BI-2852 manufacturers
- BI-2852
-
- $118.00
-
2026-08-15
- CAS:2375482-51-0
- Purity: 98.98%
- Supply Ability: 10g
- BI-2852
-
- $118.00
-
2026-08-15
- CAS:2375482-51-0
- Purity: 98.98%
- Supply Ability: 10g
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| | BI-2852 Basic information |
| Product Name: | BI-2852 | | Synonyms: | (S)-5-hydroxy-3-(2-(((1-((1-methyl-1H-imidazol-4-yl)methyl)-1H-indol-6-yl)methylamino)methyl)-1H-indol-3-yl)isoindolin-1-one;BI-2852;1H-Isoindol-1-one, 2,3-dihydro-5-hydroxy-3-[2-[[[[1-[(1-methyl-1H-imidazol-4-yl)methyl]-1H-indol-6-yl]methyl]amino]methyl]-1H-indol-3-yl]-, (3S)-;BI-2852,Ras,inhibit,BI 2852,Inhibitor,BI2852;BI-2852, 10 mM in DMSO;(3S)-5-Hydroxy-3-[2-[[[1-[(1-methylimidazol-4-yl)methyl]indol-6-yl]methylamino]methyl]-1H-indol-3-yl]-2,3-dihydroisoindol-1-one | | CAS: | 2375482-51-0 | | MF: | C31H28N6O2 | | MW: | 516.59 | | EINECS: | | | Product Categories: | | | Mol File: | 2375482-51-0.mol |  |
| | BI-2852 Chemical Properties |
| Boiling point | 906.5±65.0 °C(Predicted) | | density | 1.41±0.1 g/cm3(Predicted) | | storage temp. | Store at -20°C | | solubility | DMSO:77.5(Max Conc. mg/mL);150.02(Max Conc. mM)
Ethanol:23.0(Max Conc. mg/mL);44.52(Max Conc. mM) | | form | Solid | | pka | 8.95±0.40(Predicted) | | color | Off-white to light yellow | | InChIKey | JYEQLXOWWLNVDX-PMERELPUSA-N | | SMILES | O=C1C2=C([C@H](N1)C3=C(NC4=C3C=CC=C4)CNCC5=CC6=C(C=C5)C=CN6CC7=CN(C=N7)C)C=C(C=C2)O |
| WGK Germany | WGK 3 | | Storage Class | 11 - Combustible Solids |
| | BI-2852 Usage And Synthesis |
| Uses | BI-2852 is a KRAS inhibitor for the switch I/II pocket (SI/II-pocket) by structure-based agent design with nanomolar affinity. BI-2852 is mechanistically distinct from covalent KRASG12C inhibitor (binds to switch II pocket) and binds ten-fold more strongly to active KRASG12D versus KRASwt (740 nM vs 7.5 μM). BI-2852 blocks GEF, GAP, and effector interactions with KRAS, leading to inhibition of downstream signaling and an antiproliferative effect in KRAS mutant cells. | | Biological Activity | BI-2852 is a switch SI/II pocket KRAS inhibitor with nanomolar affinity through structure-based drug design. It is mechanistically distinct from covalent KRASG12C inhibitors (binding switch II), binding to active KRASG12D 10-fold more strongly than KRAS wt (740 nM vs 7.5 μM). BI-2852 blocks GEF, GAP and effector interactions with KRAS, resulting in inhibition of downstream signaling and antiproliferative effects in KRAS mutant cells. | | in vitro | BI-2852 (Compound 1) (10 nM-10 μM; 2 hours) shows a dose-dependent pERK modulation and antiproliferative effect at EC 50 s of 5.8 μM and 6.7 μM in soft agar and low serum conditions in NCI-H358 cells. | | target | | KRAS(G12C) 450 nM (IC 50 ) | KRAS(G12C) < p> 750 nM (Kd) | | | IC 50 | KRAS(G12C): 450 nM (IC50); KRAS(G12C): 750 nM (Kd) | | References | [1] Kessler D, et al. Drugging an undruggable pocket on KRAS. Proc Natl Acad Sci U S A. 2019 Aug 6; 116(32):15823-15829. DOI:10.1073/pnas.1904529116
[2] Dirk Kessler, et al. Drugging all RAS isoforms with one pocket. FUTURE MEDICINAL CHEMISTRY |
| | BI-2852 Preparation Products And Raw materials |
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