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BI-2852

Chemical Structure : BI-2852

CAS No.: 2375482-51-0

BI-2852 (BI 2852)

Catalog No.: PC-72332Not For Human Use, Lab Use Only.

BI-2852 (BI 2852) is a potent pan-Ras inhibitor, targets GTP-bound KRAS, binds to KRASG12D with a KD of 740 nM (ITC), inhibits GTP-KRAS G12D binding to effectors like SOS1, CRAF and PI3Kα with an IC50 of 490, 770 and 500 nM.

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Purity & Documentation Purity: >98% (HPLC) Select Batch:

Biological Activity

BI-2852 (BI 2852) is a potent pan-Ras inhibitor, targets GTP-bound KRAS, binds to KRASG12D with a KD of 740 nM (ITC), inhibits GTP-KRAS G12D binding to effectors like SOS1, CRAF and PI3Kα with an IC50 of 490, 770 and 500 nM.
BI-2852 showed pERK(2h) modulation and antiproliferative effects in KRASmut cells (NCI-H358) at 5.8 uM and 6.7 uM, displays an IC50 of 490 nM in a GTP-KRASG12D::SOS1 AlphaScreen (AS) assay leading to low micromolar inhibition of pERK (in H358 cell line).
BI-2852 can serve as an excellent small molecule tool inhibitor of KRAS for testing biological hypotheses in vitro.

Physicochemical Properties

M.Wt C31H28N6O2
Formula 516.605
Appearance Solid
CAS No.
Storage
Solide Powder
-20°C 12 Months; 4°C 6 Months
In Solvent
-80°C 6 Months; -20°C 6 Months
Shipping
Solubility

10 mM in DMSO

Chemical Name/SMILES

(S)-5-Hydroxy-3-(2-((((1-((1-methyl-1H-imidazol-4-yl)methyl)-1H-indol-6-yl)methyl)amino)methyl)-1H-indol-3-yl)isoindolin-1-one

References

1. Kessler D, et al. Proc Natl Acad Sci U S A. 2019 Aug 6;116(32):15823-15829.

2. Tran TH, et al. Proc Natl Acad Sci U S A. 2020 Feb 18;117(7):3363-3364.

3. Kessler D, et al. Future Med Chem. 2020 Nov;12(21):1911-1923.

4. Nomura TK, et al. Cell Chem Biol. 2021 Nov 18;28(11):1581-1589.e6.

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