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JNJ-63576253 free base

Name: JNJ-63576253 free base
Brand: TargetMol
SKU: T8933
Rating: 4.5 (1 reviews)

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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

😃Good

Catalog No. T8933Alias TRC253, JNJ-63576253Cas No. 2110426-27-0

Pack Size	Price	Availability
2 mg	$34	Backorder
5 mg	$48	Backorder
10 mg	$82	Backorder
25 mg	$170	Backorder
50 mg	$271	Backorder
100 mg	$398	Backorder
200 mg	$568	Backorder
1 mL x 10 mM (in DMSO)	$83	Backorder

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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.
Synonyms	TRC253, JNJ-63576253

Chemical Properties

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)
Color	Yellow
Appearance	solid

Storage & Solubility Information

Storage

Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.

Solubility Information

DMSO: 45 mg/mL (89.55 mM), Sonication is recommended.

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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DMSO+30% PEG300+5% Tween 80+60% Saline/PBS/ddH₂O. So your working solution concentration is 2 mg/mL。

Mother liquor preparation method: 2 mg of drug dissolved in 50 μL DMSO TargetMol | reagent

(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.

Preparation method for in vivo formula: Take 50 μL DMSO TargetMol | reagent

main solution, add 300 μLPEG300 TargetMol | reagent

mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLSaline/PBS/ddH₂O TargetMol | reagent

mix well and clarify

For Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.

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