WCA-814
WCA-814 is an androgen receptor (AR) antagonist-Hsp90 inhibitor conjugate. WCA-814 induces the degradation of full-length and AR-V7. WCA-814 has cytotoxic effect in prostatic cancer cells (IC50: 171.2 nM, 26.5 nM for LNCaP, 22Rv1 cell).
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研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 2951858-45-8
- 分子式: C46H53ClN10O5
- 分子量:861.43
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
生物活性
製品説明
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| CWR22R | IC50 |
26.5 nM
Compound: 6; WCA-814
|
Cytotoxicity against human 22Rv1 cells assessed as inhibition of cell growth incubated for 5 days in presence of AR agonist, R1881 by WST-1 assay
Cytotoxicity against human 22Rv1 cells assessed as inhibition of cell growth incubated for 5 days in presence of AR agonist, R1881 by WST-1 assay
|
[PMID: 36960664] |
| LNCaP | IC50 |
171.2 nM
Compound: 6; WCA-814
|
Cytotoxicity against AR-positive human LNCaP cells assessed as inhibition of cell growth incubated for 5 days in presence of AR agonist, R1881 in charcoal stripped serum by WST-1 assay
Cytotoxicity against AR-positive human LNCaP cells assessed as inhibition of cell growth incubated for 5 days in presence of AR agonist, R1881 in charcoal stripped serum by WST-1 assay
|
[PMID: 36960664] |
化学情報
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CAS 番号 2951858-45-8
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分子量 861.43
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分子式 C46H53ClN10O5
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SMILES
CC(C1=C(C=C(C(C2=NNC(N2C3=CC=C(C=C3)CN4CCN(CC4)CC5CCN(CC5)C6=CC=C(N=N6)C(N[C@H]7CC[C@@H](CC7)OC8=CC(Cl)=C(C=C8)C#N)=O)=O)=C1)O)O)C
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
プロトコル
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Research Protocol for Endocrine Diseases
Endocrine diseases often arise from disrupted hormone production, hormone signaling, or target-tissue responsiveness; for diabetes-focused endocrine disease models, insulin signaling regulates glucose uptake, hepatic glucose output, lipid metabolism, and β-cell compensation. Type 2 diabetes develops through interacting defects in insulin resistance, β-cell dysfunction, adipose inflammation, hepatic glucose overproduction, altered incretin signaling, and ectopic lipid metabolism. A major unresolved question is whether endocrine dysfunction is driven primarily by target-tissue insulin resistance, intrinsic β-cell failure, immune/inflammatory stress, or combined multi-organ failure that differs by disease stage.
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Cell Viability Determination by MTT Colorimetric Assay
The following protocol uses the MTT colorimetric assay as a classic literature-established method for assessing cell viability/metabolic activity in cultured mammalian cells. MTT[3-(4,5-dimethylthiazol-2-yl)-2,5-diphenyltetrazolium bromide] is reduced by metabolically active cells to a colored formazan product; the amount of formazan is quantified spectrophotometrically and provides an indirect measure of metabolically active viable cells. Importantly, MTT reduction reflects cellular oxidoreductase/metabolic activity rather than an absolute direct count of living cells, so changes in cellular metabolism can alter the signal independently of cell number.
純度とドキュメンテーション
参考文献
Calculators
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)