PROTAC SOS1 degrader-4
PROTAC SOS1 degrader-4 (Compound 10) is a PROTAC degrader that targets the SOS1 protein for degradation by recruiting cereblon. It degrades SOS1 in NCI-H358, A-427, SW-620, and DLD-1 cells and inhibits the proliferation of various KRAS-mutant tumor cells, making it a useful tool for cancer research.
(Pink: SOS1 ligand (HY-175575); Blue: Cereblon ligand (HY-W115490); Black: linker).
For research use only. We do not sell to patients.
- Formula: C53H65ClN8O7S
- Molecular Weight:993.65
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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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Help & FAQs
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Biological Activity
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SOSA |
PROTAC SOS1 degrader-4 (Compound 10) (0.03-3000 nM; 24 h) degrades SOS1 in KRAS-mutant NCI-H358, A-427, SW-620 and DLD-1 cells, with a DC50 ≤50 nM in all cell lines. Its Dmax reaches 50-<80% in NCI-H358 cells, and 80-100% in A-427, SW-620 and DLD-1 cells[1].
PROTAC SOS1 degrader-4 (0.008-20000 nM; 7 days) potently inhibits the proliferation of NCI-H441 (KRASG12V) human cancer cells, with an IC50 falling into the "A" potency class; after 7 days of incubation, this compound also inhibits the proliferation of AsPC-1 (KRASG12D) human cancer cells, with an IC50 belonging to the "C" potency class[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:NCI-H358 (KRAS G12C); A-427 (KRAS G12D); SW-620 (KRAS G12V); DLD-1 (KRAS G13D)
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Concentration:0.03-3000 nM
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Incubation Time:24 h
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Result:Degraded SOS1 with DC50≤50 nM in all four cell lines.
Dmax was 50-<80% in NCI-H358 and 80-100% in A-427, SW-620 and DLD-1
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Cell Line:NCI-H358 (KRAS G12C); NCI-H441 (KRAS G12V); DLD-1 (KRAS G13D); AsPC-1 (KRAS G12D)
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Concentration:0.008-20000 nM
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Incubation Time:7 days
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Result:Inhibited proliferation with IC50≤15 nM in NCI-H358 and NCI-H441, >15-≤30 nM in DLD-1, and >30-≤50 nM in AsPC-1.
Chemical Information
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Molecular Weight 993.65
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Formula C53H65ClN8O7S
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SMILES
O=C(N1CCN(CC2CCC3(CCN(C(C4=CC=C(Cl)C(N5CCC(NC5=O)=O)=C4)=O)CC3)CC2)CC1)[C@H]6CC[C@H](C7=CC8=C(N[C@H](C)C9=CC=CC%10=C9CCS%10(=O)=O)N=C(C)N=C8C=C7OC)CC6
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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-4 Related Classifications
HY-153674 Related Classifications
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- PROTAC SOS1 degrader-4
- PROTACs
- SOS1
- DLD-1 (KRAS G13D) human cancer cells
- AsPC-1 (KRAS G12D) human cancer cells
- SW620 (KRAS G12V) human cancer cells
- NCI-H441 (KRAS G12V) human cancer cells
- Ras-SOS1 interactions
- SOS1 protein
- cancer
- Rac-SOS1 interactions
- NCI-H358 (KRAS G12C) human cancer cells
- A427 (KRAS G12D) human cancer cells
- Inhibitor
- inhibitor
- inhibit