BCR-ABL degrader 1
BCR-ABL degrader 1 is a hydrophobic tag degrader with GNF‑2 (HY-11007) as the ligand and Boc2His (HY-185595) as the hydrophobic tag. BCR-ABL degrader 1 mediates the degradation of BCR‑ABL with a DC50 of 19.9 μM. BCR-ABL degrader 1 induces the degradation of BCR-ABL fusion protein via the ubiquitin-proteasome pathway, a process involving Hsp70 and Hsp90. BCR-ABL degrader 1 downregulates p‑STAT5 and p‑SHP2, the downstream signaling molecules of BCR‑ABL. BCR-ABL degrader 1 can be used in the research of chronic myeloid leukemia.
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- Formule: C33H36F3N7O6
- Masse moléculaire:683.68
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Activité biologique
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Chemical Information
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Activité biologique
Description
IC50 & Target
[1]|
Bcr-Abl |
STAT5 |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| K562 | DC50 |
19.9 μM
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BCR-ABL degradation in human K562 (BCR-ABL-positive chronic myeloid leukemia) cells measured via Western blot after 20 h treatment.
BCR-ABL degradation in human K562 (BCR-ABL-positive chronic myeloid leukemia) cells measured via Western blot after 20 h treatment.
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41406910 |
| K562 | IC50 |
8.68 μM
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Antiproliferative activity against human K562 (BCR-ABL-positive chronic myeloid leukemia) cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay.
Antiproliferative activity against human K562 (BCR-ABL-positive chronic myeloid leukemia) cells assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay.
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41406910 |
| BaF3 | IC50 |
11.5 μM
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Antiproliferative activity against BaF3 cells expressing BCR-ABL E225K mutant assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay.
Antiproliferative activity against BaF3 cells expressing BCR-ABL E225K mutant assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay.
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41406910 |
| BaF3 | IC50 |
1.74 μM
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Antiproliferative activity against BaF3 cells expressing BCR-ABL T315I mutant assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay.
Antiproliferative activity against BaF3 cells expressing BCR-ABL T315I mutant assessed as reduction in cell viability incubated for 48 hrs by CCK-8 assay.
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41406910 |
In Vitro
BCR-ABL degrader 1 (10-30 μM; 20 h) dose-dependently inhibits the downstream signaling pathways of BCR-ABL (p-BCR-ABL, p-STAT5, p-SHP2) in K562 cells[1].
BCR-ABL degrader 1 (48 h) potently inhibits the proliferation of K562 cells with an IC50 of 8.68 μM, and exhibits extremely low toxicity toward non-cancerous HEK 293T cells[1].
BCR-ABL degrader 1 (10-50 μM; 20 h) degrades drug-resistant BCR-ABLE225K and BCR-ABLT315I mutants in BaF3 cells, potently inhibits their proliferation, with IC50 values of 11.5 μM (E225K) and 1.74 μM (T315I) against the two mutants, respectively[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:K562 (BCR-ABL-positive chronic myeloid leukemia) cells
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Concentration:10 μM, 20 μM, 30 μM, 40 μM
30 μM (wash out) -
Incubation Time:6 h, 12 h, 16 h, 20 h, 24 h
12 h, 24 h, 36 h post-washout -
Result:Induced 85% degradation of BCR-ABL at 40 μM and 75% degradation at 20 μM after 20 h incubation.
Induced 75-80% degradation at 40 μM, 30 μM, and 20 μM after 20 h, with no degradation observed at 10 μM.
Showed no degradation before 12 h of 30 μM incubation, significant degradation after 16 h, and complete degradation after 24 h.
Showed no recovery of BCR-ABL protein levels within 36 h after 20 h incubation with 30 μM followed by washout.
Had a DC50 of 19.9 μM for BCR-ABL degradation.
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Cell Line:K562 cells
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Concentration:10 μM, 20 μM, 30 μM
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Incubation Time:20 h
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Result:Led to dose-dependent reductions in p-BCR-ABL, p-STAT5, and p-SHP2 levels, corresponding to reduced BCR-ABL protein levels.
Parmacokinetics
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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Masse moléculaire 683.68
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Formule C33H36F3N7O6
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SMILES
O=C(N1C(C[C@H](NC(OC(C)(C)C)=O)C(NC2=CC=CC(C3=NC=NC(NC4=CC=C(OC(F)(F)F)C=C4)=C3)=C2)=O)=CN=C1)OC(C)(C)C
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
BCR-ABL degrader 1 Related Classifications
HY-180798 Related Classifications
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