SAH-SOS1A
SAH-SOS1A is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM), directly and independently blocks nucleotide association, impairs KRAS-driven cancer cell viability, and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS.
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- CAS No.: 1652561-87-9
- Formule: C100H159N27O28
- Masse moléculaire:2187.50
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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
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KRAS-SOS1 |
KRas G12C 140 nM (EC50) |
KRas G12D 109 nM (EC50) |
KRas G12V 154 nM (EC50) |
KRas G12S 155 nM (EC50) |
KRas Q61H 175 nM (EC50) |
K-Ras WT 106 nM (EC50) |
SAH-SOS1A (0.625-40 μM) dose-responsively impairs the viability of cancer cells bearing G12D, G12C, G12V, G12S, G13D, and Q61H mutations with IC50 values in the 5- to 15-μM range. Cancer cells expressing wild-type KRAS, such as HeLa and Colo320-HSR cells, are similarly affected[1].
SAH-SOS1A (5-40 μM; 4 hours) dose-responsively inhibits MEK1/2, ERK1/2, and AKT phosphorylation[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Cell Line:Panc 10.05 cells bearing the KRAS G12D mutation
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Concentration:0.625-40 μM
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Incubation Time:24 hours
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Result:Dose-responsively impaired the viability of cancer cells bearing KRAS G12D.
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Cell Line:Panc 10.05 cells
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Concentration:5-40 μM
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Incubation Time:Indicated doses for 4 h, followed by 15-min stimulation with EGF
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Result:Dose-responsively inhibited MEK1/2, ERK1/2, and AKT phosphorylation.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 1652561-87-9
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Masse moléculaire 2187.50
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Formule C100H159N27O28
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Sequence
Arg-Arg-Phe-Phe-Gly-Ile-{Aaa}-Leu-Thr-Asn-{Aaa}-Leu-Lys-Thr-Glu-Glu-Gly-Asn (Covalent bridge:Aaa7-Aaa11)
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Sequence Shortening
RRFFGI{Aaa}LTN{Aaa}LKTEEGN (Covalent bridge:Aaa7-Aaa11)
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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)
SAH-SOS1A Related Classifications
HY-P2265 Related Classifications
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