BI-3406, SOS1 inhibitor (TBI3956)

Description

Product Details

Formal Name: N-[(1R)-1-[3-Amino-5-(trifluoromethyl)phenyl]ethyl]-7-methoxy-2-methyl-6-[(3S)-oxolan-3-yl]oxyquinazolin-4-amine

Molecular Formula: C₂₃H₂₅F₃N₄O₃

Formula Weight: 462.5

CAS Number: 2230836-55-0

Purity: >98%

Formulation: Powder

Solubility: Soluble in DMSO (up to 70 mg/ml)

Storage: -20°C

Stability: ≥ 2 years.

Applications

SOS1 inhibitor

Functions

Potent (IC₅₀ = 5 nM), selective, and orally bioavailable SOS1 inhibitor. It blocks SOS1 interaction with KRAS preventing activation of KRAS. BI-3406 was active against multiple cancer cell types and xenograft models harboring various KRAS mutant alleles including G12C,V,S,A,and G13D. It displayed strong synergistic effects with the MEK inhibitor trametinib and this combination was able to overcome resistance to the KRAS inhibitors sotorasib and adagrasib. BI-3406 acted synergistically with the KRAS inhibitor adagrasib in KRAS G12C mutant lung and colorectal cancer models.

Application Procedures

First dissolved in DMSO (up to 70 mg/ml), then diluted to aqueous buffer. Solutions in DMSO may be stored at -20°C for up to 3 months.

Research use only.

Additional information

Datasheet:

TBI3956_BI-3406_datasheet

MSDS:

TBI3956_BI-3406_MSDS

Research use only.