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首页-小分子抑制剂&激动剂-Cell Cycle/DNA Damage-ATM/ATR-ART0380
ART0380

Chemical Structure : ART0380

CAS No.: 2267316-76-5

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ART0380 (ART-0380, ART 0380)

货号: PC-21873Not For Human Use, Lab Use Only.

ART0380 (ART-0380) is a potent, selective and ATP-competitive ATR kinase inhibitor, inhibits ATR-ATRIP complex enzyme activity with IC50 of 51.7 nM, and phospho-Chk1 IC50 of 22 nM in cell western assay.

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纯度 & COA & 质检文件 纯度: >98% (HPLC)

生物&药学活性

ART0380 (ART-0380) is a potent, selective and ATP-competitive ATR kinase inhibitor, inhibits ATR-ATRIP complex enzyme activity with IC50 of 51.7 nM, and phospho-Chk1 IC50 of 22 nM in cell western assay.
ART0380 shows no effect on downstream markers of the ATR related enzymes ATM, DNA-PKcs, mTOR, and SMG1 at 3 uM in response to DNA damage induced by etoposide in NCI-H460 cells.
ART0380 induces robust inhibition of cell growth (LoVo, EC50=1 uM; NCI-H23, EC50=0.13 uM), with little to no effect in CCD-18Co normal fibroblasts (EC50=6.4 uM).
ART0380 is effective in vivo in cancers with varying types of ATM, showing modulation of pChk1 Ser345 in tumor xenograft tissues
ART0380 (30 or 50 mg/kg) exhibits tumor growth inhibition in mice bearing ATM LOF Granta-519 xenografts.
ART0380 (100 mg/kg) exhibits tumor regression on patient-derived xenograft (PDX) model harboring a deleterious ATM gene variant (p.E473*), which induced a near total loss of ATM protein.

物理化学性质&存储条件

分子量 388.49
分子式 C18H24N6O2S
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

(S)-((2-(2-aminopyridin-4-yl)-6-((R)-3-methylmorpholino)pyrimidin-4-yl)imino)(cyclopropyl)(methyl)-l6-sulfanone

参考文献

1. Pilie PG, et al. Clin Cancer Res. 2024 Feb 28.

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