Reagents and instruments for immunology, cell biology and molecular biology.

BI-3406 [2230836-55-0]

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Cat# HY-125817-1ml

Size : 10mM/1mL

Brand : MedChemExpress

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Description

BI-3406 (compound I-6) is an orally active, highly potent and selective inhibitor of the interaction between KRAS and Son of Sevenless 1 (SOS1) with an IC₅₀ of 6 nM. BI-3406 potently reduces the formation of GTP-loaded KRAS, and inhibits MAPK pathway signaling. BI-3406 has anticancer activity^[1]^[2].

IC₅₀ & Target^[1]

KRAS-SOS1

6 nM (IC₅₀)

Cellular Effect

Cell Line	Type	Value	Description	References
A549	IC₅₀	263 nM Compound: BI-3406	Antiproliferative activity against human A549 cells harboring KRAS G12S mutant assessed as inhibition of cell proliferation incubated for 7 days by CellTiterGlo-3D proliferation assay Antiproliferative activity against human A549 cells harboring KRAS G12S mutant assessed as inhibition of cell proliferation incubated for 7 days by CellTiterGlo-3D proliferation assay	[PMID: 36897932]
ASPC1	IC₅₀	64.4 nM Compound: BI-3406	Antiproliferative activity against human ASPC1 cells harboring KRAS G12D mutant assessed as inhibition of cell proliferation incubated for 7 days by CellTiterGlo-3D proliferation assay Antiproliferative activity against human ASPC1 cells harboring KRAS G12D mutant assessed as inhibition of cell proliferation incubated for 7 days by CellTiterGlo-3D proliferation assay	[PMID: 36897932]
LoVo	IC₅₀	142 nM Compound: BI-3406	Antiproliferative activity against human LoVo cells harboring KRAS G13D mutant assessed as inhibition of cell proliferation incubated for 7 days by CellTiterGlo-3D proliferation assay Antiproliferative activity against human LoVo cells harboring KRAS G13D mutant assessed as inhibition of cell proliferation incubated for 7 days by CellTiterGlo-3D proliferation assay	[PMID: 36897932]
MIA PaCa-2	IC₅₀	24.8 nM Compound: BI-3406	Antiproliferative activity against human MIA PaCa-2 cells harboring KRAS G12C mutant assessed as inhibition of cell proliferation incubated for 7 days by CellTiterGlo-3D proliferation assay Antiproliferative activity against human MIA PaCa-2 cells harboring KRAS G12C mutant assessed as inhibition of cell proliferation incubated for 7 days by CellTiterGlo-3D proliferation assay	[PMID: 36897932]
MIA PaCa-2	IC₅₀	30 nM Compound: 4; BI-3406	Antiproliferative activity against human MIA PaCa-2 cells harboring G12C mutant assessed as cell growth inhibition incubated for 7 days by Celltiter-Glo 3D cell viability assay Antiproliferative activity against human MIA PaCa-2 cells harboring G12C mutant assessed as cell growth inhibition incubated for 7 days by Celltiter-Glo 3D cell viability assay	[PMID: 36793426]
NCI-H358	IC₅₀	16.5 nM Compound: BI-3406	Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant assessed as inhibition of cell proliferation incubated for 7 days by CellTiterGlo-3D proliferation assay Antiproliferative activity against human NCI-H358 cells harboring KRAS G12C mutant assessed as inhibition of cell proliferation incubated for 7 days by CellTiterGlo-3D proliferation assay	[PMID: 36897932]
PANC-1	IC₅₀	17.8 nM Compound: BI-3406	Antiproliferative activity against human PANC-1 cells harboring KRAS G12D mutant assessed as inhibition of cell proliferation incubated for 7 days by CellTiterGlo-3D proliferation assay Antiproliferative activity against human PANC-1 cells harboring KRAS G12D mutant assessed as inhibition of cell proliferation incubated for 7 days by CellTiterGlo-3D proliferation assay	[PMID: 36897932]
SW-620	IC₅₀	30.1 nM Compound: BI-3406	Antiproliferative activity against human SW620 cells harboring KRAS G12V mutant assessed as inhibition of cell proliferation incubated for 7 days by CellTiterGlo-3D proliferation assay Antiproliferative activity against human SW620 cells harboring KRAS G12V mutant assessed as inhibition of cell proliferation incubated for 7 days by CellTiterGlo-3D proliferation assay	[PMID: 36897932]

In Vitro

BI-3406 is an inhibitor of the interaction between KRAS and its Guanine Nucleotide Exchange Factor (GEF) SOS1. BI-3406 does not block the interaction of KRAS with SOS2 but elicits activity on a broad panel of KRAS oncogenic variants, including all major G12 and G13 oncoproteins. Down-modulation of this signaling cascade by BI-3406 in KRAS G12 or G13 mutant cells effectively limits cell proliferation^[2].

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

Solvent & Solubility

In Vitro:

DMSO : 100 mg/mL (216.23 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Ethanol : 100 mg/mL (216.23 mM; Need ultrasonic)

Preparing
Stock Solutions

Concentration Solvent Mass	1 mg	5 mg	10 mg

1 mM	2.1623 mL	10.8117 mL	21.6235 mL
5 mM	0.4325 mL	2.1623 mL	4.3247 mL
10 mM	0.2162 mL	1.0812 mL	2.1623 mL

View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month (stored under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Select the appropriate dissolution method based on your experimental animal and administration route.

For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for in vivo experiments, it is recommended to prepare freshly and use it on the same day.
The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.

Protocol 1

Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 2

Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: 2.5 mg/mL (5.41 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 2.5 mg/mL.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 3

Add each solvent one by one: 10% DMSO 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.
Protocol 4

Add each solvent one by one: 10% EtOH 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (5.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
Protocol 5

Add each solvent one by one: 10% EtOH 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.5 mg/mL (5.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
Protocol 6

Add each solvent one by one: 10% EtOH 90% Corn Oil
Solubility: ≥ 2.5 mg/mL (5.41 mM); Clear solution

This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown). If the continuous dosing period exceeds half a month, please choose this protocol carefully.
Taking 1 mL working solution as an example, add 100 μL EtOH stock solution (25.0 mg/mL) to 900 μL Corn oil, and mix evenly.

Purity & Documentation

Purity: 99.95%

Data Sheet (278 KB) SDS (393 KB)

COA (253 KB) HNMR (273 KB) LCMS (94 KB)

Handling Instructions (2659 KB)

References

[1]. Michael Gmachl, et al. Novel benzylamino substituted quinazolines and derivatives as sos1 inhibitors. WO2018115380A1.

[2]. Marco H Hofmann, et al. Abstract PL06-01: Discovery of BI-3406: A potent and selective SOS1::KRAS inhibitor opens a new approach for treating KRAS-driven tumors. December 2019.

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BI-3406 [2230836-55-0]

Cat# HY-125817-1ml

Brand : MedChemExpress

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