BI-2852 is a KRAS inhibitor for the switch I/II pocket. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitors because it binds to a different pocket present in both the active and inactive forms of KRAS. BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells. BI-2852 (10 nM-10 µM; 2 hours) shows a dose-dependent pERK modulation and antiproliferative effect at EC50s of 5.8 µM and 6.7 µM in soft agar and low serum conditions in NCI-H358 cells.
|Body Surface Area (m2)||0.007||0.025||0.15||0.05||0.02||0.5|
|Animal A (mg/kg) = Animal B (mg/kg) multiplied by||Animal B Km|
|Animal A Km|
For example, to modify the dose of Compound A used for a mouse (20 mg/kg) to a dose based on the BSA for a rat, multiply 20 mg/kg by the Km factor for a mouse and then divide by the Km factor for a rat. This calculation results in a rat equivalent dose for Compound A of 10 mg/kg.
|Solubility||DMSO ≥ 37 mg/mL|
|Storage||2-8°C, dry, sealed|
The Small Molecule BI-2852 Induces a Nonfunctional Dimer of KRAS
Timothy H Tran, et al. Proc Natl Acad Sci U S A. 2020 Feb 18;117(7):3363-3364. PMID: 32047043.
|Related Ras Products|
CID-1067700 (ML282) is a competitive inhibitors of nucleotide binding by Ras-related GTPases with a Ki of 13 nM for Rab7.
MLS000532223 is a selective inhibitor of Rho family GTPases, with EC50 ranging from 16 μM to 120 μM.
BI-3406 is a highly potent and selective SOS1::KRAS inhibitor (IC50=6 nM), which selectively binds to SOS1 and blocks the interaction with KRAS, irrespective of the KRAS mutation.
ZT-12-037-01 is a potent, selective, ATP-competitive STK19 inhibitor with IC50 values of 23.96 nM and 27.94 nM for STK19 (WT) and STK19 (D89N), respectively.
MRTX849 (Adagrasib) is a potent, highly selective, oral available KRAS G12C inhibitor.
Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.