SIAIS562055
SIAIS562055 is a potent cereblon-based SOS1 PROTAC with a Kd of 95.9 nM. SIAIS562055 exhibits sustained degradation of SOS1 and inhibition of downstream ERK pathways. SIAIS562055 effectively blocked the binding of KRASG12C or KRASG12D to SOS1, with the IC50 values of 95.7 nM and 134.5 nM, respectively. SIAIS562055 exhibits potent anticancer activity.
(Pink: SOS1 ligand (HY-168638); Blue: Cereblon ligand (HY-W586108); Black: linker (HY-W009145)).
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- CAS No.: 3062106-15-1
- Formule: C49H62F3N7O5S
- Masse moléculaire:918.12
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Activité biologique
Description
IC50 & Target
[1]|
Cereblon |
SOS1 95.9 nM (Kd) |
In Vitro
SIAIS562055 (10-1000 nM; 24 h) exhibits sustained degradation of SOS1 and inhibition of downstream ERK pathways, resulting in superior anti-proliferative activity compared to small molecule inhibitors[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 and GP2d cells
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Concentration:10 nM, 100 nM, 1000 nM
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Incubation Time:24 h
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Result:Exhibited sustained degradation of SOS1 and inhibition of downstream ERK pathways.
In Vivo
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female BALB/c mice (6-7-week-old) injected with MIA PaCa-2 cells[1]
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Dosage:20 mg/kg; 40 mg/kg; 50 mg/kg
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Administration:ip; daily; for 3 weeks
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Result:Displayed promising antitumor potency.
Chemical Information
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CAS No. 3062106-15-1
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Masse moléculaire 918.12
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Formule C49H62F3N7O5S
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SMILES
COC1=CC2=C(C(N[C@@H](C3=CC(N)=CC(C(F)(F)F)=C3)C)=NC(C)=N2)C=C1OC4CCN(CC4)CCCCCCCCCCCCSC5=C6C(C(N(C6)C7C(NC(CC7)=O)=O)=O)=CC=C5
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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)
SIAIS562055 Related Classifications
HY-168637 Related Classifications
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