5.32996

Androgen Receptor DBD Inhibitor, VPC-14449

• 別名: Androgen Receptor DBD Inhibitor, VPC-14449, AR-DBD Inhibitor, VPC-14449, VPC14449, VPC 14449
• 実験式（ヒル表記法）: C₁₀H₁₀Br₂N₄OS
• CAS番号: 1621375-32-3
• 分子量: 394.09
• MDL番号: MFCD32206764
• UNSPSCコード: 12352200
• PubChem Substance ID: 135150480
• NACRES: NA.77

特性

• アッセイ: ≥98% (HPLC)
• 品質水準: 100
• フォーム: solid
• 有効性: 947 nM IC₅₀
• メーカー／製品名: Calbiochem^®
• 保管条件: OK to freeze; protect from light
• 色: off-white
• 溶解性: DMSO: 50 mg/mL
• 保管温度: 2-8°C
• SMILES記法: C1COCCN1C2=NC(=CS2)N3C=C(N=C3Br)Br
• InChI: 1S/C10H10Br2N4OS/c11-7-5-16(9(12)13-7)8-6-18-10(14-8)15-1-3-17-4-2-15/h5-6H,1-4H2
• InChI Key: AZLNRGRZOLVWRX-UHFFFAOYSA-N

詳細

詳細

A cell-permeable morpholinyl thiazole compound that selectively binds to the DNA-binding domain of androgen receptor (AR) and blocks its activity (IC₅₀ = 340 nM in PC3 cells). Its inhibitory effect is comparable to enzalutamide (IC₅₀ = 314 nM). Does not affect Y594D and Q592D mutant forms of AR. However, Y594A and Q592A mutant AR activity can be inhibited at much higher concentrations (3 - 6 mM). Shown to down-regulate the expression of AR-responsive genes in LNCaP Cells, however, it does not affect genotoxin-responsive genes expression. Suppresses the growth of androgen-sensitive LNCaP xenografts in mice (~100 mg/kg, i.p., b.i.d.).

Please note that the molecular weight for this compound is batch-specific due to variable water content. Please refer to the vial label or the certificate of analysis for the batch-specific molecular weight. The molecular weight provided represents the baseline molecular weight without water.

VPC-14449, is a cell-permeable compound that selectively binds to the DNA-binding domain of androgen receptor (AR) and blocks its activity (IC₅₀ = 340 nM in PC3 cells).

生物化学的／生理学的作用

Cell permeable: yes

Primary Target
Androgen Receptor

警告

Toxicity: Standard Handling (A)

再構成

Following reconstitution, aliquot and freeze (-20°C). Stock solutions are stable for up to 3 months at -20°C.

その他情報

Dalal, K., et al. 2014. J. Biol. Chem.289, 26417.

法的情報

CALBIOCHEM is a registered trademark of Merck KGaA, Darmstadt, Germany

安全性情報

• 保管分類コード: 11 - Combustible Solids
• WGK: WGK 3
• 引火点(°F): Not applicable
• 引火点(℃): Not applicable