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BI-3406

BI-3406 (compound I-13) is a potent, selective and orally active inhibitor of the interaction between KRAS and Son of Sevenless 1 (SOS1) with IC50 of 5 nM. BI-3406 reduces the formation of GTP-loaded KRAS, and inhibits MAPK pathway signaling. BI-3406 exhibits anti-tumor activities.

BI-3406 Chemical Structure

BI-3406 Chemical Structure

CAS: 2230836-55-0

Selleck's BI-3406 has been cited by 4 publications

Purity & Quality Control

Batch: Purity: 99.87%
99.87

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Signaling Pathway

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Ras Signaling Pathway

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Biological Activity

Description BI-3406 (compound I-13) is a potent, selective and orally active inhibitor of the interaction between KRAS and Son of Sevenless 1 (SOS1) with IC50 of 5 nM. BI-3406 reduces the formation of GTP-loaded KRAS, and inhibits MAPK pathway signaling. BI-3406 exhibits anti-tumor activities.
Targets
K-ras [1]
(Cell-free assay)
5 nM
In vitro
In vitro

BI-3406, a selective SOS1 inhibitor, enhanced the AMG 510-induced growth suppression in MIA PaCa-2 cells. Treatment with 5 µM BI-3406 following the excision of endogenous mutant KRAS abolishes both ERK and AKT activation, consistent with the inhibition of WT RAS signaling.[1]
Cell Research Cell lines MIA PaCa-2, mT42 cells
Concentrations 5 μM, 20 μM to 2 nM
Incubation Time 4 days
Method

MIA PaCa-2 cells were seeded at 2,000 cells per well and treated 24 h after seeding with 5 μM BI-3406 or DMSO control and AMG 510 (from 5 μM to 0.1 nM). Cell viability was measured after 4 d with CellTiter-Glo. mT42 cells were seeded at 1,000 cells per well and treated with 4-OHT or DMSO control and BI-3406 in a dose–response manner (from 20 μM to 2 nM). Cell viability was measured using CellTiter-Glo Luminescence assay at day 4. FPC cell line mT42 cells were treated with 5 μM BI-3406, 20 nM trametinib, or DMSO vehicle control in the presence or absence of mutant KRAS by treatment with DMSO vehicle control or 4-OHT, respectively. Immunoblotting was performed for RAS pathways by phospho-ERK and phospho-AKT and the RSK1 substrate phospho-S6.
In Vivo
In vivo

BI-3406, a potent and selective SOS1-KRAS Interaction Inhibitor, is effective in KRAS-driven cancers through combined MEK inhibition.[2]
Animal Research Animal Models NSG female mice of KRAS G12V and KRAS Q61K mutant pancreatic PDX model
Dosages 50 mg/kg
Administration p.o.

Chemical Information & Solubility

Molecular Weight 462.46 Formula

C23H25F3N4O3
CAS No. 2230836-55-0 SDF --
Smiles CC1=NC2=CC(=C(C=C2C(=N1)NC(C)C3=CC(=CC(=C3)N)C(F)(F)F)OC4CCOC4)OC
Storage (From the date of receipt) 3 years -20°C powder

In vitro
Batch:

DMSO : 92 mg/mL ( (198.93 mM)； Moisture-absorbing DMSO reduces solubility. Please use fresh DMSO.)

Ethanol : 92 mg/mL

Water : Insoluble


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In vivo
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Tech Support

Answers to questions you may have can be found in the inhibitor handling instructions. Topics include how to prepare stock solutions, how to store inhibitors, and issues that need special attention for cell-based assays and animal experiments.

Handling Instructions

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