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BI-2852

Cat. No. M9578
BI-2852 Structure
Synonym:

BI2852

Size Price Availability
5mg USD 349  USD349 Custom Synthesis
10mg USD 547  USD547 Custom Synthesis
25mg USD 995  USD995 Custom Synthesis
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Quality Control & Documentation
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.

Chemical Information
Molecular Weight 516.59
Formula C31H28N6O2
CAS Number 2375482-51-0
Solubility (25°C) DMSO ≥ 37 mg/mL
Storage 2-8°C, dry, sealed
Conversion of different model animals based on BSA (PMID: 27057123)
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.

References

[1] Timothy H Tran, et al. Proc Natl Acad Sci U S A. The Small Molecule BI-2852 Induces a Nonfunctional Dimer of KRAS

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


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