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Chemical Structure : ACBI3
CAS No.: 2938169-76-5
Catalog No.: PC-21662Not For Human Use, Lab Use Only.
ACBI3 is a selective, potent and in vivo active pan-KRAS PROTAC degrader, potently degrades 13 out of 17 of the most prevalent oncogenic KRAS alleles (DC50=3.9 nM in GP2d cells).
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|---|---|---|---|
| 2 mg | $398 | In stock | |
| 5 mg | $598 | In stock | |
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| 25 mg | Get quote | ||
| 100 mg | Get quote |
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ACBI3 is a selective, potent and in vivo active pan-KRAS PROTAC degrader, potently degrades 13 out of 17 of the most prevalent oncogenic KRAS alleles (DC50=3.9 nM in GP2d cells).
ACBI3 exhibits potent intracellular VHL engagement, ternary complex formation and ubiquitination translating into overall E3-ligase dependent cellular degradation potency.
ACBI3 is broadly active on cancer cell lines bearing KRAS mutations vs KRAS WT cell lines (IC50, 478 nM vs 8.3 µM, respectively).
ACBI3 (30 mg/kg, daily s.c.) resulted in pronounced tumour regressions with a tumour growth inhibition of 127% in GP2d tumour bearing mice.
ACBI3 effectively acts on the majority of KRAS mutants with high prevalence in cancer patients, and as a result potently inhibit proliferation in KRAS mutant cell lines covering a wide range of tumour types.
| M.Wt | 1019.26 | |
| Formula | C50H62N14O6S2 | |
| Appearance | Solid | |
| Storage |
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| Solubility |
10 mM in DMSO |
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| Chemical Name/SMILES |
(2S,4R)-1-((S)-2-(4-(4-((S)-4-(4-(5-((S)-2-amino-3-cyano-4-methyl-4,5,6,7-tetrahydrobenzo[b]thiophen-4-yl)-1,2,4-oxadiazol-3-yl)pyrimidin-2-yl)-3-methyl-1,4-diazepan-1-yl)butoxy)-1H-1,2,3-triazol-1-yl)-3-methylbutanoyl)-4-hydroxy-N-((R)-2-hydroxy-1-(4-(4-methylthiazol-5-yl)phenyl)ethyl)pyrrolidine-2-carboxamide |
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1. Johannes Popow, et al. Targeting cancer with small molecule pan-KRAS degraders. bioRxiv October 26, 2023.
2. Patent WO2023099620 A1.
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