SIAIS100
SIAIS100 is a potent BCR-ABL PROTAC degrader with an DC50 value of 2.7 nM. SIAIS100 can be used to research chronic myeloid leukemia (CML).
(Pink: Target protein ligand; Blue: Cereblon ligand (HY-W586108); Black: linker (HY-Y0860)).
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- No. CAS: 3033463-06-5
- Fòrmula: C44H50ClF2N9O5S
- Peso molecular:890.44
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Almacenamiento:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Actividad biológica
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Actividad biológica
DC50: 2.7 nM [1]
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| K562 | IC50 |
12 nM
Compound: 30; IAIS100
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Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 2 days by CCK8 assay
Antiproliferative activity against human K562 cells assessed as inhibition of cell growth incubated for 2 days by CCK8 assay
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[PMID: 36306539] |
SIAIS100 exhibits anti-proliferative activity against K562 cells with an IC50 value of 12 nM[1].
SIAIS100 degrades BCR-ABL with degradation ratio of 81.78% and 91.20% at 5 nM and 100 nM, respectively[1].
SIAIS100 (100 nM; 8 h) significantly decreases BCR-ABL in K562 cells[1].
SIAIS100 (100 nM; 6 h) induced sustained and robust BCR-ABL degradation and maintained a durable cellular response after drug removal[1].
SIAIS100 (1-1000 nM) significantly degrade mutation G250E/T315I dose-dependently accompanied by the inhibition of BCR-ABL signaling assessed by the level of p-BCR-ABL in 32D cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:K562
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Concentration:100 nM
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Incubation Time:8 h
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Result:Significantly decreases BCR-ABL.
Chemical Information
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No. CAS 3033463-06-5
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Peso molecular 890.44
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Fòrmula C44H50ClF2N9O5S
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SMILES
O=C1CCC(C(N1)=O)N2CC3=C(C2=O)C=CC=C3SCCCCCCN4CCN(CC4)C5CCN(CC5)C6=NC=C(C=C6C7=CC=NN7)C(NC8=CC=C(C=C8)OC(F)(Cl)F)=O
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureza y Documentación
Referencias
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
SIAIS100 Related Classifications
HY-152036 Related Classifications
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