BMS-986497
Based on 1 Customer Validation
BMS-986497 (ORM-6151) is a CD33-targeting antibody-conjugated GSPT1 degrader. BMS-986497 delivers the GSPT1 degrader SMol006 to CD33-expressing cells and induces GSPT1 protein degradation. BMS-986497 shows potential for research on acute myeloid leukemia (AML).
Nur für Forschungszwecke. Wir verkaufen nicht an Patienten.
- Reinheit : 99.59%
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Speicherung:
-80°C
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Biologische Aktivität
Beschreibung
In Vitro
ORM-6151 (BMS-986497) (picomolar concentrations) shows picomolar cytotoxic activity in CD33-expressing AML cell lines, including Mylotarg-resistant AML193 and Kasumi6 cell lines, with 10-1000-fold greater potency than reference GSPT1 degrader molecules[1].
ORM-6151 (BMS-986497) (picomolar concentrations) shows picomolar cytotoxic potency in primary relapsed/refractory AML patient blasts, with better potency than CC-90009 and Mylotarg[1].
ORM-6151 (BMS-986497) exhibits minimal cytotoxic activity in healthy hematopoietic progenitor cells, with 10-10,000-fold less toxicity than CC-90009 or Mylotarg[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:xenograft model[1]
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Dosage:1 mg/kg
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Administration:single treatment
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Result:Demonstrated robust anti-tumor efficacy, with superior activity compared to CC-90009.
Showed tumor growth inhibition correlated with the degree and duration of GSPT1 depletion and changes in expression of integrated stress response biomarker genes.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date |
Phase
|
|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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Appearance Liquid
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Color Colorless to light yellow
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SMILES
[BMS-986497]
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Synonyms
ORM-6151
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Versand
Shipping with dry ice.
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Speicherung
-80°C
Reinheit & Dokumentation
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Data Sheet (278 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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Handling Instructions (2659 KB)
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Keywords
- BMS-986497
- ORM-6151
- BMS986497
- BMS 986497
- ORM6151
- ORM 6151
- Antibody-Drug Conjugates (ADCs)
- Eukaryotic Release Factor (eRF)
- Transmembrane Glycoprotein
- CD33
- acute myeloid leukemia xenograft models
- myelodysplastic neoplasms
- AML193
- Kasumi6
- acute myeloid leukemia cells
- healthy hematopoietic progenitor cells
- MV4-11
- GSPT1
- primary relapsed/refractory acute myeloid leukemia blasts
- Inhibitor
- inhibitor
- inhibit