(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 manufacturers
- BI-2852
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- $118.00 / 1mg
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2024-11-19
- CAS:2375482-51-0
- Min. Order:
- Purity: 98.98%
- Supply Ability: 10g
- BI-2852
-
- $118.00 / 1mg
-
2024-11-19
- CAS:2375482-51-0
- Min. Order:
- Purity: 98.98%
- Supply Ability: 10g
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| (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 Basic information |
| (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 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 |
| (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 Usage And Synthesis |
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) | |
| (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 Preparation Products And Raw materials |
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