ACBI3 | pan-KRAS PROTAC | Probechem Biochemicals

Chemical Structure : ACBI3

CAS No.: 2938169-76-5

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ACBI3 (pan-KRAS degrader ACBI3)

货号: 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).

规格	价格	库存
2 mg	￥2580	In stock
5 mg	￥4280	In stock
10 mg	￥7280	In stock
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100 mg		Get quote

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生物&药学活性

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.

物理化学性质&存储条件

分子量	1019.26
分子式	C50H62N14O6S2
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	(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

参考文献

1. Johannes Popow, et al. Targeting cancer with small molecule pan-KRAS degraders. bioRxiv October 26, 2023.

2. Patent WO2023099620 A1.

ACBI3 (pan-KRAS degrader ACBI3)

生物&药学活性

物理化学性质&存储条件

参考文献

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ACBI3 (pan-KRAS degrader ACBI3)

生物&药学活性

物理化学性质&存储条件

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