg
1 mM1.9900 mL9.9501 mL19.9001 mL99.5005 mL
5 mM0.3980 mL1.9900 mL3.9800 mL19.9001 mL
10 mM0.1990 mL0.9950 mL1.9900 mL9.9501 mL
20 mM0.0995 mL0.4975 mL0.9950 mL4.9750 mL
50 mM0.0398 mL0.1990 mL0.3980 mL1.9900 mL

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