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SAH-SOS1A (TFA)

SAH-SOS1A TFA is a peptide-based SOS1/KRAS protein interaction inhibitor. SAH-SOS1A TFA binds to wild-type and mutant KRAS (G12D, G12V, G12C, G12S, and Q61H) with nanomolar affinity (EC50=106-175 nM) . SAH-SOS1A TFA directly and independently blocks nucleotide association. SAH-SOS1A TFA impairs KRAS-driven cancer cell viability and exerts its effects by on-mechanism blockade of the ERK-MAPK phosphosignaling cascade downstream of KRAS[1].

Product Specifications

CAS Number

[2896737-31-6]

UNSPSC

12352209

Target

Ras; SOS1

Type

Peptides

Related Pathways

GPCR/G Protein; MAPK/ERK Pathway

Applications

Cancer-Kinase/protease

Field of Research

Cancer

Assay Protocol

https://www.medchemexpress.com/sah-sos1a-tfa.html

Purity

96.79

Solubility

H2O : 33.33 mg/mL (ultrasonic)

Smiles

C[C@]1(C(N[C@H](C(N[C@@](C(N[C@H](C(N[C@@](C)(CCC/C=C/CCC1)C(N[C@@H](CC(C)C)C(N[C@@H](CCCCN)C(N[C@@H]([C@H](O)C)C(N[C@@H](CCC(O)=O)C(N[C@@H](CCC(O)=O)C(NCC(N[C@H](C(O)=O)CC(N)=O)=O)=O)=O)=O)=O)=O)=O)=O)CC(N)=O)=O)([H])[C@H](O)C)=O)CC(C)C)=O)NC([C@H]([C@@H](C)CC)NC(CNC([C@H](CC2=CC=CC=C2)NC([C@@H](NC([C@H](CCCNC(N)=N)NC([C@@H](NC(C)=O)CCCNC(N)=N)=O)=O)CC3=CC=CC=C3)=O)=O)=O)=O.OC(C(F)(F)F)=O

Molecular Formula

C102H160N27F3O30

Molecular Weight

2301.55

References & Citations

[1]Leshchiner ES, et al. Direct inhibition of oncogenic KRAS by hydrocarbon-stapled SOS1 helices. Proc Natl Acad Sci U S A. 2015;112 (6) :1761-1766.

Shipping Conditions

Blue Ice

Storage Conditions

-80°C, 2 years; -20°C, 1 year (Powder, sealed storage, away from moisture and light, under nitrogen)

Scientific Category

Peptides

Clinical Information

No Development Reported

Isoform

K-Ras

Available Sizes

Curated Selection

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