BMS-871
BMS-871 is an orally active pan-Notch inhibitor with IC50 values of 4/1/4/3 nM for Notch1/2/3/4, respectively. BMS-871 significantly inhibited the proliferation of TALL-1 and MDA-MB-157 cells and demonstrated significant antitumor activity in T-acute lymphoblastic leukemia and triple-negative breast cancer xenograft models. BMS-871 can be used to study leukemia and breast cancer.
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- CAS. Nr.: 1584631-89-9
- Formel: C29H27F3N4O3
- Molecular Weight:536.54
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
Biologische Aktivität
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Cell Line
|
Type | Value | Description | References |
|---|---|---|---|---|
| HeLa | IC50 |
1 nM
Compound: 30, BMS-871
|
Inhibition of Notch2 intracellular domain fragment transfected in human HeLa cells co-transfected with CBF1-PGL3 luciferase reporter vector by transactivation assay
Inhibition of Notch2 intracellular domain fragment transfected in human HeLa cells co-transfected with CBF1-PGL3 luciferase reporter vector by transactivation assay
|
[PMID: 25857941] |
| HeLa | IC50 |
3 nM
Compound: 30, BMS-871
|
Inhibition of Notch4 intracellular domain fragment transfected in human HeLa cells co-transfected with CBF1-PGL3 luciferase reporter vector by transactivation assay
Inhibition of Notch4 intracellular domain fragment transfected in human HeLa cells co-transfected with CBF1-PGL3 luciferase reporter vector by transactivation assay
|
[PMID: 25857941] |
| HeLa | IC50 |
4 nM
Compound: 30, BMS-871
|
Inhibition of Notch1 intracellular domain fragment transfected in human HeLa cells co-transfected with CBF1-PGL3 luciferase reporter vector by transactivation assay
Inhibition of Notch1 intracellular domain fragment transfected in human HeLa cells co-transfected with CBF1-PGL3 luciferase reporter vector by transactivation assay
|
[PMID: 25857941] |
| HeLa | IC50 |
4 nM
Compound: 30, BMS-871
|
Inhibition of Notch3 intracellular domain fragment transfected in human HeLa cells co-transfected with CBF1-PGL3 luciferase reporter vector by transactivation assay
Inhibition of Notch3 intracellular domain fragment transfected in human HeLa cells co-transfected with CBF1-PGL3 luciferase reporter vector by transactivation assay
|
[PMID: 25857941] |
| TALL-1 | IC50 |
4 nM
Compound: 30, BMS-871
|
Anticancer activity against human TALL-1 cells assessed as cell number by coulter channelyzer
Anticancer activity against human TALL-1 cells assessed as cell number by coulter channelyzer
|
[PMID: 25857941] |
Chemical Information
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CAS. Nr. 1584631-89-9
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Molecular Weight 536.54
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Formel C29H27F3N4O3
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SMILES
O=C(N[C@@H]1C(N(C)C2=CC=CC=C2C(C3=CC=CC=C3)=N1)=O)[C@H](CCC(F)(F)F)[C@H](C4=CC=CC=C4)C(N)=O
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)