5.32996

Androgen Receptor DBD Inhibitor, VPC-14449

• 同義詞: Androgen Receptor DBD Inhibitor, VPC-14449, AR-DBD Inhibitor, VPC-14449, VPC14449, VPC 14449
• 經驗公式（希爾表示法）: C₁₀H₁₀Br₂N₄OS
• CAS號碼: 1621375-32-3
• 分子量：: 394.09
• MDL號碼: MFCD32206764
• 分類程式碼代碼: 12352200
• PubChem物質ID: 135150480
• NACRES: NA.77

屬性

• 化驗: ≥98% (HPLC)
• 品質等級: 100
• 形狀: solid
• 效力: 947 nM IC₅₀
• 製造商／商標名: Calbiochem^®
• 儲存條件: OK to freeze; protect from light
• 顏色: off-white
• 溶解度: DMSO: 50 mg/mL
• 儲存溫度: 2-8°C
• SMILES 字串: 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 密鑰: AZLNRGRZOLVWRX-UHFFFAOYSA-N

描述

一般說明

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).

生化／生理作用

Cell permeable: yes

Primary Target
Androgen Receptor

警告

Toxicity: Standard Handling (A)

重構

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

其他說明

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

法律資訊

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

安全資訊

• 儲存類別代碼: 11 - Combustible Solids
• 水污染物質分類（WGK）: WGK 3
• 閃點（°F）: Not applicable
• 閃點（°C）: Not applicable