BMS-986449
BMS-986449 is a potent and orally active CELMoD molecular glue and an IKZF2/IKZF4 degrader. BMS-986449 targets the degradation of transcription factors Helios (IKZF2) and Eos (IKZF4) in regulatory T (Treg) cells. BMS-986449 redirects the E3 ubiquitin ligase Cereblon to induce the degradation of Helios and Eos, reprogramming Treg cells and enhancing antitumor immunity. BMS-986449 is promising for research of advanced solid tumors.
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。
- 分子式: C21H21FN4O3
- 分子量:396.41
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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生物活性
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化学情報
- 純度とドキュメンテーション
- 参考文献
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Help & FAQs
生物活性
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IKZF2 |
IKZF4 |
Upon activation culture, human primary Treg cells treated with BMS‑986449 has a reprogrammed transcriptional phenotype by day 8: increased protein expression of effector molecules (e.g., Granzyme B) and abundant expression of inflammatory gene transcripts[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
BMS‑986449 has antitumor activity in the CT26, MB49, and MC38 tumor models in human CRBN knock‑in tumor‑bearing mice, with maximum tumor growth inhibition (TGI) values of up to 75%, 62%, and 42%, respectively. When combined with anti‑PD‑1 immune checkpoint inhibitor, the efficacy was significantly enhanced, with TGI values of 95%, 97%, and 92%, respectively[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
化学情報
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分子量 396.41
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分子式 C21H21FN4O3
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SMILES
NC1=NC(C2=C(F)C([C@@H](C)N([C@H]3CCC(NC3=O)=O)C4=O)=C4C=C2)=CC(C)=C1C
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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)
BMS-986449 関連分類
HY-173630 関連分類
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