PROTAC SOS1 degrader-3
PROTAC SOS1 degrader-3 is a PROTAC degrader targeting SOS1, which induces the targeted degradation of SOS1 via the ubiquitin-proteasome system, with DC50 values ranging from 0.19 μM to 0.75 μM in multiple distinct colorectal cancer cell lines. PROTAC SOS1 degrader-3 inhibits the phosphorylation of AKT and ERK. PROTAC SOS1 degrader-3 induces apoptosis and morphological changes in KRAS-mutant colorectal cancer organoids. PROTAC SOS1 degrader-3 can be applied in studies related to kras-mutant colorectal cancer.
(Pink: SOS1 ligand (HY-125817); Blue: Cereblon ligand (HY-W039233); Black: linker).
For research use only. We do not sell to patients.
- CAS No.: 3029320-99-5
- Formula: C34H32F3N7O6
- Molecular Weight:691.66
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Storage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
- Purity & Documentation
- References
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Biological Activity
Description
IC50 & Target
[1]|
SOS1 0.19-0.75 μM (DC50) |
Cereblon |
Cellular Effect
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Cell Line
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Type | Value | Description | References |
|---|---|---|---|---|
| SW-620 | DC50 |
0.59 μM
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Concentration-dependent SOS1 degradation in SW620 human colorectal cancer cells after 24 h incubation measured by immunoblot assay.
Concentration-dependent SOS1 degradation in SW620 human colorectal cancer cells after 24 h incubation measured by immunoblot assay.
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36459180 |
| HCT-116 | DC50 |
0.75 μM
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Concentration-dependent SOS1 degradation in HCT116 human colorectal cancer cells after 24 h incubation measured by immunoblot assay.
Concentration-dependent SOS1 degradation in HCT116 human colorectal cancer cells after 24 h incubation measured by immunoblot assay.
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36459180 |
| SW1417 | DC50 |
0.19 μM
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Concentration-dependent SOS1 degradation in SW1417 human colorectal cancer cells after 24 h incubation measured by immunoblot assay.
Concentration-dependent SOS1 degradation in SW1417 human colorectal cancer cells after 24 h incubation measured by immunoblot assay.
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36459180 |
In Vitro
PROTAC SOS1 degrader-3 (compound P7) (0.01-10 μM; 3-48 h) induces robust time-dependent SOS1 degradation that reaches 92% at 48 h following treatment with 1 μM compound in SW620 colorectal cancer cells[1].
PROTAC SOS1 degrader-3 (0.1-10 μM; 24 h) induces concentration-dependent SOS1 degradation in multiple distinct colorectal cancer cell lines, with DC50 values of 0.19 μM to 0.75 μM at the 24 h timepoint[1].
Targeted SOS1 protein degrader-3 (1 μM; 24-72 h) effectively degrades SOS1 and inhibits the viability of SOS1 inhibitor-sensitive KRAS-mutant colorectal cancer patient-derived organoid models, with IC50 values ranging from 0.48 μM to 1.4 μM[1].
PROTAC SOS1 degrader-3 (1 μM) in SW620 cells is fully mediated by the canonical cereblon E3 ligase / ubiquitin-proteasome degradation pathway[1].
PROTAC SOS1 degrader-3 (1 μM; 24 h) demonstrates exceptional specificity for SOS1 degradation with no off-target degradation of canonical cereblon neosubstrate proteins in SW620 cells[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:SW620 human colorectal cancer cells
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Concentration:1 μM (time course); 0.01 μM, 0.1 μM, 1 μM, 10 μM (6 h time point)
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Incubation Time:3 h, 6 h, 12 h, 24 h, 48 h (1 μM); 6 h (0.1-10 μM)
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Result:Achieved 64% degradation of SOS1 after 6 h of 1 μM treatment.
Reached 92% maximum SOS1 degradation at 48 h of 1 μM treatment.
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Cell Line:SW620, HCT116, C2BB, and SW1417 human colorectal cancer cell lines
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Concentration:0.1 μM, 1 μM, 10 μM
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Incubation Time:24 h
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Result:Induced concentration-dependent SOS1 degradation across all four tested CRC cell lines.
Calculated DC50 values after 24 h treatment as 0.59 μM for SW620, 0.75 μM for HCT116, and 0.19 μM for SW1417.
Reached maximum SOS1 degradation of 87% for SW620, 76% for HCT116, and 83% for SW1417 at 10 μM after 24 h.
Chemical Information
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CAS No. 3029320-99-5
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Molecular Weight 691.66
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Formula C34H32F3N7O6
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SMILES
NC1=CC(C(F)(F)F)=CC([C@H](NC2=C3C=C(OC)C(OCC(NC4=CC=CC(C5=O)=C4CN5C(C(N6)=O)CCC6=O)=O)=CC3=NC(C)=N2)C)=C1
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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)
PROTAC SOS1 degrader-3 Related Classifications
HY-152145 Related Classifications
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Keywords
- PROTAC SOS1 degrader-3
- 3029320-99-5
- PROTACs
- SOS1
- Ras
- Akt
- ERK
- Apoptosis
- AKT
- ubiquitin-proteasome system
- colorectal cancer cells
- colorectal cancer cell lines
- KRAS-mutant colorectal cancer patient-derived organoid models
- SW620 colorectal cancer cells
- cereblon E3 ligase
- KRAS-mutant colorectal cancer organoids
- Inhibitor
- inhibitor
- inhibit