Proxalutamide

SKU: orb2815832

Description

Proxalutamide is a potent and selective androgen receptor (AR) antagonist. It is used in research to investigate AR signaling in vitro and has been studied in vivo for conditions like prostate cancer.

Research Area

Infectious Disease & Virology, Metabolism Research

Images & Validation

−

Key Properties

−

CAS Number	1398046-21-3
MW	517.5
Purity	99.31% (May vary between batches)
Formula	C₂₄H₁₉F₄N₅O₂S
SMILES	CC1(C)N(C(=S)N(C1=O)c1ccc(C#N)c(c1F)C(F)(F)F)c1ccc(CCCc2ncco2)nc1
Target	Androgen Receptor,SARS-CoV
Solubility	DMSO:100 mg/mL (193.24 mM)

Bioactivity

−

In Vivo

The mean Proxalutamide (GT0918) half-life estimate from the pHM-SD tablets (7.9±2.2 h) was similar to that of the conventional tablets (8.4±0.5 h), remaining consistent with the following pharmacokinetic theory: the extent and rate of absorption should not affect elimination. The relative bioavailability (frel) of the pHM-SD tablets is 125.6% of that for the conventional tablets on average, revealing that the bioavailability of the former is higher. The tmax for the pHM-SD and conventional tablets are 0.9±0.4 h and 2.5±1.1 h, respectively, meaning that the pHM-SD tablets dissolve more quickly than the conventional tablets. The mean Cmax and the AUC0-36 are 5.1±2.4 μg/mL and 38.3±8.2 μgh/mL for the pHM-SD tablets versus 3.1±1.5 μg/mL and 42.1±22.3 μgh/mL for conventional tablets, respectively .

In Vitro

Proxalutamide inhibits the proliferation of hormone-sensitive CaP cells and more potently inhibits the proliferation of CRPC cells. Proxalutamide inhibits the growth of AR-positive breast cancer cells. Proxalutamide more effectively inhibits androgen binding with AR's ligand-binding domain than Bicalutamide (11.4x) and MDV3100 (3.5x). Proxalutamide displays stronger potency to block AR function of gene transcription than Bicalutamide (~5-10) and MDV3100 (2-5x) while maintaining full antagonism in CRPC cells, in both hormone-sensitive (LNCaP) and CRPC (C4-2) cancer cells. Proxalutamide has minimum effects on the growth of AR-negative CaP cells (PC-3 and DU145), showing it is a selective AR pathway inhibitor. Proxalutamide impairs androgen stimulates AR translocation to cell nuclei hence blocks its binding DNA and shuts down the downstream oncogenic signaling and Proxalutamide also causes AR downregulation in prostate cancer cells .

Storage & Handling

−

Storage	Powder: -20°C for 3 years \| In solvent: -80°C for 1 year \| Shipping with blue ice/Shipping at ambient temperature.
Expiration Date	12 months from date of receipt.
Disclaimer	For research use only

Alternative Names

−

prostate, SARS coronavirus, SARS-CoV, SARSCoV, resistant, Pruxelutamide, Proxalutamide, Inhibitor, GT0918, GT-0918, GT 0918, inhibit, MOA, castration, cancer, Androgen Receptor, Androgen Receptor[1]., AndrogenReceptor, CRPC

Quality Guarantee

Explore bioreagents carefree to elevate your research. All our products are rigorously tested for performance. If a product does not perform as described on its datasheet, our scientific support team will provide expert troubleshooting, a prompt replacement, or a refund. For full details, please see our Terms & Conditions and Buying Guide. Contact us at [email protected].

Compound Identifiers

PubChem CID

60194102 ↗

Key Properties

−

No computed properties available.

Documents Download

Datasheet

Product Information

Download

Request a Document

Protocol Information

Find More Protocols

Proxalutamide (orb2815832)

Based on 0 reviews

Participating in our Biorbyt product reviews program enables you to support fellow scientists by sharing your firsthand experience with our products.

No reviews yet

Purity:	>98%
CAS Number:	1398046-21-3
MW:	517.5
Formula:	C₂₄H₁₉F₄N₅O₂S

Proxalutamide

Description

Research Area

Images & Validation

Key Properties

Bioactivity

Storage & Handling

Alternative Names

Similar Products

Proxalutamide [orb783564]

Quality Guarantee

Compound Identifiers

Key Properties

Documents Download

Request a Document

Protocol Information

Proxalutamide (orb2815832)

Step 1: Enter information below

Step 2: Enter the in vivo formulation

Available Sizes

Email

UK Office

US Office

CN Office

Distributors