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CFT1946
Catalog No. T77972Cas No. 2882165-79-7
CFT1946 is a Bifunctional Degradation Activating Compound (BiDAC) degrader that contains a ligand targeting the BRAF kinase domain linked to a cereblon ligand. CFT1946 is able to degrade BRAF V600E (class I), G469A (class II), G466V (class III) mutations and p61-BRAFV600E splice variants while maintaining excellent selectivity for the proteome including WT BRAF and CRAF.
CFT1946
Catalog No. T77972Cas No. 2882165-79-7
CFT1946 is a Bifunctional Degradation Activating Compound (BiDAC) degrader that contains a ligand targeting the BRAF kinase domain linked to a cereblon ligand. CFT1946 is able to degrade BRAF V600E (class I), G469A (class II), G466V (class III) mutations and p61-BRAFV600E splice variants while maintaining excellent selectivity for the proteome including WT BRAF and CRAF.
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Product Introduction
Bioactivity
Chemical Properties
| Description | CFT1946 is a Bifunctional Degradation Activating Compound (BiDAC) degrader that contains a ligand targeting the BRAF kinase domain linked to a cereblon ligand. CFT1946 is able to degrade BRAF V600E (class I), G469A (class II), G466V (class III) mutations and p61-BRAFV600E splice variants while maintaining excellent selectivity for the proteome including WT BRAF and CRAF. |
| In vitro | In A375 cells, CFT1946 effectively degraded BRAFV600E (Emax = 26%; DC50 = 14 nM, 24 hours) and inhibited ERK phosphorylation (IC50 = 11 nM, 24 hours) and cell growth (GI50 = 94 nM, 96 hours), while having no effect on the mutant KRAS-driven cell line HCT116. [2] |
| In vivo | METHODS: CFT1946 (10 mg/kg, orally, twice daily) was used to treat A375 xenograft mice, and tumor growth in the mice was observed. RESULTS: CFT1946 resulted in deeper tumor regression. [2] |
| Molecular Weight | 958 |
| Formula | C45H49F2N11O9S |
| Cas No. | 2882165-79-7 |
Storage & Solubility Information
| Storage | Shipping with blue ice. |
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(mother liquor concentration of 40 mg/mL), if you need to configure a concentration that exceeds the solubility of the product, please contact us first.Preparation method for in vivo formula: Take 50 μL DMSO main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarify
main solution, add 300 μLPEG300 mix well and clarify, then add 50 more μL Tween 80, mix well and clarify, then add 600 more μLddH2O mix well and clarifyFor Reference Only. Please develop an appropriate dissolution method based on your laboratory animals and route of administration.
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