Free shipping on all orders over $ 500

BI-2852

Cat. No. M9578
BI-2852 Structure
Synonym:

BI2852

Size Price Availability
5mg USD 314.1  USD349 Custom Synthesis
10mg USD 492.3  USD547 Custom Synthesis
25mg USD 895.5  USD995 Custom Synthesis
Free Delivery on orders over USD 500 Bulk Inquiry?

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
References

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)

CID-1067700 (ML282) is a competitive inhibitors of nucleotide binding by Ras-related GTPases with a Ki of 13 nM for Rab7.

MLS000532223

MLS000532223 is a selective inhibitor of Rho family GTPases, with EC50 ranging from 16 μM to 120 μM.

BI-3406

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

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)

MRTX849 (Adagrasib) is a potent, highly selective, oral available KRAS G12C inhibitor.

  Catalog
Abmole Inhibitor Catalog 2017




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

Contact Us

Products are for research use only. Not for human use. We do not sell to patients.
© Copyright 2010-2020 AbMole BioScience. All Rights Reserved.