BI-2852

• UNSPSC 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.

• Target Antigen:

  Ras

• Type:

  Reference compound

• Related Pathways:

  GPCR/G Protein;MAPK/ERK Pathway

• Field of Research:

  Cancer

• Assay Protocol:

  https://www.medchemexpress.com/bi-2852.html

• Purity:

  99.57

• 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]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

• Shipping Conditions:

  Room Temperature

• Storage Conditions:

  4°C (Powder, stored under nitrogen)

• Clinical Information:

  No Development Reported

• CAS Number:

  2375482-51-0