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Chemical Structure : CFT1946
CAS No.: 2882165-79-7
Catalog No.: 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.
| Packing | Price | Stock | Quantity |
|---|---|---|---|
| 2 mg | $298 | In stock | |
| 5 mg | $498 | In stock | |
| 10 mg | $788 | In stock | |
| 25 mg | Get quote |
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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.
| M.Wt | 958.01 | |
| Formula | C45H49F2N11O9S | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| 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 |
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1. Mathew E. Sowa, et al. Cancer Res (2022) 82 (12_Supplement): 2158.
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