(R)-BI-2852
Product Specifications
UNSPSC Description
(R)-BI-2852 is the isomer of BI-2852 (HY-126247), and can be used as an experimental control. 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.
Target Antigen
Others
Type
Reference compound
Related Pathways
Others
Field of Research
Cancer
Assay Protocol
https://www.medchemexpress.com/r-bi-2852.html
Purity
97.32
Solubility
DMSO : 55 mg/mL (ultrasonic)
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
Molecular Weight
516.59
References & Citations
[1]Dirk Kessler, et al. Drugging all RAS isoforms with one pocket. FUTURE MEDICINAL CHEMISTRY|[2]Kessler D, et al. Drugging an undruggable pocket on KRAS. Proc Natl Acad Sci U S A. 2019 Aug 6; 116(32):15823-15829.
Shipping Conditions
Room Temperature
Storage Conditions
4°C (Powder, stored under nitrogen)
Product Datasheet
http://file.medchemexpress.com/batch_PDF/HY-126247B/R-BI-2852-DataSheet-MedChemExpress.pdf
Product MSDS
http://file.medchemexpress.com/batch_PDF/HY-126247B/R-BI-2852-SDS-MedChemExpress.pdf
Clinical Information
No Development Reported
CAS Number
2375482-49-6
Available Sizes
Curated Selection
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