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Art. -Nr.: HY-173630

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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.

Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.

Formel: C₂₁H₂₁FN₄O₃
Molecular Weight:396.41

Speicherung:

Please store the product under the recommended conditions in the Certificate of Analysis.

Data Sheet (270 KB)

BMS-986449 Chemical Structure

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Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Reinheit & Dokumentation
Verweise
Calculators
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

IKZF2

IKZF4

Alle IKZF Family Isoform-spezifische Produkte anzeigen :

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.

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

NCT Number	Sponsor	Condition	Start Date	Phase A549
NCT01329991	Plexxikon\|		2011-05	PHASE1

Chemical Information

Molecular Weight 396.41
Formel 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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

Please store the product under the recommended conditions in the Certificate of Analysis.

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (270 KB)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Barnes M J. Selective degradation of Helios induces Treg cell reprogramming and enhanced antitumor immunity[J]. Cancer Research, 2025, 85(8_Supplement_1): 2249-2249.

[2]. Barnes M J. Selective degradation of Helios induces Treg cell reprogramming and enhanced antitumor immunity. Cancer Research, 2025, 85(8_Supplement_1): 2249-2249.

[3]. Balog A. Abstract ND05: The discovery of BMS-986449, a highly potent and selective degrader of the transcription factors Helios (IKZF2) and Eos (IKZF4) for the treatment of solid tumors. Cancer Research, 2025, 85(8_Supplement_2): ND05-ND05.

Calculators

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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MOQ

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100 mg

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Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- In Vivo
- Clinical Trial
Chemical Information
Reinheit & Dokumentation
Verweise

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BMS-986449

High-Throughput Bioactive Compound Library

Alle IKZF Family Isoform-spezifische Produkte anzeigen

Biologische Aktivität

Chemical Information

Reinheit & Dokumentation

Verweise

Calculators

Help & FAQs

BMS-986449 Related Classifications

HY-173630 Related Classifications