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首页-抗体药物偶连体和PROTACs-PROTAC-CFT1946
CFT1946

Chemical Structure : CFT1946

CAS No.: 2882165-79-7

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CFT1946 (CFT-1946, CFT 1946)

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

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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2 mg ￥2980 In stock
5 mg ￥4980 In stock
10 mg ￥7880 In stock
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纯度 & COA & 质检文件 纯度: >98% (HPLC) Select Batch:

生物&药学活性

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

FC1=CC=C(NS(=O)(N(C)CC)=O)C(C#N)=C1OC2=CC=C(N=CN(C3CC4(CCN(C(CC5(O)CCN(C6=CC7=C(C(N8C(NC(CC8)=O)=O)=NN7C)C=C6F)CC5)=O)CC4)OC3)C9=O)C9=C2

参考文献

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

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