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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 Size | Price | Availability | Quantity |
---|---|---|---|
2 mg | $34 | In Stock | |
5 mg | $48 | In Stock | |
10 mg | $82 | In Stock | |
25 mg | $170 | In Stock | |
50 mg | $271 | In Stock | |
100 mg | $398 | In Stock | |
200 mg | $568 | In Stock | |
1 mL x 10 mM (in DMSO) | $83 | In Stock |
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. |
Alias | TRC253, JNJ-63576253 |
Molecular Weight | 502.51 |
Formula | C23H21F3N6O2S |
Cas No. | 2110426-27-0 |
Smiles | FC(F)(F)c1cc(cnc1C#N)N1C(=S)N(c2ccc(OC3CCNCC3)nc2)C2(CCC2)C1=O |
Relative Density. | 1.53 g/cm3 (Predicted) |
Storage | Powder: -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
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