product name 6H05
Description: 6H05 is a selective inhibitorof the common oncogenic mutant K-Ras (G12C). 6H05 allosterically modifies and inhibits the oncogenic G12C mutant of highly homologous protein H-Ras, not affecting the wild-type K-Ras. Although it’s necessary to perform continued chemical optimization of 6H05 to be assessed in vivo, preliminary evaluation of 6H05 in lung cancer cell lines suggests that 6H05 shows allele-specific impairment of K-Ras function.
References: Nature. 2013 Nov 28;503(7477):548-51; Med Res Rev. 2014 Nov;34(6):1242-85.
590.14
Formula
C20H30ClN3O2S3.CF3COOH
CAS No.
1469337-95-8
Storage
-20℃ for 3 years in powder form
-80℃ for 2 years in solvent
Solubility (In vitro)
DMSO: 100 mg/mL (169.5 mM)
Water: 100 mg/mL (169.5 mM)
Ethanol: 100 mg/mL (169.5 mM)
Solubility (In vivo)
Synonyms
other peoduct :
| In Vitro |
In vitro activity: 6H05 gives the greatest degree of modification, which allosterically modifies the oncogenic G12C mutant of highly homologous protein H-Ras without affecting wild-type K-Ras. Furthermore, 6H05 can be used as an intermediate for the synthesis of other oncogenic K-Ras(G12C) inhibitors. Kinase Assay: Cell Assay: Although it’s necessary to perform continued chemical optimization of 6H05 to be assessed in vivo, preliminary evaluation of 6H05 in lung cancer cell lines suggests that 6H05 shows allele-specific impairment of K-Ras function[1]. There are questions still need to be illustrated that the selectivity and efficiency of 6H05 in vivo, as well as its effects on the subcellular localization of other farnesylated GTPases should be assessed further. |
|---|---|
| In Vivo | |
| Animal model | |
| Formulation & Dosage | |
| References | Nature. 2013 Nov 28;503(7477):548-51; Med Res Rev. 2014 Nov;34(6):1242-85. |
