SAH-SOS1A( —— )

Catalog No. M30796 CAS No. 1652561-87-9

KRas/son of sevenless 1 (SOS1) interaction inhibitor. Binds within nucleotide binding pocket of KRas (Kd values are 106 - 176 nM for wild type KRas and various KRas mutants). Inhibits nucleotide binding to KRas in a concentration dependent manner. Displays cytotoxicity in KRas-driven cancer cell lines and inhibits downstream ERK-MAPK signaling. Cell permeable.

Purity : >98% (HPLC)

COA

Datasheet

HNMR

HPLC

MSDS

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Biological Information

Product Name

SAH-SOS1A
Note

Research use only, not for human use.
Brief Description

KRas/son of sevenless 1 (SOS1) interaction inhibitor. Binds within nucleotide binding pocket of KRas (Kd values are 106 - 176 nM for wild type KRas and various KRas mutants). Inhibits nucleotide binding to KRas in a concentration dependent manner. Displays cytotoxicity in KRas-driven cancer cell lines and inhibits downstream ERK-MAPK signaling. Cell permeable.
Description

KRas/son of sevenless 1 (SOS1) interaction inhibitor. Binds within nucleotide binding pocket of KRas (Kd values are 106 - 176 nM for wild type KRas and various KRas mutants). Inhibits nucleotide binding to KRas in a concentration dependent manner. Displays cytotoxicity in KRas-driven cancer cell lines and inhibits downstream ERK-MAPK signaling. Cell permeable.
In Vitro

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.SAH-SOS1A (5-40 μM; 4 hours) dose-responsively inhibits MEK1/2, ERK1/2, and AKT phosphorylation. Cell Viability Assay Cell Line:Panc 10.05 cells bearing the KRAS G12D mutation Concentration:0.625-40 μM Incubation Time:24 hours Result:Dose-responsively impaired the viability of cancer cells bearing KRAS G12D.Western Blot Analysis Cell Line:Panc 10.05 cells Concentration:5-40 μM Incubation Time:Indicated doses for 4 h, followed by 15-min stimulation with EGF Result:Dose-responsively inhibited MEK1/2, ERK1/2, and AKT phosphorylation.
In Vivo

SAH-SOS1A (0.2 μL of 10 mM solution; injection; 48 hours; abdomens of D. melanogaster Ras85DV12/ActinGS) treatment notably decreases the phosphorylation state of ERK1/2.
Synonyms

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Pathway

MAPK/ERK Signaling
Target

Ras
Recptor

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Research Area

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Indication

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Chemical Information

CAS Number

1652561-87-9
Formula Weight

2187.53
Molecular Formula

C100H159N27O28
Purity

>98% (HPLC)
Solubility

water:1 mg/mL
SMILES

[H][C@](NC(=O)CNC(=O)[C@H](CC1=CC=CC=C1)NC(=O)[C@H](CC1=CC=CC=C1)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCCNC(N)=N)NC(C)=O)([C@@H](C)CC)C(=O)N[C@@]1(C)CCCC=CCCC[C@](C)(NC(=O)[C@H](CC(N)=O)NC(=O)[C@@]([H])(NC(=O)[C@H](CC(C)C)NC1=O)[C@@H](C)O)C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCCCN)C(=O)N[C@@H]([C@@H](C)O)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CCC(O)=O)C(=O)NCC(=O)N[C@@H](CC(N)=O)C(O)=O
Chemical Name

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