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Cat. No. M9578
BI-2852 Structure


Size Price Availability
5mg USD 314.1  USD349 Custom Synthesis
10mg USD 492.3  USD547 Custom Synthesis
25mg USD 895.5  USD995 Custom Synthesis
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Quality Control
  • Current batch:
  • Purity >98%
  • COA
  • MSDS
Biological Activity

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.

Conversion of different model animals based on BSA (Value based on data from FDA Draft Guidelines)
Species Mouse Rat Rabbit Guinea pig Hamster Dog
Weight (kg) 0.02 0.15 1.8 0.4 0.08 10
Body Surface Area (m2) 0.007 0.025 0.15 0.05 0.02 0.5
Km factor 3 6 12 8 5 20
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.

Chemical Information
Molecular Weight 516.59
Formula C31H28N6O2
CAS Number 2375482-51-0
Purity >98%
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.

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Abmole Inhibitor Catalog 2017

Keywords: BI-2852, BI2852 supplier, Ras, inhibitors

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