Tagarafdeg (CFT1946, CFT-1946) | mutant BRAF PROTAC | Probechem Biochemicals

Chemical Structure : CFT1946

CAS No.: 2882165-79-7

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CFT1946 (Tagarafdeg, CFT-1946, CFT 1946)

货号: PC-20593Not For Human Use, Lab Use Only.

Tagarafdeg (CFT1946, CFT-1946) is a potent, selective CRBN-based PROTAC degrader of mutant BRAF, selectively degrades BRAF V600E (Class I), G469A (Class II), G466V (Class III) mutations and the p61-BRAFV600E splice variant, but not WT BRAF and CRAF.

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10 mg	￥4580	In stock
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生物&药学活性

Tagarafdeg (CFT1946, CFT-1946) is a potent, selective CRBN-based PROTAC degrader of mutant BRAF, selectively degrades BRAF V600E (Class I), G469A (Class II), G466V (Class III) mutations and the p61-BRAFV600E splice variant, but not WT BRAF and CRAF.
CFT1946 potently degraded BRAFV600E in A375 cells (DC50=14 nM at 24hr), inhibited ERK phosphorylation (IC50=11nM at 24hr) and cell growth (GI50=94nM at 96hr) while having no effect in the mutant KRAS driven cell line HCT116.
CFT1946 (10 mg/kg PO BID) resulted in deeper tumor regressions in A375 xenografts.
CFT1946 degraded BRAFV600E and caused robust tumor growth inhibition in engineered A375-BRAFV600E/NRASQ61K double mutant model of BRAF inhibitor resistance, caused tumor regressions when combined with the MEK inhibitor, trametinib.
CFT1946, but not Encorafenib (Cat. PC-49770), inhibited proliferation of the BRAFG466V heterozygous lung tumor cell line H1666.

物理化学性质&存储条件

分子量	958.01
分子式	C45H49F2N11O9S
外观性状	Solid
CAS No.
储存条件	固体粉末 -20°C 12 个月; 4°C 6 个月	配置液 -80°C 6 个月; -20°C 6 个月
Shipping
Solubility	10 mM in DMSO
Chemical Name/SMILES	N'-[2-Cyano-4-fluoro-3-[[3-[(3R)-8-[2-[1-[5-fluoro-1-methyl-3-(tetrahydro-2,4-dioxo-1(2H)-pyrimidinyl)-1H-indazol-6-yl]-4-hydroxy-4-piperidinyl]acetyl]-1-oxa-8-azaspiro[4.5]dec-3-yl]-3,4-dihydro-4-oxo-6-quinazolinyl]oxy]phenyl]-N-ethyl-N-methylsulfamide

参考文献

1. Mathew E. Sowa, et al. Cancer Res (2022) 82 (12_Supplement): 2158.

CFT1946 (Tagarafdeg, CFT-1946, CFT 1946)

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CFT1946 (Tagarafdeg, CFT-1946, CFT 1946)

生物&药学活性

物理化学性质&存储条件

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