(R)-BI-2852

(R)-BI-2852

• CAS Number: 2375482-49-6
• 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)
• Clinical Information: No Development Reported