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NSC 658497
CAS No. 909197-38-2
NSC 658497( NSC658497 )
Catalog No. M16534 CAS No. 909197-38-2
NSC 658497 is a small molecule inhibitor of Ras GEF, SOS1, binds to SOS1 with Kd of 7 uM but no H-Ras.
Purity : >98% (HPLC)
COA
Datasheet
HNMR
HPLC
MSDS
Handing Instructions
| Size | Price / USD | Stock | Quantity |
| 5MG | 873 | Get Quote |
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| 50MG | 1782 | Get Quote |
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| 100MG | 2250 | Get Quote |
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| 200MG | Get Quote | Get Quote |
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| 500MG | Get Quote | Get Quote |
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| 1G | Get Quote | Get Quote |
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Biological Information
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Product NameNSC 658497
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NoteResearch use only, not for human use.
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Brief DescriptionNSC 658497 is a small molecule inhibitor of Ras GEF, SOS1, binds to SOS1 with Kd of 7 uM but no H-Ras.
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DescriptionNSC 658497 is a small molecule inhibitor of Ras GEF, SOS1, binds to SOS1 with Kd of 7 uM but no H-Ras, competitively suppresses SOS1-Ras interaction, and dose-dependently inhibits SOS1 GEF activity; showes dose-dependent efficacy in inhibiting Ras, downstream signaling activities, and associated cell proliferation.
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In VitroNSC-658497 (0-20 μM; 2 hours; NIH/3T3 cells) dose-dependently inhibits EGF (50 ng/mL)-stimulated Ras, but not EGFR activation.Concomitant to Ras inhibition, NSC-658497 (0-100 μM; 2 hours; NIH/3T3 cells) dose-dependently inhibited the EGF activated, Ras downstream targets ERK1/2 and AKT.Consistent with these results, NSC-658497 dose-dependently suppressed Ras signaling mediated by the overexpression of an active SOS1 mutant (W729L), originally identified in Noonan’s Syndrome, in human embryonic kidney cells.NSC-658497 dose-dependently inhibits 50 nM SOS1-cat mediated GDP/GTP nucleotide exchange upon 2 μM H-Ras (aa. 1-166) in the BODIPYFL-GDP dissociation assay (IC50=15.4μM).NSC-658497 (0-60 μM; 3 days; PC-3 and DU-145 cells) inhibits proliferation of prostate cancer cells.NSC-658497 (0-60 μM; 2 hours; PC-3 and DU-145 cells) dose-dependently inhibits Ras-GTP activity and the downstream p-ERK1/2 and p-Akt activities. Cell Proliferation AssayCell Line:PC-3 and DU-145 cells Concentration:0-60 μMIncubation Time:3 days Result:Dose-dependently inhibited proliferation of PC-3 and DU-145 cells.Western Blot Analysis Cell Line:PC-3 and DU-145 cells Concentration:0-60 μM Incubation Time:2 hours Result:Dose-dependently inhibited Ras-GTP activity and the downstream p-ERK1/2 and p-Akt activities.
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In Vivo——
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SynonymsNSC658497
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PathwayMAPK/ERK Signaling
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TargetRas
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RecptorRas
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Research Area——
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Indication——
Chemical Information
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CAS Number909197-38-2
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Formula Weight438.428
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Molecular FormulaC20H10N2O6S2
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Purity>98% (HPLC)
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Solubility——
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SMILESO=C1/C(C(C2=C(O1)C=CC=C2)=O)=C\N(C/3=O)C(SC3=C/C4=CC=C([N+]([O-])=O)C=C4)=S
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Chemical Name(Z)-3-(((Z)-5-(4-nitrobenzylidene)-4-oxo-2-thioxothiazolidin-3-yl)methylene)chroman-2,4-dione
Shipping & Storage Information
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Storage(-20℃)
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ShippingWith Ice Pack
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Stability≥ 2 years
Reference
1. Evelyn CR, et al. Chem Biol. 2014 Dec 18;21(12):1618-28.
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