BI-3406 | SOS1 inhibitor

BI-3406 (2230836-55-0) is a potent (IC50 = 5 nM), selective, and orally bioavailable SOS1 inhibitor.1 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 trametinib1,2 and this combination was able to overcome resistance to the KRAS inhibitors sotorasib and adagrasib3. BI-3406 acted synergistically with the KRAS inhibitor adagrasib in KRAS G12C mutant lung and colorectal cancer models.4

BI-3406 (2230836-55-0)는 강력하고 선택적이며 경구 생체이용가능한 SOS1 억제제입니다. 이 약물은 SOS1과 KRAS의 상호작용을 차단하여 KRAS 활성화를 방지합니다. BI-3406는 다양한 KRAS 돌연변이 대립 유전자를 보유한 여러 암 세포 유형 및 이식된 모델에서 활성을 보였습니다. 또한 MEK 억제제 trametinib과 강력한 시너지 효과를 나타냈으며, KRAS 억제제 sotorasib 및 adagrasib에 대한 저항성을 극복할 수 있었습니다. KRAS G12C 돌연변이 폐암 및 대장암 모델에서 KRAS 억제제 adagrasib와 함께 시너지 작용을 했습니다.

CAS:2230836-55-0

Catalog Number:10-3956

Activity:SOS1 inhibitor

Chemical Names:

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

Molecular Weight:462.47

Molecular Formula:C23H25F3N4O3

Solubility:Soluble in DMSO (>70 mg/ml)

Physical Properties:White solid

Purity:>98% HPLC

NMR: (Conforms)

Storage Temperature:-20°C

Stability:Stable for up to 2 years when stored as supplied @ -20°C. Solutions in DMSO may be stored at -20°C for up to 3 months.

Shipping Code:RT