BI-3406

Based on 14 reference(s) in Google Scholar 8 10 14

Axon 3471

CAS [2230836-55-0]

MF C23H25F3N4O3
MW 462.46

  • Purity: 99%
  • Optical purity: 99% d.e.
  • Soluble in DMSO
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BI-3406

Description

BI-3406 is an orally bioavailable, highly potent and selective KRAS/Son of Sevenless 1 (SOS1) interaction inhibitor (IC50 = 6 nM), binding to the catalytic domain of the guanine nucleotide exchange factor (GEF) SOS1 thereby preventing the interaction with KRAS-GDP. 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. In KRAS-dependent cancers, BI-3406 potently reduces the formation of GTP-loaded KRAS, and inhibits MAPK pathway signaling both in vitro and in vivo. Down-modulation of this signaling cascade by BI-3406 in KRAS G12 or G13 mutant cells effectively limits cell proliferation. As a monotherapy, BI-3406 modulates signaling, as assessed by p-ERK and target genes, and displays marked anti-tumor efficacy in KRAS mutant xenografts.

* Sold in collaboration with Chemietek.

KEYWORDS: BI-3406 | Suppliers | KRAS-SOS1 inhibitor | BI3406 | BI 3406 | CT-BI3406 | CAS [2230836-55-0] | GTP | KRAS | Inhibitor | Enzymes

The purity of Axon Ligands™ is confirmed by HPLC-MS, 1H-NMR and/or microanalysis. Analytical data are available upon request.

Caution: Axon Ligands™ are not fully tested. They are for research purposes only! Not for human consumption!

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