| Identification | Back Directory | [Name]
ACBI3 | [CAS]
2938169-76-5 | [Synonyms]
ACBI3
(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
2-Pyrrolidinecarboxamide, 1-[(2S)-2-[4-[4-[(3S)-4-[4-[5-[(4S)-2-amino-3-cyano-4,5,6,7-tetrahydro-4-methylbenzo[b]thien-4-yl]-1,2,4-oxadiazol-3-yl]-2-pyrimidinyl]hexahydro-3-methyl-1H-1,4-diazepin-1-yl]butoxy]-1H-1,2,3-triazol-1-yl]-3-methyl-1-oxobutyl]-4-hydroxy-N-[(1R)-2-hydroxy-1-[4-(4-methyl-5-thiazolyl)phenyl]ethyl]-, (2S,4R)- | [Molecular Formula]
C50H62N14O6S2 | [MOL File]
2938169-76-5.mol | [Molecular Weight]
1019.25 |
| Hazard Information | Back Directory | [Uses]
ACBI3 (compound 7) is a PROTAC targeting KRAS. ACBI3 is composed of PROTAC target protein ligand pan-KRAS degrader 1 (HY-162960) (red part), E3 ligase ligand E3 ligase Ligand 43 (HY-401613) (blue part) and PROTAC Linker 1-Bromo-4-(ethynyloxy)butane (HY-169992) (black part), among which the conjugate of E3 ubiquitin ligase ligand + Linker is E3 Ligase Ligand-linker Conjugate 143 (HY-169995). ACBI3 achieves in vivo degradation of oncogenic KRAS, resulting in durable pathway modulation and tumor regressions in KRAS mutant xenograft mouse models[1][2][3]. | [in vivo]
ACBI3 (2 mg/kg i.v. or 30 mg/kg s.c., or 30 mg/kg i.p., once a day for 3 days) achieves in vivo degradation of oncogenic KRAS, resulting in durable pathway modulation and tumor regressions in KRAS mutant xenograft mouse models[1].
| Animal Model: | KRAS mutant xenograft mouse models[1] | | Dosage: | 2 mg/kg i.v. or 30 mg/kg s.c. or 30 mg/kg i.p. | | Administration: | once a day for 3 days | | Result: | Resulted in pronounced tumor regressions with a tumor growth inhibition of 127% in KRAS mutant xenograft mouse models. |
| [References]
[1] Popow J, et al. Targeting cancer with small molecule pan-KRAS degraders[J]. bioRxiv, 2023: 2023.10. 24.563163.
[2] Hamilton G, et al. Development of PROTACS degrading KRAS and SOS1. Oncol Res. 2024 Jul 17;32(8):1257-1264. DOI:10.32604/or.2024.051653
[3] Cox AD, et al. KRAS takes the road to destruction. Science. 2024 Sep 20;385(6715):1274-1275. DOI:10.1126/science.ads2150 |
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| Company Name: |
BOC Sciences
|
| Tel: |
1-631-485-4226; 16314854226 |
| Website: |
https://www.bocsci.com |
| Company Name: |
DC Chemicals
|
| Tel: |
021-58447131 13564518121 |
| Website: |
www.chemicalbook.com/showsupplierproductslist927327/0_en.htm |
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