2. PROTAC Immunology/Inflammation
  3. Molecular Glues IKZF Family
  4. 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.

For research use only. We do not sell to patients.

BMS-986449

BMS-986449 Chemical Structure

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5 mg Get quote 11 - 12 weeks 10 - 11 weeks 12 - 13 weeks 10 - 11 weeks
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50 mg Get quote 11 - 12 weeks 10 - 11 weeks 12 - 13 weeks 10 - 11 weeks
100 mg Get quote 11 - 12 weeks 10 - 11 weeks 12 - 13 weeks 10 - 11 weeks
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Other Forms of BMS-986449:

BMS-986449 Related Antibodies

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IKZF1 IKZF2 IKZF3 IKZF4

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Description

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[1][2][3].

IC50 & Target[1]

IKZF2

 

IKZF4

 

In Vitro

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 Related Antibodies
In Vivo

BMS‑986449 (0.3 mg/kg; oral; once daily) is well tolerated in cynomolgus monkeys and maintained greater than 80% degradation of Helios in circulating Treg cells within 24 hours[2].
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.
Clinical Trial
Molecular Weight

396.41

Formula

C21H21FN4O3
SMILES

NC1=NC(C2=C(F)C([C@@H](C)N([C@H]3CCC(NC3=O)=O)C4=O)=C4C=C2)=CC(C)=C1C
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
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BMS-986449 Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

BMS-986449BMS986449BMS 986449Molecular GluesIKZF FamilyIkaros zinc finger protein familymolecular glueHeliosEosregulatory T (Treg) cellsadvanced solid tumorsInhibitorinhibitorinhibit

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