BI-2852

• 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.

• UNSPSC :

  12352005

• Hazard Statement :

  H302, H315, H319, H335

• Target :

  Ras

• Type :

  Reference compound

• Related Pathways :

  GPCR/G Protein; MAPK/ERK Pathway

• Applications :

  Neuroscience-Neuromodulation

• Field of Research :

  Cancer

• Assay Protocol :

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

• Purity :

  99.46

• 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 Formula :

  C31H28N6O2

• Molecular Weight :

  516.59

• Precautions :

  H302, H315, H319, H335

• 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)

• Scientific Category :

  Reference compound1

• Clinical Information :

  No Development Reported

• Isoform :

  K-Ras

• CAS Number :

  [2375482-51-0]