5.32996

Androgen Receptor DBD Inhibitor, VPC-14449

• 동의어(들): Androgen Receptor DBD Inhibitor, VPC-14449, AR-DBD Inhibitor, VPC-14449, VPC14449, VPC 14449
• 실험식(Hill 표기법): C₁₀H₁₀Br₂N₄OS
• CAS Number: 1621375-32-3
• Molecular Weight: 394.09
• MDL number: MFCD32206764
• UNSPSC 코드: 12352200
• PubChem Substance ID: 135150480
• NACRES: NA.77

속성

• 분석: ≥98% (HPLC)
• Quality Level: 100
• 양식: solid
• 효능: 947 nM IC₅₀
• 제조업체/상표: Calbiochem^®
• 저장 조건: OK to freeze; protect from light
• 색상: off-white
• solubility: DMSO: 50 mg/mL
• 저장 온도: 2-8°C
• SMILES string: 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

설명

일반 설명

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.

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).

생화학적/생리학적 작용

Cell permeable: yes

Primary Target
Androgen Receptor

경고

Toxicity: Standard Handling (A)

재구성

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

기타 정보

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

법적 정보

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

안전성 정보

• Storage Class Code: 11 - Combustible Solids
• WGK: WGK 3
• Flash Point (°F): Not applicable
• Flash Point (°C): Not applicable