900897-56-5
900897-56-5 structure
- Name: KRAS inhibitor 11
- Chemical Name: 2-[4-(2-Methyl-3,5-diphenylpyrazolo[1,5-a]pyrimidin-7-yl)-1-piperazinyl]ethanol
- CAS Number: 900897-56-5
- Molecular Formula: C25H27N5O
- Molecular Weight: 413.515
- Catalog: Signaling Pathways GPCR/G Protein Ras
- Create Date: 2020-01-11 19:12:55
- Modify Date: 2024-01-19 05:34:38
-
KRAS inhibitor 11 is a first-in-class, high-affinity, noncovalent allosteric KRAS inhibitor, disrupts KRAS-Raf interaction with Kd of 1.2 uM; binds to activated KRAS with sub-micromolar affinity and disrupts effector binding, thereby inhibiting KRAS signaling and cancer cell growth; dose-dependently decreases both p-ERK and p-cRaf levels in BHK cells expressing KRASG12D and KRASG12V, suggesting inhibition of RAS signaling via the MAPK pathway.
| Name | 2-[4-(2-Methyl-3,5-diphenylpyrazolo[1,5-a]pyrimidin-7-yl)-1-piperazinyl]ethanol |
|---|---|
| Synonyms |
2-[4-(2-Methyl-3,5-diphenylpyrazolo[1,5-a]pyrimidin-7-yl)-1-piperazinyl]ethanol
1-Piperazineethanol, 4-(2-methyl-3,5-diphenylpyrazolo[1,5-a]pyrimidin-7-yl)- |
| Description | KRAS inhibitor 11 is a first-in-class, high-affinity, noncovalent allosteric KRAS inhibitor, disrupts KRAS-Raf interaction with Kd of 1.2 uM; binds to activated KRAS with sub-micromolar affinity and disrupts effector binding, thereby inhibiting KRAS signaling and cancer cell growth; dose-dependently decreases both p-ERK and p-cRaf levels in BHK cells expressing KRASG12D and KRASG12V, suggesting inhibition of RAS signaling via the MAPK pathway. |
|---|---|
| References | References 1. McCarthy MJ, et al. ACS Omega. 2019 Feb 28;4(2):2921-2930. View Related Products by Target Ras |
| Density | 1.3±0.1 g/cm3 |
|---|---|
| Molecular Formula | C25H27N5O |
| Molecular Weight | 413.515 |
| Exact Mass | 413.221558 |
| LogP | 2.90 |
| Index of Refraction | 1.672 |