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.
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- 화학식: C21H21FN4O3
- 분자량:396.41
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보관:
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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Biological Activity
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Chemical Information
- 순도&문서
- References
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Help & FAQs
Biological Activity
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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 |
Chemical Information
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분자량 396.41
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화학식 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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선적
Room temperature in continental US; may vary elsewhere.
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보관
Please store the product under the recommended conditions in the Certificate of Analysis.
순도&문서
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BMS-986449 Related Classifications
HY-173630 Related Classifications
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