CST905
CST905 is a potent BRAF-V600E PROTAC degrader with a DC50 of 18 nM. CST905 recruits the VHL E3 ligase to form a ternary complex, mediating the degradation of BRAF-V600E via the ubiquitin-proteasome pathway. The ligand of CST905 disrupts the RAF dimerization interface, thereby preventing the aberrant activation of the harmful MAPK/ERK pathway in RAS-mutated cells while degrading the target protein. CST905 can be used in studies related to malignant melanoma and neuroblastoma.
(Pink: BRAF-V600E ligand (HY-41747); Blue: VHL ligand (HY-125845); Black: linker (HY-78378)).
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- CAS No.: 3094183-98-6
- Formule: C51H58F2N10O7S2
- Masse moléculaire:1025.20
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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]|
BRafV600E 18 nM (DC50) |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| SK-MEL-28 | GI50 |
61 nM
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Exerts inhibitory effects on cell proliferation and reduces cell viability in human malignant melanoma SK-MEL-28 cells.
Exerts inhibitory effects on cell proliferation and reduces cell viability in human malignant melanoma SK-MEL-28 cells.
|
35814929 |
In Vitro
CST905 (0.1-10 μM; 4-24 h) exerts effects of degrading BRAF-V600E protein (IC50 = 18 nM) and inhibiting ERK1/2 phosphorylation (IC50 = 31 nM) in human malignant melanoma SK-MEL-28 cells[1].
CST905 (up to 10 μM; 120 h) exerts inhibitory effects on cell proliferation and reduces cell viability in human malignant melanoma SK-MEL-28 cells (GI50 = 61 nM)[1].
CST905 (0.1-10 μM; 4-24 h) does not induce abnormal activation of p-ERK1/2 or p-MEK1/2, nor does it affect the expression of wild-type BRAF protein or the level of p-ERK1/2 in human neuroblastoma SK-N-AS cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
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Cell Line:SK-MEL-28 cell line and SK-N-AS cell line
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Concentration:0.1, 1, 10 μM
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Incubation Time:4 h
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Result:Decreased the intracellular expression level of the mutant target protein and effectively down-regulated the phosphorylation activation of downstream signaling molecules.
Did not cause paradoxical hyperphosphorylation and activation of downstream key kinase signals in the mutant cells, avoiding undesirable paradoxical activation.
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Cell Line:SK-MEL-28 cell line
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Concentration:1.56 nM, 3.13 nM, 6.25 nM, 12.5 nM, 25 nM, 50 nM, 100 nM, 1 μM, 10 μM
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Incubation Time:4 h
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Result:Induced degradation of the mutant target protein in a concentration-dependent manner, achieved maximal degradation at 50 nM, and concentration-dependently suppressed the phosphorylation activation of downstream signaling molecules.
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Cell Line:SK-MEL-28 cell line
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Concentration:0.59 nM, 1.77 nM, 5.33 nM, 16.0 nM, 48.0 nM, 144.0 nM, 432.0 nM, 1296.0 nM, 3888.0 nM, 10 μM
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Incubation Time:120 h
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Result:Inhibited the in vitro proliferation and viability of tumor cells in a concentration-dependent manner.
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Cell Line:SK-N-AS cell line
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Concentration:0.1, 1, 10 μM (4 h treatment) and 10 μM (24 h treatment)
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Incubation Time:4 h, 24 h
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Result:Did not alter the normal expression abundance of the wild-type target protein and did not disturb basal downstream phosphorylation levels.
Chemical Information
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CAS No. 3094183-98-6
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Masse moléculaire 1025.20
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Formule C51H58F2N10O7S2
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SMILES
O=C([C@H]1N(C([C@@H](NC(CN2CCN(C3=CC=C(C4=CN=C(NC=C5C(C6=C(F)C=CC(NS(=O)(N(CC)C)=O)=C6F)=O)C5=C4)C=C3)CC2)=O)C(C)(C)C)=O)C[C@H](O)C1)NCC7=CC=C(C8=C(C)N=CS8)C=C7
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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)
CST905 Related Classifications
HY-175435 Related Classifications
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