NEO-811
NEO-811 is a selective and orally active ARNT (HIF-1β) molecular glue degrader. NEO-811 is mediated by CRL4-CRBN E3 ligase for ARNT degradation. NEO-811 can be used for the study of clear cell renal cell carcinoma (ccRCC).
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
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: 3084635-77-5
- 分子式: C30H30FN5O4
- 分子量:543.59
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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
IC50 & Target
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HIF-1β |
体外実験
NEO-811 is highly selective and does not degrade well-known neosubstrates. Transcriptomic profiling of NEO-811 activity across several VHL-deficient ccRCC cell lines confirmed suppression of HIF-2α target genes, including cyclin D and vascular endothelial growth factor (VEGF). NEO-811 also uniquely suppresses expression of target genes regulated by other Class I bHLH-PAS transcription factors, including HIF-1α and aryl hydrocarbon receptor (AHR). NEO-811 retaines activity in HIF-2α inhibitor-resistant cells that harbored previously described mutations[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
臨床実験
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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CAS 番号 3084635-77-5
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分子量 543.59
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分子式 C30H30FN5O4
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SMILES
O=C1CCC(C2=CN=C(C=CC([C@@]3(O)CCN(CC4=CC=C(C5=NOC=N5)C=C4)CC3(C)C)=C6F)C6=C2)C(N1)=O
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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.
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)