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Cat. No.: HY-184586

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SOS1-IN-28

SOS1-IN-28 is an orally active, blood-brain barrier permeable SOS1 inhibitor with an IC₅₀ value of 0.11 μM. SOS1-IN-28 disrupts the SOS1: KRAS protein-protein interaction, with an IC₅₀ of 0.29 μM for the KRAS-RAF interaction. SOS1-IN-28 blocks GTP loading of KRAS, inhibits RAS-MAPK pathway activity, and reduces cancer cell proliferation. SOS1-IN-28 can be used for the research of KRAS^G12C-mutant lung cancer.

For research use only. We do not sell to patients.

Formula: C₁₆H₁₄F₄N₄O₂
Molecular Weight:370.30

Storage:

Please store the product under the recommended conditions in the Certificate of Analysis.

SOS1-IN-28 Chemical Structure

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Top Publications Citing

Use of MCE Products

Fluorescent Dye

Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Purity & Documentation
References
Calculators
Help & FAQs
Classifications
Bioz

Biological Activity

Description

IC₅₀ & Target^[1]

SOS1

0.11 μM (IC₅₀)

All Ras Isoforms :

All p38 MAPK Isoforms :

In Vitro

SOS1-IN-28 (Compound 27) (0.03 nM-30 μM; 6 days) inhibits the proliferation of NCI-H358 SOS2^-/- cell spheroids in a 3D assay with a GI₅₀ of 0.33 μM^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Parmacokinetics

Species	Dose	Route	CL	V_ss	T_1/2	Bioavailability
Rat^[1]	0.5 mg/kg	i.v.	12 mL/min/kg	1.4 L/kg	1.6 h	/
Rat^[1]	1 mg/kg	p.o.	/	/	/	100 %

In Vivo

SOS1-IN-28 (Compound 27) (100 mg/kg; p.o.; single dose) deepens and sustains suppression of RAS-MAPK pathway markers (DUSP6 mRNA and pERK) when combined with a KRAS^G12C inhibitor in LU99 KRAS^G12C xenograft tumors^[1].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model:

Nude male mice (Envigo)^[1]
Dosage:

100 mg/kg
Administration:

p.o.; single dose
Result:

Produced deeper, more sustained suppression of DUSP6 mRNA and phosphorylated ERK (pERK) at 4 h, 8 h, and 16 h compared to KRASG12C inhibitor alone.
Reduced DUSP6 mRNA expression.
Reduced pERK protein levels statistically significantly relative to vehicle control at all three time points.
Maintained unbound plasma concentrations above its biochemical and cellular proliferation IC₅₀ for up to 16 h.

Chemical Information

Molecular Weight 370.30
Formula C₁₆H₁₄F₄N₄O₂
SMILES

FC1=C(C(F)(F)F)C=CC=C1[C@@H](C)NC(C2=CC=NC(C(NC)=O)=N2)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage

Please store the product under the recommended conditions in the Certificate of Analysis.

Purity & Documentation

Handling Instructions (2659 KB)

References

[1]. Bagal SK, et al. Discovery of CNS Penetrant SOS1 Inhibitors for the Treatment of KRAS-Dependent Cancers. Journal of medicinal chemistry. 2026 Jun 16. [Content Brief]

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Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

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100 mg

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Biological Activity
- Description
- IC₅₀ & Target
- In Vitro
- In Vivo
Chemical Information
Purity & Documentation
References

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SOS1-IN-28

All Ras Isoforms

All p38 MAPK Isoforms

Biological Activity

Chemical Information

Purity & Documentation

References

Calculators

Help & FAQs

SOS1-IN-28 Related Classifications

HY-184586 Related Classifications