6H05 TFA
- Product Name
- 6H05 TFA
- CAS No.
- 2061344-88-3
- Chemical Name
- 6H05 TFA
- Synonyms
- 6H05 TFA;K-RAS INHIBITOR;6H05 TFA;6H05 (TFA), 10 mM in DMSO;Inhibitor,inhibit,6H05 (TFA),Ras,6H-05 (TFA)
- CBNumber
- CB45419656
- Molecular Formula
- C22H31ClF3N3O4S3
- Formula Weight
- 590.13
- MOL File
- 2061344-88-3.mol
6H05 TFA Property
- storage temp.
- Store at -20°C
- solubility
- DMSO: ≥ 51 mg/mL (86.42 mM)
- form
- A crystalline solid
- color
- White to off-white
N-Bromosuccinimide Price
- Product number
- 17985
- Product name
- 6H05 (trifluoroacetate salt)
- Packaging
- 1mg
- Price
- $49
- Updated
- 2024/03/01
- Product number
- 17985
- Product name
- 6H05 (trifluoroacetate salt)
- Packaging
- 25mg
- Price
- $593
- Updated
- 2024/03/01
- Product number
- 17985
- Product name
- 6H05 (trifluoroacetate salt)
- Packaging
- 5mg
- Price
- $216
- Updated
- 2024/03/01
- Product number
- 17985
- Product name
- 6H05 (trifluoroacetate salt)
- Packaging
- 10mg
- Price
- $333
- Updated
- 2024/03/01
- Product number
- CS-3428
- Product name
- 6H05TFA
- Purity
- 99.55%
- Packaging
- 10mg
- Price
- $294
- Updated
- 2021/12/16
6H05 TFA Chemical Properties,Usage,Production
Description
The Ras family of small GTPases (H-Ras, K-Ras, and N-Ras) function as molecular switches, cycling between a GTP-bound active state and a GDP-bound inactive state, to turn on downstream Raf protein kinases. This initiates complex signaling pathways involved in cell growth, differentiation, and apoptosis. Mutations leading to aberrant Ras activation are frequently associated with various human cancers. 6H05 is a small molecule that allosterically binds to a mutant cysteine on oncogenic K-Ras(G12C), thus inhibiting its function. Binding of 6H05 to K-Ras(G12C) disrupts both switch-I and switch-II, altering the native nucleotide preference to favor GDP over GTP, which impedes binding to Raf. Because 6H05 is selective for mutant Cys-12, it does not affect wild-type K-Ras.
Uses
6H05 TFA is a selective, and allosteric inhibitor of oncogenic mutant K-Ras(G12C). IC50 value: Target: K-Ras G12C 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 [1]. 6H05 can be used as an intermediate for the synthesis of other oncogenic K-Ras(G12C) inhibitors [2].
References
[1] Ostrem JM, et al. K-Ras(G12C) inhibitors allosterically control GTP affinity and effector interactions. Nature. 2013 Nov 28;503(7477):548-51. DOI:10.1038/nature12796
[2] Lu S, et al. Harnessing allostery: a novel approach to drug discovery. Med Res Rev. 2014 Nov;34(6):1242-85. DOI:10.1002/med.21317
6H05 TFA Preparation Products And Raw materials
Raw materials
Preparation Products
6H05 TFA Suppliers
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