产品详情
简单介绍：
KRAS-C9,K-Ras(G12C)Inhibitor
详情介绍：
Product Information
| Molecular Weight: | 513.78 |
| Formula: | C16H21ClN3O4S |
| Purity: | ≥98% |
| CAS#: | 1469337-91-4 |
| Solubility: | DMSO up to 100 mM |
| Chemical Name: | N-(1-(2-((4-chloro-5-iodo-2-methoxyphenyl)amino)acetyl)piperidin-4-yl)ethenesulfonamide |
| Storage: | Powder: 4oC 1 year. DMSO: 4oC 3 month; -20oC 1 year. |
Biological Activity:
KRAS-C9 is a potent and selective allosteric inhibitor of oncogenic K-Ras(G12C). It irreversibly binds to a common oncogenic mutant K-Ras(G12C) and blocks K-Ras(G12C) interactions, therefore does not affect the wild-type protein. Binding of KRAS-C9 to K-Ras(G12C) disrupts both switch-I and switch-II, subverting the native nucleotide preference to favour GDP over GTP and impairing binding to Raf. It can decrease viability and increase apoptosis of K-Ras(G12C)-containing cancer cell lines. KRAS-C9 provides structure-based validation of a new allosteric regulatory site on Ras that is targetable in a mutant-specific manner.
How to Use:
- In vitro: KRAS-C9 was used at 10 µM final concentration in various in vitro assays.
- In vivo: n/a
Reference:
- 1. Ostrem JM, et al. K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions. (2013) Nature. 503(7477):548-51.
Products are for research use only. Not for human use.
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