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KRAS-C9, K-Ras(G12C) Inhibitor

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KRAS-C9, K-Ras(G12C) Inhibitor

$139.00
A potent and selective allosteric inhibitor of oncogenic K-Ras(G12C).
Catalog No. Unit Price Qty
M60219-2s 2 mg solid $139.00

Details

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. 

Description

Details

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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