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SAH-SOS1A TFA

Cat. No. M10600
SAH-SOS1A TFA Structure
Size Price Availability Quantity
5mg USD 410  USD410 In stock
10mg USD 680  USD680 In stock
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Quality Control & Documentation
Biological Activity

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) and directly and independently blocks nucleotide association. SAH-SOS1A TFA (0.625-40 μM; 24 hours) 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.

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.

Sequence: Arg-Arg-Phe-Phe-Gly-Ile-Aaa-Leu-Thr-Asn-Aaa-Leu-Lys-Thr-Glu-Glu-Gly-Asn (Covalent bridge: Aaa7-Aaa11)

Chemical Information
Molecular Weight 2301.55
Formula C102H160N27F3O30
CAS Number 1652561-87-9 (free base)
Storage -20°C, protect from light, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
Animal A (mg/kg) = Animal B (mg/kg) multiplied by  Animal B Km
Animal A Km

For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.

References

[1] Elizaveta S Leshchiner, et al. Proc Natl Acad Sci U S A. Direct inhibition of oncogenic KRAS by hydrocarbon-stapled SOS1 helices

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Keywords: SAH-SOS1A TFA supplier, Ras, inhibitors, activators


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