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BI-3406

KRAS and Son of Sevenless 1 (SOS1), KRAS BI3406, SOS1 BI3406

Catalog No. Product Name Size List Price (US$) Quantity
APIM050400 BI-3406 5 mg 250.00
APIM050400 BI-3406 10 mg 500.00
APIM050400 BI-3406 50 mg 1800.00
APIM050400 BI-3406 100 mg 3000.00
Description

APIM050400: BI-3406 (BI3406)

A potent and selective inhibitor of the interaction between KRAS and SOS1.
CAS No.: 2230836-55-0
IUPAC/Chemical Name: N-((R)-1-(3-amino-5-(trifluoromethyl)phenyl)ethyl)-7-methoxy-2-methyl-6-(((S)-tetrahydrofuran-3-yl)oxy)quinazolin-4-amine
Molecular Formula: C23H25F3N4O3
Molecular Weight: 462.46
Purity: >99.5%
QC: Achiral and Chiral HPLCs, MS, NMR, and Quantitative Elemental Analysis Report
Solubility: Soluble in DMSO (37.0 mg/ml, 80 mM)
Storage: Store at 0 °C (short term), -20 °C (long term), Desiccated

Note: Please contact us for COA, Spectra, and SDS information.

Background Information:

KRAS functions as a molecular switch, cycling between inactive (GDP-bound) and active (GTP-bound) states to transduce extracellular signals via cell-surface receptors. KRAS signaling occurs through engagement with effector proteins that orchestrate intracellular signaling cascades regulating tumor cell survival and proliferation. Mutations in the KRAS gene occur in approximately one of seven of all human cancers. Up to 90% of pancreatic tumors bear activating KRAS mutations. Direct KRAS blockade has proved challenging, and inhibition of a key downstream effector pathway, the RAF–MEK–ERK cascade, has shown limited success because of activation of feedback networks that keep the pathway in check. SOS1, a KRAS activator and important feedback node, represents an effective approach to treat KRAS-driven cancers. BI-3406 (CAS No. 2230836-55-0) is a highly potent, selective, and orally bioavailable 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"""

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