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BI-2852
$350 – $2,900
Products Details
Product Description
– BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based agent design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitor (binds to switch II pocket) and binds ten-fold more strongly to active KRASG12D versus KRASwt (740 nM vs 7.5 μM). BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells.
Web ID
– HY-126247
Storage Temperature
– 4°C (Powder, stored under nitrogen)
Shipping
– Room Temperature
Applications
– Neuroscience-Neuromodulation
Molecular Formula
– C31H28N6O2
References
– [1]Kessler D, et al. Drugging an undruggable pocket on KRAS. Proc Natl Acad Sci U S A. 2019 Aug 6; 116(32):15823-15829.|[2]Dirk Kessler, et al. Drugging all RAS isoforms with one pocket. FUTURE MEDICINAL CHEMISTRY
CAS Number
– 2375482-51-0
Molecular Weight
– 516.59
Compound Purity
– 99.57
SMILES
– OC(C=C1)=CC([C@@H](C2=C(CNCC3=CC4=C(C=CN4CC5=CN(C)C=N5)C=C3)NC6=CC=CC=C62)N7)=C1C7=O
Clinical Information
– No Development Reported
Research Area
– Cancer
Solubility
– DMSO : 55 mg/mL (ultrasonic)
Target
– Ras
Isoform
– K-Ras
Pathway
– GPCR/G Protein
Product type
– Reference compound
Disclaimer: All products are for Research use only unless clearly stated otherwise on the product datasheet. Datasheets provided on the website are drafts for reference purpose only and you are requested to always refer to the hard copy included in the kit for your experimentation. Agdia Products are available for delivery only in Canada.
