BMS-986497
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).
For research use only. We do not sell to patients.
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Help & FAQs
Biological Activity
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.
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.
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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SMILES
[BMS-986497]
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Synonyms
ORM-6151
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Shipping
Room temperature in continental US; may vary elsewhere.
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Storage
Please store the product under the recommended conditions in the Certificate of Analysis.
Purity & Documentation
References
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BMS-986497 Related Classifications
Cat. No.: HY-171792
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- BMS-986497
- ORM-6151
- BMS986497
- BMS 986497
- ORM6151
- ORM 6151
- 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